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  • 1.
    Abd El-Gaber, Amira S.
    et al.
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm, Egypt.
    El Gendy, Abdel Nasser G.
    Natl Res Ctr, Med & Aromat Plants Res Dept, 33 El Bohouth St,PO 12622, Giza, Egypt.
    Elkhateeb, Ahmed
    Natl Res Ctr, Phytochem & Plant Systemat Dept, 33 El Bohouth St,PO 12622, Giza, Egypt.
    Saleh, Ibrahim A.
    Natl Res Ctr, Phytochem Dept, 33 El Bohouth St,PO 12622, Giza, Egypt.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm, Egypt;Univ Karachi, ICCBS, Karachi 75270, Pakistan.
    Microwave Extraction of Essential Oil from Anastatica hierochuntica (L): Comparison with Conventional Hydro-Distillation and Steam Distillation2018In: Journal of Essential Oil-Bearing Plants (JEOBP), ISSN 0972-060X, E-ISSN 0976-5026, Vol. 21, no 4, p. 1003-1010Article in journal (Refereed)
    Abstract [en]

    This article stands to introduce microwave assisted extraction (MAE) as a more effective method for extraction of Anastatica hierochuntica (L) essential oils (EOs) compared to traditional hydrodistillation (HD) and steam distillation (SD) methods. Analysis of EOs by gas chromatography-mass spectrometry (GC/MS) showed significant differences in the constituents and percentages of the obtained oils. Using MAE and HD obtained oxygenated monoterpenes 50.79 % whereas SD obtained sesquiterpene hydrocarbons 79.84 % as major contents of the extracted oils. This is the first report of EO composition of the aerials parts of A. heirochunatica. It offered several advantages of MAE technique as a green method with shorter extraction time (60 min) and better yield.

  • 2.
    Abdelmoniem, Amr M.
    et al.
    Cairo Univ, Dept Chem, Fac Sci, Giza, Egypt.
    Elnagdi, Mohamed H.
    Cairo Univ, Giza, Egypt;Kuwait Univ, Safat, Kuwait.
    Elsehemy, Mohamed S.
    Cairo Univ, Dept Chem, Fac Pharm, Giza, Egypt.
    El-Seedi, Hesham R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt.
    Abdelhamid, Ismail A.
    Cairo Univ, Dept Chem, Fac Sci, Giza, Egypt.
    Synthesis, Chemistry and Utilities of Diaminoazoles with Special Reference to 3,5-Diaminopyrazoles2018In: Current Organic Synthesis, ISSN 1570-1794, E-ISSN 1875-6271, Vol. 15, no 4, p. 487-514Article, review/survey (Refereed)
    Abstract [en]

    Background: Although the chemistry of heteroaromatic monoamino azoles has been surveyed more than once in the last decade, the chemistry of the di- and triaminoazoles has not been reviewed. In this article we will survey the synthesis, chemistry and utility of the diaminoazoles. In this review, the chemistry of the diaminoazoles as well as their most important utilities will be surveyed. Objective: The review focuses on recent progress in diaminoazoles (i.e. diaminopyrazoles, diaminoimidazoles, diaminotriazoles and diaminothiazole) with especial references to diaminopyrazoles. The synthesis as well as pharmaceutical utilities are reported. There are several methods for synthesis of diaminopyrazoles. 3,5-Diaminopyrazole and its derivatives are prepared through the reaction of malononitrile or arylhydrazononitrile with hydrazine derivatives. 3,4-Diaminopyrazoles are prepared via nitration of 3-aminopyrazole with subsequent reduction of the produced compound. The diaminopyrazoles have several applications in cosmetic and pharmaceutical industries. They also have useful utilities as a constituent in oxidative hair dyes. Conclusion: We managed to report the common methods for the synthesis of diaminoazoles with especial reference to aminopyrazoles that are prepared through the reaction of malononitrile or hydrazononitriles with hydrazine derivatives. Some important applications that include pharmaceutical utilities such as hair dye constituents are reported.

  • 3.
    Aboye, Teshome L.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Gunasekera, Sunithi
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Bruhn, Jan G.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Rosengren, K. Johan
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    A Cactus-Derived Toxin-Like Cystine Knot Peptide with Selective Antimicrobial Activity2015In: ChemBioChem (Print), ISSN 1439-4227, E-ISSN 1439-7633, Vol. 16, no 7, p. 1068-1077Article in journal (Refereed)
    Abstract [en]

    Naturally occurring cystine knot peptides show a wide range of biological activity, and as they have inherent stability they represent potential scaffolds for peptide-based drug design and biomolecular engineering. Here we report the discovery, sequencing, chemical synthesis, three-dimensional solution structure determination and bioactivity of the first cystine knot peptide from Cactaceae (cactus) family: Ep-AMP1 from Echinopsis pachanoi. The structure of Ep-AMP1 (35 amino acids) conforms to that of the inhibitor cystine knot (or knottin) family but represents a novel diverse sequence; its activity was more than 500 times higher against bacterial than against eukaryotic cells. Rapid bactericidal action and liposome leakage implicate membrane permeabilisation as the mechanism of action. Sequence homology places Ec-AMP1 in the plant C6-type of antimicrobial peptides, but the three dimensional structure is highly similar to that of a spider neurotoxin.

  • 4. Al-Henhena, Nawal
    et al.
    Ying, Rozaida Poh Yuen
    Ismail, Salmah
    Najm, Wala
    Khalifa, Shaden A. M.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Abdulla, Mahmood Ameen
    Chemopreventive Efficacy of Andrographis paniculata on Azoxymethane-Induced Aberrant Colon Crypt Foci In Vivo2014In: PLoS ONE, ISSN 1932-6203, E-ISSN 1932-6203, Vol. 9, no 11, article id e111118Article in journal (Refereed)
    Abstract [en]

    Andrographis paniculata is a grass-shaped medicinal herb, traditionally used in Southeast Asia. The aim of this study was to evaluate the chemoprotective effects of A. paniculata on colorectal cancer. A. paniculata ethanol extract was tested on azoxymethane (AOM)-induced aberrant crypt foci (ACF) in vivo and in vitro. A. paniculata treated groups showed a significant reduction in the number of ACF of the treated rats. Microscopically, ACF showed remarkably elongated and stratified cells, and depletion of the submucosal glands of AOM group compared to the treated groups. Histologically, staining showed slightly elevated masses above the surrounding mucosa with oval or slit-like orifices. Immunohistochemically, expression of proliferating cell nuclear antigen (PCNA) and beta-catenin protein were down-regulated in the A. paniculata treated groups compared to the AOM group. When colon tissue was homogenized, malondialdehyde (MDA) and nitric oxide (NO) levels were significantly decreased, whereas superoxide dismutase (SOD) activity was increased in the treated groups compared to the AOM group. A. paniculata ethanol extract showed antioxidant and free radical scavenging activity, as elucidated by the measure of oxidative stress markers. Further, the active fractions were assessed against cell lines of CCD841 and HT29 colon cancer cells.

  • 5.
    Ali, Sara E.
    et al.
    German Univ Cairo, Fac Pharm & Biotechnol, Dept Pharmaceut Biol, New Cairo 12613, Egypt.
    El Gedaily, Rania A.
    Cairo Univ, Fac Pharm, Pharmacognosy Dept, Kasr el Aini St, Cairo 11562, Egypt.
    Mocan, Andrei
    Iuliu Hatieganu Univ Med & Pharm, Dept Pharmaceut Bot, Cluj Napoca 400337, Romania.
    Farag, Mohamed A.
    Cairo Univ, Fac Pharm, Pharmacognosy Dept, Kasr el Aini St, Cairo 11562, Egypt;Amer Univ Cairo, Sch Sci & Engn, Dept Chem, New Cairo 11835, Egypt.
    El-Seedi, Hesham R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Fac Sci, Shibin Al Kawm 32512, Egypt.
    Profiling Metabolites and Biological Activities of Sugarcane (Saccharum officinarum Linn.) Juice and Its Product Molasses via a Multiplex Metabolomics Approach2019In: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 24, no 5, article id 934Article in journal (Refereed)
    Abstract [en]

    Sugarcane (Saccharum officinarum L.) is an important perennial grass in the Poaceae family cultivated worldwide due to its economical and medicinal value. In this study, a combined approach using mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy was employed for the large-scale metabolite profiling of sugarcane juice and its by-product molasses. The polyphenols were analysed via UPLC-UV-ESI-MS, whereas the primary metabolites such as sugars and organic and amino acids were profiled using NMR spectroscopy and gas chromatography/mass spectrometry (GC/MS). UPLC/MS was more effective than NMR spectroscopy or GC/MS for determining differences among the metabolite compositions of the products. Under the optimized conditions, UPLC/MS led to the identification of 42 metabolites, including nine flavonoids, nine fatty acids, and two sterols. C/O Flavone glycosides were the main subclass detected, with tricin-7-O-deoxyhexosyl glucuronide being detected in sugarcane and molasses for the first time. Based on GC/MS analysis, disaccharides were the predominant species in the sugarcane juice and molasses, with sucrose accounting for 66% and 59%, respectively, by mass of all identified metabolites. The phenolic profiles of sugarcane and molasses were further investigated in relation to their in vitro antioxidant activities using free radical scavenging assays such as 2,2-Diphenyl-1-picrylhydrazyl free radical-scavenging ability (DPPH), Trolox equivalent antioxidant capacity (TEAC) and ferric reducing antioxidant power (FRAP). In view of its higher total phenolic content (TPC) (196 +/- 2.1 mg GAE/100 g extract) compared to that of sugarcane juice (93 +/- 2.9 mg GAE/100 g extract), molasses exhibited a substantially higher antioxidant effect. Interestingly, both extracts were also found to inhibit alpha-glucosidase and alpha-amylase enzymes, suggesting a possible antihyperglycaemic effect. These findings suggest molasses may be a new source of natural antioxidants for functional foods.

  • 6.
    Amir, Mohd.
    et al.
    Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India.
    Kumar, Vijay
    Amity Univ Noida, Amity Inst Neuropsychol & Neurosci, Noida, UP, India.
    Dohare, Ravins
    Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India;King Saud Univ, Dept Pharmacogmosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    Rehman, Md. Tabish
    King Saud Univ, Dept Pharmacogmosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    Hussain, Afzal
    King Saud Univ, Dept Pharmacogmosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    Alajmi, Mohamed F.
    King Saud Univ, Dept Pharmacogmosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Hassan, Hani Mutlak A.
    King Abdulaziz Univ, King Fand Med Res Ctr, POB 80216, Jeddah 21589, Saudi Arabia;King Abdulaziz Univ, Fac Appl Med Sci, Dept Med Lab Technol, POB 80216, Jeddah 21589, Saudi Arabia.
    Islam, Asimul
    Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India.
    Ahmad, Faizan
    Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India.
    Hassan, Md. Imtaiyaz
    Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India.
    Investigating architecture and structure-function relationships in cold shock DNA-binding domain family using structural genomics-based approach2019In: International Journal of Biological Macromolecules, ISSN 0141-8130, E-ISSN 1879-0003, Vol. 133, p. 484-494Article in journal (Refereed)
    Abstract [en]

    Oligonucleotide/oligosaccharide-binding fold (OB-fold) plays a major role in the regulation of central dogma of life via binding though DNA and RNA. The OB-fold domains are diverse in nature and present in large number of proteins with verities of molecular functions. Here, we have investigated the distribution of sequence, structure and repeats of cold shock DNA-binding proteins (CSDB), a member of OB-fold, in all three kingdoms to establish functional relationships. The CSDB is consists of 30 domains with a major contribution of S1 (>110,601 sequences), S12 (>23,760 sequences), S17 (>14,833 sequences) and S28e (>1615 sequence) domains. These domains are largely found in bacteria (70-90%). The number of S1 domain repeats in eukaryota varies from 1 to 15 and are well-correlated with the protein size. The molecular function analysis suggests that a large number of repeats in the S1 domain are involved in diverse molecular functions in bacteria and eukaryotes. In-depth structure analysis of Si, S12, S17 and S28e domain-containing proteins of the OB-fold family provides a reasonable basis to understand the relationship of size and number of repeats with the corresponding molecular functions.

  • 7.
    Aneja, Babita
    et al.
    Jamia Millia Islamia, Dept Biosci, New Delhi 110025, India;Jamia Millia Islamia, Dept Chem, New Delhi 110025, India.
    Khan, Nashrah Sharif
    Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India;Jamia Millia Islamia, Dept Biotechnol, New Delhi 110025, India.
    Khan, Parvez
    Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India.
    Queen, Aarfa
    Jamia Millia Islamia, Dept Chem, New Delhi 110025, India.
    Hussain, Afzal
    King Saud Univ, Coll Pharm, Dept Pharmacognosy, Riyadh 11451, Saudi Arabia.
    Rehman, Md. Tabish
    King Saud Univ, Coll Pharm, Dept Pharmacognosy, Riyadh 11451, Saudi Arabia.
    Alajmi, Mohamed F.
    King Saud Univ, Coll Pharm, Dept Pharmacognosy, Riyadh 11451, Saudi Arabia.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Ali, Sher
    Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India.
    Hassan, Md. Imtaiyaz
    Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India.
    Abid, Mohammad
    Jamia Millia Islamia, Dept Biosci, New Delhi 110025, India.
    Design and development of Isatin-triazole hydrazones as potential inhibitors of microtubule affinity-regulating kinase 4 for the therapeutic management of cell proliferation and metastasis2019In: European Journal of Medicinal Chemistry, ISSN 0223-5234, E-ISSN 1768-3254, Vol. 163, p. 840-852Article in journal (Refereed)
    Abstract [en]

    Microtubule affinity-regulating kinase 4 (MARK4) is a potential drug target as the same is found to be over expressed in several types of cancers. In search of effective MARK4 inhibitors, we have synthesized and characterized Isatin-triazole hydrazones (9a-i) and evaluated their inhibitory potential. Of all the compounds, 9g showed better binding affinity and enzyme inhibition potential in sub micromolar range. Human serum albumin (HSA) binding assay suggested an easy transportation of 9g in blood stream due to its binding affinity. In vitro anticancer studies performed on MCF-7, MDA-MB-435s and HepG2 cells using 9g showed inhibition of cell proliferation and cell migration. Further, 9g induces apoptosis in these cancerous cells, with IC50 values of 6.22, 9.94 and 8.14 mu M, respectively. Putatively, 9g seems to cause oxidative stress resulting in apoptosis. Functional assay of 9g with a panel of 26 kinases showed MARK4 specific profile. In conclusion, 9g seems to possess an effective inhibitory potential towards MARK4 adding an additional repertoire to anticancer therapeutics.

  • 8.
    Benchoula, Khaled
    et al.
    Int Islamic Univ Malaysia, Kulliyyah Pharm, Dept Basic Med Sci, Kuantan 25200, Pahang, Malaysia.
    Khatib, Alfi
    Int Islamic Univ Malaysia, Kulliyyah Pharm, Dept Pharmaceut Chem, Kuantan 25200, Pahang, Malaysia.
    Quzwain, Fairuz M. C.
    Univ Jambi, Fac Med, Jambi 36122, Indonesia.
    Mohamad, Che Anuar Che
    Int Islamic Univ Malaysia, Kulliyyah Pharm, Dept Basic Med Sci, Kuantan 25200, Pahang, Malaysia.
    Sulaiman, Wan Mohd Azizi Wan
    Int Islamic Univ Malaysia, Kulliyyah Pharm, Dept Basic Med Sci, Kuantan 25200, Pahang, Malaysia.
    Wahab, Ridhwan Abdul
    Int Islamic Univ Malaysia, Dept Biomed Sci, Kulliyyah Allied Hlth Sci, Kuantan 25200, Pahang, Malaysia.
    Ahmed, Qamar Uddin
    Int Islamic Univ Malaysia, Kulliyyah Pharm, Dept Pharmaceut Chem, Kuantan 25200, Pahang, Malaysia.
    Ghaffar, Majid Abdul
    Int Islamic Univ Malaysia, Kulliyyah Pharm, Dept Pharmaceut Chem, Kuantan 25200, Pahang, Malaysia.
    Saiman, Mohd Zuwairi
    Univ Malaya, Inst Biol Sci, Fac Sci, Kuala Lumpur 50603, Malaysia.
    Alajmi, Mohamed F.
    King Saud Univ, Dept Pharmacognosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Optimization of Hyperglycemic Induction in Zebrafish and Evaluation of Its Blood Glucose Level and Metabolite Fingerprint Treated with Psychotria malayana Jack Leaf Extract2019In: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 24, no 8, article id 1506Article in journal (Refereed)
    Abstract [en]

    A standard protocol to develop type 1 diabetes in zebrafish is still uncertain due to unpredictable factors. In this study, an optimized protocol was developed and used to evaluate the anti-diabetic activity of Psychotria malayana leaf. The aims of this study were to develop a type 1 diabetic adult zebrafish model and to evaluate the anti-diabetic activity of the plant extract on the developed model. The ability of streptozotocin and alloxan at a different dose to elevate the blood glucose levels in zebrafish was evaluated. While the anti-diabetic activity of P. malayana aqueous extract was evaluated through analysis of blood glucose and LC-MS analysis fingerprinting. The results indicated that a single intraperitoneal injection of 300 mg/kg alloxan was the optimal dose to elevate the fasting blood glucose in zebrafish. Furthermore, the plant extract at 1, 2, and 3 g/kg significantly reduced blood glucose levels in the diabetic zebrafish. In addition, LC-MS-based fingerprinting indicated that 3 g/kg plant extract more effective than other doses. Phytosterols, sugar alcohols, sugar acid, free fatty acids, cyclitols, phenolics, and alkaloid were detected in the extract using GC-MS. In conclusion, P. malayana leaf aqueous extract showed anti-diabetic activity on the developed type 1 diabetic zebrafish model.

  • 9.
    Boldbaatar, Delgerbat
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    El-Seedi, Hesham R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Findakly, Meriana
    Jabri, Safa
    Javzan, Batkhuu
    Choidash, Battsetseg
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Hellman, Bjorn
    Antigenotoxic and antioxidant effects of the Mongolian medicinal plant Leptopyrum fumarioides (L): An in vitro study2014In: Journal of Ethnopharmacology, ISSN 0378-8741, E-ISSN 1872-7573, Vol. 155, no 1, p. 599-606Article in journal (Refereed)
    Abstract [en]

    Ethnopharmacological relevance: Leptopyrum fumarioides has been used in the traditional medicine of Mongolia for the treatment of various diseases, including drug intoxications. However, since there is only sparse information about its chemistry, active components, and pharmacological and toxicological effects, the major aim of the present study employing mouse lymphoma cells was to evaluate the genotoxic and antigenotoxic/antioxidative effects of extracts and components isolated from this plant. Material and methods: A crude methanol extract was separated into three different sub-extracts: dichloromethane, n-butanol, and water. The major constituent of the n-butanol extract, i.e., the flavone luteolin-7-O-glucoside and a mixture of the most abundant compounds in the dichloromethane sub-extract were then isolated. DNA damage was evaluated using the comet assay; the antioxidant activity was evaluated using the DPPH radical scavenging assay. Results: The crude methanol extract, the dichloromethane sub-extract and the mixture of compounds isolated from the latter fraction, increased the level of DNA damage after three hours of exposure. In contrast, no increase in DNA damage was observed in the cells that had been exposed to the n-butanol and water sub-extracts, or to the pure flavone. When non-DNA damaging concentrations of extracts and compounds were tested together with the DNA damaging agent catechol, all sub-extracts were found to reduce the catechol-induced DNA damage (the flavone was then found to be the most effective protective agent). The n-butanol sub-extract and the flavone were also found to have the most prominent antioxidative effects. Conclusion: Based on the results from the present study, components in Leptopyrum fumarioides were found to protect the DNA damage induced by catechol, probably by acting as potent antioxidants.

  • 10.
    Bruhn, Jan G.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    De Smet, Peter A. G. M.
    El-Seedi, Hesham R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Beck, Olof
    Mescaline use for 5700 years2002In: The Lancet, ISSN 0140-6736, E-ISSN 1474-547X, Vol. 359, no 9320, p. 1866-Article in journal (Refereed)
    Abstract [en]

    Archaeological investigations in northeast Mexico and Trans-Pecos, Texas have shown that the use of psychotropic drugs in this region goes back to around 8500 BC. The aboriginal inhabitants of this region used the mescal bean, Sophora secundiflora, and buttons from the peyote cactus, Lophophora williamsii1.

    From an archaeological site in Coahuila, Mexico, several peyote buttons were retrieved and radiocarbon-dated to AD 810–1070. Alkaloid analysis revealed the presence of mescaline and four related tetrahydroisoquinoline alkaloids2. We have, however, analysed two much older samples of peyote buttons. These samples are thought to have been found in Shumla Cave number five on the Rio Grande, TX, USA, and are in the collection of the Witte Museum in San Antonio3. Radiocarbon dating showed a mean age of 5700 years.

    Standard alkaloid extraction procedures done on the samples gave residues that were analysed by thin-layer chromatography and gas chromatography-mass spectrometry. We were able to identify mescaline in both samples, based on identical retention times and Rf values, and similar mass-to-charge ratios and fragmentation pattern. The detection of mescaline in two different samples, both analysed by two methods based on different principles, is reliable evidence for the presence of this psychotropic drug.

    Freshly prepared peyote buttons can contain up to 8% of total alkaloids. The previously studied 1000-year-old sample had a lower content, around 2·25%. In our analysis, alkaloid content had fallen to 2%, and mescaline was the only peyote alkaloid we could identify. There was no trace of any of the other tetrahydroisoquinoline alkaloids typical for peyote.

    Earlier, nicotine and caffeine had been identified in plant remains from a medicine man's tomb in Bolivia, aged 1600 years4. Morphine has been found in a 3500 year old ceramic container from Cyprus5.

    From a scientific perspective, the studied peyote material seems to be the oldest plant drug that yielded a major bioactive compound on chemical analysis. From a cultural point of view, our identification of mescaline strengthens the evidence that Native Americans already recognised and valued the psychotropic properties of peyote as long as 5700 years ago.

  • 11.
    Channar, Pervaiz Ali
    et al.
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Saeed, Aamer
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Larik, Fayaz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Batool, Bakhtawar
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Kalsoom, Saima
    Int Islamic Univ, SA CIRBS, Islamabad, Pakistan.
    Hasan, M. M.
    PIEAS, Islamabad, Pakistan.
    Erben, Mauricio F.
    UNLP, CONICET, Fac Ciencias Exactas, CEQUINOR,CCT La Plata,Dept Quim, CC 962, RA-1900 La Plata, Buenos Aires, Argentina.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Ali, Musrat
    Quaid I Azam Univ, Dept Biol Sci, Islamabad 45320, Pakistan.
    Ashraf, Zaman
    Allama Iqbal Open Univ, Dept Chem, Islamabad 44000, Pakistan.
    Synthesis of aryl pyrazole via Suzuki coupling reaction, in vitro mushroom tyrosinase enzyme inhibition assay and in silico comparative molecular docking analysis with Kojic acid2018In: Bioorganic chemistry (Print), ISSN 0045-2068, Vol. 79, p. 293-300Article in journal (Refereed)
    Abstract [en]

    Aryl pyrazoles are well recognized class of heterocyclic compounds found in several commercially available drugs. Owing to their significance in medicinal chemistry, in this current account we have synthesized a series of suitably substituted aryl pyrazole by employing Suzuki cross-coupling reaction. All compounds were evaluated for inhibition of mushroom tyrosinase enzyme both in vitro and in silico. Compound 3f (IC50 = 1.568 +/- 0.01 mu M) showed relatively better potential compared to reference kojic acid (IC50 = 16.051 +/- 1.27 mu M). A comparative docking studies showed that compound 3f have maximum binding affinity against mushroom tyrosinase (PDBID: 2Y9X) with binding energy value (-6.90 kcal/mol) as compared to Kojic acid. The 4-methoxy group in compound 3f shows 100% interaction with Cu. Compound 3f displayed hydrogen binding interaction with His61 and His94 at distance of 1.71 and 1.74 angstrom which might be responsible for higher activity compared to Kojic acid.

  • 12.
    Chen, Lei
    et al.
    Fujian Agr & Forestry Univ, Coll Food Sci, Fuzhou, Fujian, Peoples R China.
    Gnanaraj, Charles
    Univ Tunku Abdul Rahman, Fac Sci, Dept Chem Sci, Jalan Univ, Kampar, Perak, Malaysia.
    Arulselvan, Palanisamy
    Muthayammal Coll Arts & Sci, Muthayammal Ctr Adv Res, Namakkal, Tamil Nadu, India;Scigen Res & Innovat Pvt Ltd, Periyar Technol Business Incubator, Thanjavur, Tamil Nadu, India.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Teng, Hui
    Fujian Agr & Forestry Univ, Coll Food Sci, Fuzhou, Fujian, Peoples R China.
    A review on advanced microencapsulation technology to enhance bioavailability of phenolic compounds: Based on its activity in the treatment of Type 2 Diabetes2019In: Trends in Food Science & Technology, ISSN 0924-2244, E-ISSN 1879-3053, Vol. 85, p. 149-162Article, review/survey (Refereed)
    Abstract [en]

    Background: Studies on and the application of polyphenolic compounds, have recently attracted great interest in the functional foods due to their potential health benefits to humans. However, the major disadvantage associated with phenolic compounds is their constrained bioavailability, mainly caused by its low aqueous solubility, poor stability and limited membrane permeability.

    Scope and approach: The aim of this study is to give an overview of the microencapsulation technology to enhance bioavailability of phenolic compounds. Furthermore, the anti-diabetic effect of microencapsulated phenolic compounds and capability of them to produce new functional foods will be discussed.

    Key findings and conclusions: The utilization of microencapsulated polyphenols, instead of free compounds, can effectively alleviate the deficiencies. This review provided valuable insight that may be useful for identifying trends in the commercialization of microencapsulation -technological products or for identifying new research areas. The results published to date confirm that the encapsulation promotes the protection of active compounds, enabling industrial applications of active packaging.

  • 13.
    Chen, Lei
    et al.
    Fujian Agr & Forestry Univ, Coll Food Sci, Fuzhou 350002, Fujian, Peoples R China.
    Lu, Xu
    Fujian Agr & Forestry Univ, Coll Food Sci, Fuzhou 350002, Fujian, Peoples R China.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Teng, Hui
    Fujian Agr & Forestry Univ, Coll Food Sci, Fuzhou 350002, Fujian, Peoples R China.
    Recent advances in the development of sesquiterpenoids in the treatment of type 2 diabetes2019In: Trends in Food Science & Technology, ISSN 0924-2244, E-ISSN 1879-3053, Vol. 88, p. 46-56Article, review/survey (Refereed)
    Abstract [en]

    Background: Treatment of type 2 diabetes mellitus (T2DM) through dietary terpenoids is receiving a promising interest and sesquiterpenoids' importance for food and pharmaceutical industries is mainly based on the existed scientific works. Scope and approach: Sesquiterpenoids might contribute to prevent or delay T2DM by inhibiting key enzymes relevant for hyperglycemia, modulating beta-cells function, targeting insulin signaling route, etc. Sesquiterpenoids also have been demonstrated to stimulate glucose uptake by enhancing glucose transport, repressing glucose production, or improving lipid metabolism. Key findings and conclusions: In this review, we summarized the latest developments of sesquiterpenoids in the treatment of type 2 diabetes as well as sesquiterpenoids-rich herbs against key enzymes relevant to hyperglycemia, and discussed their underlying molecular mechanisms of anti-diabetic potential. We also suggested a better evaluation of the pharmacological profile of sesquiterpenoids and their derivate with a clear-cut choice of possible human pathologies.

  • 14.
    Demma, Jemal
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Engidawork, Ephrem
    Aboye, Teshome Leta
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Hellman, Björn
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
    An in vitro Study on the DNA Damaging Effects of Phytochemicals Partially Isolated from an Extract of Glinus lotoides2013In: Phytotherapy Research, ISSN 0951-418X, E-ISSN 1099-1573, Vol. 27, no 4, p. 507-514Article in journal (Refereed)
    Abstract [en]

    An extract of Glinus lotoides, a medicinal plant used in Africa and Asia for various therapeutic purposes, was recently shown to cause DNA damage in vitro. To further explore the potential genotoxicity of this plant, fractionation of the crude extract was performed using reverse phase solid-phase extraction and a stepwise gradient elution of methanol in water. Four fractions were collected and subsequently analysed for their DNA damaging effects in mouse lymphoma cells using an alkaline version of the comet assay. To identify potential genotoxic and non-genotoxic principles, each fraction was then subjected to liquid chromatography coupled to mass spectrometry, LC-MS/MS. 1D and 2D nuclear magnetic resonance analyses were used to confirm the identity of some saponins. Although fractions containing a mixture of flavonoids and oleanane-type saponins or oleanane-type saponins alone produced no DNA damage, those containing hopane-type saponins exhibited a pronounced DNA damaging effect without affecting the viability of the cells. To conclude, even if this study presents evidence that hopane-type of saponins are endowed with a DNA damaging ability, further studies are needed before individual saponins can be cited as a culprit for the previously reported genotoxicity of the crude extract of G. lotoides.

  • 15.
    Efferth, Thomas
    et al.
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Banerjee, Mita
    Johannes Gutenberg Univ Mainz, Dept English & Linguist, Amer Studies, Ctr Comparat Native & Indigenous Studies, Mainz, Germany.
    Abu-Darwish, Mohammad Sanad
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany;Al Balqa Appl Univ, Shoubak Univ Coll, Salt, Jordan.
    Abdelfatah, Sara
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Böckers, Madeleine
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Bhakta-Guha, Dipita
    SASTRA Univ, Sch Chem & Biotechnol, Thanjavur 613401, TN, India.
    Bolzani, Vanderlan
    Sao Paulo State Univ, Dept Organ Chem, Inst Chem, Araraquara, Brazil.
    Daak, Salah
    Dr Salah Wanesi Fdn Canc Res & Control, Khartoum, Sudan.
    Demirezer, Ömur Lutfiye
    Hacettepe Univ, Fac Pharm, Dept Pharmacognosy, Ankara, Turkey.
    Dawood, Mona
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Efferth, Monika
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Univ Malaya, Chem Dept, Fac Sci, Kuala Lumpur, Malaysia.
    Fischer, Nicolas
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Greten, Henry J.
    Univ Porto, Biomed Sci Inst Abel Salazar, Porto, Portugal;Heidelberg Sch Chinese Med, Heidelberg, Germany.
    Hamdoun, Sami
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Hong, Chunlan
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Horneber, Markus
    Paracelsus Med Univ, Dept Internal Med, Div Hematol & Oncol, Klinikum Nurnberg, Nurnberg, Germany.
    Kadioglu, Onat
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Khalid, Hassan E.
    Univ Khartoum, Dept Pharmacognosy, Khartoum, Sudan.
    Khalid, Sami A.
    Univ Sci & Technol, Fac Pharm, Omdurman, Sudan;Univ Khartoum, Fac Pharm, Karthoum, Sudan.
    Kuete, Victor
    Univ Dschang, Dept Biochem, Fac Sci, Dschang, Cameroon.
    Mahmoud, Nuha
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Marin, Jose
    Univ Salamanca, Dept Biochem & Mol Biol, Expt Hepatol & Drug Targeting HEVEFARM, CIBERehd,IBSAL, Campus Miguel Unamuno, Salamanca 37007, Spain.
    Mbaveng, Armelle
    Univ Dschang, Dept Biochem, Fac Sci, Dschang, Cameroon.
    Midiwo, Jacob
    Univ Nairobi, Dept Chem, Nairobi, Kenya.
    Nakagawa, Hiroshi
    Chubu Univ, Dept Appl Biol Chem, Grad Sch Biosci & Biotechnol, Kasugai, Aichi, Japan.
    Nass, Janine
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Ngassapa, Olipa
    Muhimbili Univ Hlth & Allied Sci, Dar Es Salaam, Tanzania.
    Ochwang'i, Dominic
    Univ Nairobi, Dept Vet Anat & Physiol, Nairobi, Kenya.
    Omosa, Leonida K.
    Univ Nairobi, Dept Chem, Nairobi, Kenya.
    Ooko, Edna A.
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Özenver, Nadire
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Poornima, Paramasivan
    Univ Abertay, Mol & Cellular Pharmacol Lab, Sch Sci Engn & Technol, Dundee, Scotland.
    Rodriguez Romero, Marta
    Univ Salamanca, Dept Biochem & Mol Biol, Expt Hepatol & Drug Targeting HEVEFARM, CIBERehd,IBSAL, Campus Miguel Unamuno, Salamanca 37007, Spain.
    Saeed, Mohamed E. M.
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Salgueiro, Ligia
    Univ Coimbra, Ctr Neurosci & Cell Biol, Coimbra, Portugal;Univ Coimbra, Fac Pharm, Coimbra, Portugal.
    Seo, Ean-Jeong
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Yan, Ge
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Inst Pharm & Biochem, Staudinger Weg 5, D-55128 Mainz, Germany.
    Yasin, Zahir
    Tayba Canc Ctr, Khartoum, Sudan.
    Saeed, Elfatih M.
    Fed Govt Sudan, Khartoum, Sudan.
    Paul, Norbert W.
    Johannes Gutenberg Univ Mainz, Inst Hist Philosophy & Eth Med, Med Ctr, Mainz, Germany.
    Biopiracy versus One-World Medicine-From colonial relicts to global collaborative concepts2019In: Phytomedicine, ISSN 0944-7113, E-ISSN 1618-095X, Vol. 53, p. 319-331Article, review/survey (Refereed)
    Abstract [en]

    Background: Practices of biopiracy to use genetic resources and indigenous knowledge by Western companies without benefit-sharing of those, who generated the traditional knowledge, can be understood as form of neo-colonialism. Hypothesis: The One-World Medicine concept attempts to merge the best of traditional medicine from developing countries and conventional Western medicine for the sake of patients around the globe. Study design: Based on literature searches in several databases, a concept paper has been written. Legislative initiatives of the United Nations culminated in the Nagoya protocol aim to protect traditional knowledge and regulate benefit-sharing with indigenous communities. The European community adopted the Nagoya protocol, and the corresponding regulations will be implemented into national legislation among the member states. Despite pleasing progress, infrastructural problems of the health care systems in developing countries still remain. Current approaches to secure primary health care offer only fragmentary solutions at best. Conventional medicine from industrialized countries cannot be afforded by the impoverished population in the Third World. Confronted with exploding costs, even health systems in Western countries are endangered to burst. Complementary and alternative medicine (CAM) is popular among the general public in industrialized countries, although the efficacy is not sufficiently proven according to the standards of evidence-based medicine. CAM is often available without prescription as over-the-counter products with non-calculated risks concerning erroneous self-medication and safety/toxicity issues. The concept of integrative medicine attempts to combine holistic CAM approaches with evidence-based principles of conventional medicine. Conclusion: To realize the concept of One-World Medicine, a number of standards have to be set to assure safety, efficacy and applicability of traditional medicine, e.g. sustainable production and quality control of herbal products, performance of placebo-controlled, double-blind, randomized clinical trials, phytovigilance, as well as education of health professionals and patients.

  • 16.
    El-Aarag, Bishoy
    et al.
    Menoufia Univ, Fac Sci, Chem Dept, Biochem Div, Shibin Al Kawm 32512, Egypt;Okayama Univ, Grad Sch Nat Sci & Technol, Div Chem & Biotechnol, Okayama 7008530, Japan.
    Magdy, Mohamed
    Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt.
    AlAjmi, Mohamed F.
    King Saud Univ, Dept Pharmacognosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    Khalifa, Shaden A. M.
    Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, S-10691 Stockholm, Sweden.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt;Univ Karachi, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
    Melittin Exerts Beneficial Effects on Paraquat-Induced Lung Injuries in Mice by Modifying Oxidative Stress and Apoptosis2019In: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 24, no 8, article id 1498Article in journal (Refereed)
    Abstract [en]

    Melittin (MEL) is a 26-amino acid peptide with numerous biological activities. Paraquat (PQ) is one of the most widely used herbicides, although it is extremely toxic to humans. To date, PQ poisoning has no effective treatment, and therefore the current study aimed to assess for the first time the possible effects of MEL on PQ-induced lung injuries in mice. Mice received a single intraperitoneal (IP) injection of PQ (30 mg/kg), followed by IP treatment with MEL (0.1 and 0.5 mg/kg) twice per week for four consecutive weeks. Histological alterations, oxidative stress, and apoptosis in the lungs were studied. Hematoxylin and eosin (H&E) staining indicated that MEL markedly reduced lung injuries induced by PQ. Furthermore, treatment with MEL increased superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) activity, and decreased malonaldehyde (MDA) and nitric oxide (NO) levels in lung tissue homogenates. Moreover, immunohistochemical staining showed that B-cell lymphoma-2 (Bcl-2) and survivin expressions were upregulated after MEL treatment, while Ki-67 expression was downregulated. The high dose of MEL was more effective than the low dose in all experiments. In summary, MEL efficiently reduced PQ-induced lung injuries in mice. Specific pharmacological examinations are required to determine the effectiveness of MEL in cases of human PQ poisoning.

  • 17.
    El-Saied, Fathy
    et al.
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt.
    El-Aarag, Bishoy
    Menoufia Univ, Fac Sci, Chem Dept, Biochem Div, Shibin Al Kawm 32512, Egypt;Okayama Univ, Div Chem & Biotechnol, Grad Sch Nat Sci & Technol, Okayama 7008530, Japan.
    Salem, Tarek
    Univ Sadat City, Genet Engn & Biotechnol Inst, Dept Mol Biol, Sadat City 32958, Egypt.
    Said, Ghada
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt.
    Khalifa, Shaden A. M.
    Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, SE-10691 Stockholm, Sweden;Novum, Dept Expt Canc Med ECM, S-14157 Stockholm, Sweden.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt;Jiangsu Univ, Int Res Ctr Food Nutr & Safety, Zhenjiang 212013, Jiangsu, Peoples R China;Al Rayan Coll, Al Rayan Res & Innovat Ctr, Medina 42541, Saudi Arabia.
    Synthesis, Characterization, and In Vivo Anti-Cancer Activity of New Metal Complexes Derived from Isatin-N(4)antipyrinethiosemicarbazone Ligand Against Ehrlich Ascites Carcinoma Cells2019In: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 24, no 18, article id 3313Article in journal (Refereed)
    Abstract [en]

    The current study aimed to synthesize new metal coordination complexes with potential biomedical applications. Metal complexes were prepared via the reaction of isatin-N(4)anti- pyrinethiosemicarbazone ligand 1 with Cu(II), Ni(II), Co(II), Zn(II), and Fe(III) ions. The obtained metal complexes 2-12 were characterized using elemental, spectral (H-1-NMR, EPR, Mass, IR, UV-Vis) and thermal (TGA) techniques, as well as magnetic moment and molar conductance measurements. In addition, their geometries were studied using EPR and UV-Vis spectroscopy. To evaluate the in vivo anti-cancer activities of these complexes, the ligand 1 and its metal complexes 2, 7 and 9 were tested against solid tumors. The solid tumors were induced by subcutaneous (SC) injection of Ehrlich ascites carcinoma (EAC) cells in mice. The impact of the selected complexes on the reduction of tumor volume was determined. Also, the expression levels of vascular endothelial growth factor (VEGF) and cysteine aspartyl-specific protease-7 (caspase-7) in tumor and liver tissues of mice bearing EAC tumor were determined. Moreover, their effects on alanine transaminase (ALT), aspartate transaminase (AST), albumin, and glucose levels were measured. The results revealed that the tested compounds, especially complex 9, reduced tumor volume, inhibited the expression of VEGF, and induced the expression of caspase-7. Additionally, they restored the levels of ALT, AST, albumin, and glucose close to their normal levels. Taken together, our newly synthesized metal complexes are promising anti-cancer agents against solid tumors induced by EAC cells as supported by the inhibition of VEGF and induction of caspase-7.

  • 18.
    El-Seedi, Hesham
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    El-Said, A. M. A.
    Khalifa, S. A. M.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Bohlin, Lars
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Borg-Karlson, A. -K
    Verpoorte, R.
    Biosynthesis, natural sources, dietary intake, pharmacokinetic properties, and biological activities of hydroxycinnamic acids2012In: Journal of Agricultural and Food Chemistry, ISSN 0021-8561, E-ISSN 1520-5118, Vol. 60, no 44, p. 10877-10895Article, review/survey (Refereed)
    Abstract [en]

    Hydroxycinnamic acids are the most widely distributed phenolic acids in plants. Broadly speaking, they can be defined as compounds derived from cinnamic acid. They are present at high concentrations in many food products, including fruits, vegetables, tea, cocoa, and wine. A diet rich in hydroxycinnamic acids is thought to be associated with beneficial health effects such as a reduced risk of cardiovascular disease. The impact of hydroxycinnamic acids on health depends on their intake and pharmacokinetic properties. This review discusses their chemistry, biosynthesis, natural sources, dietary intake, and pharmacokinetic properties.

  • 19.
    El-Seedi, Hesham
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Jiangsu Univ, Coll Food & Biol Engn, Zhenjiang 212013, Jiangsu, Peoples R China;Al Rayan Coll, Al Rayan Res & Innovat Ctr, Medina 42541, Saudi Arabia;Menoufia Univ, Fac Sci, Dept Chem, Al Minufiyah, Egypt.
    El-Shabasy, Rehan M.
    Menoufia Univ, Fac Sci, Dept Chem, Al Minufiyah, Egypt;KTH Royal Inst Technol, Sch Chem Sci & Engn, Dept Chem, Ecol Chem Grp, Stockholm, Sweden.
    Khalifa, Shaden A. M.
    Karolinska Univ Hosp, Clin Res Ctr, Huddinge, Sweden;Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, SE-10691 Stockholm, Sweden.
    Saeed, Aamer
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Shah, Afzal
    Univ Bahrain, Coll Sci, Dept Chem, Sakhir 32038, Bahrain.
    Shah, Raza
    Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan.
    Iftikhar, Faiza Jan
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Abdel-Daim, Mohamed M.
    Suez Canal Univ, Fac Vet Med, Pharmacol Dept, Ismailia 41522, Egypt.
    Omri, Abdelfatteh
    KAU, Ctr Excellence Bionosci Res, Jeddah 21589, Saudi Arabia;KAU, Dept Biol Sci, Biotechnol Res Grp, Fac Sci, Jeddah 21589, Saudi Arabia.
    Hajrahand, Nahid H.
    KAU, Ctr Excellence Bionosci Res, Jeddah 21589, Saudi Arabia;KAU, Dept Biol Sci, Biotechnol Res Grp, Fac Sci, Jeddah 21589, Saudi Arabia.
    Sabir, Jamal S. M.
    KAU, Ctr Excellence Bionosci Res, Jeddah 21589, Saudi Arabia;KAU, Dept Biol Sci, Biotechnol Res Grp, Fac Sci, Jeddah 21589, Saudi Arabia.
    Zou, Xiaobo
    Jiangsu Univ, Coll Food & Biol Engn, Zhenjiang 212013, Jiangsu, Peoples R China.
    Halabi, Mohammed F.
    Al Rayan Coll, Al Rayan Res & Innovat Ctr, Medina 42541, Saudi Arabia.
    Sarhan, Wessam
    Zewail City Sci & Technol, Cairo, Egypt.
    Guo, Weisheng
    Guangzhou Med Univ, Affiliated Hosp 2, Translat Med Ctr, Guangzhou 510260, Guangdong, Peoples R China.
    Metal nanoparticles fabricated by green chemistry using natural extracts: biosynthesis, mechanisms, and applications2019In: RSC Advances, ISSN 2046-2069, E-ISSN 2046-2069, Vol. 9, no 42, p. 24539-24559Article, review/survey (Refereed)
    Abstract [en]

    Nanoparticles (NPs) are new inspiring clinical targets that have emerged from persistent efforts with unique properties and diverse applications. However, the main methods currently utilized in their production are not environmentally friendly. With the aim of promoting a green approach for the synthesis of NPs, this review describes eco-friendly methods for the preparation of biogenic NPs and the known mechanisms for their biosynthesis. Natural plant extracts contain many different secondary metabolites and biomolecules, including flavonoids, alkaloids, terpenoids, phenolic compounds and enzymes. Secondary metabolites can enable the reduction of metal ions to NPs in eco-friendly one-step synthetic processes. Moreover, the green synthesis of NPs using plant extracts often obviates the need for stabilizing and capping agents and yields biologically active shape- and size-dependent products. Herein, we review the formation of metallic NPs induced by natural extracts and list the plant extracts used in the synthesis of NPs. In addition, the use of bacterial and fungal extracts in the synthesis of NPs is highlighted, and the parameters that influence the rate of particle production, size, and morphology are discussed. Finally, the importance and uniqueness of NP-based products are illustrated, and their commercial applications in various fields are briefly featured.

  • 20.
    El-Seedi, Hesham R.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy. Univ Malaya, Dept Chem, Fac Sci, Kuala Lumpur 50603, Malaysia.;Royal Inst Technol, Sch Chem Sci & Engn, Dept Chem, Ecol Chem Grp,KTH, Stockholm, Sweden.;Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm, Egypt..
    Azeem, Muhammad
    Royal Inst Technol, Sch Chem Sci & Engn, Dept Chem, Ecol Chem Grp,KTH, Stockholm, Sweden.;COMSATS Inst Informat Technol, Dept Chem, Abbottabad 22060, Pakistan..
    Khalil, Nasr S.
    Royal Inst Technol, Sch Chem Sci & Engn, Dept Chem, Ecol Chem Grp,KTH, Stockholm, Sweden.;Agr Res Ctr, Cairo, Egypt..
    Sakr, Hanem H.
    Menoufia Univ, Dept Zool, Fac Sci, Shibin Al Kawm 32512, Egypt..
    Khalifa, Shaden A. M.
    Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, S-10691 Stockholm, Sweden..
    Awang, Khalijah
    Univ Malaya, Dept Chem, Fac Sci, Kuala Lumpur 50603, Malaysia..
    Saeed, Aamer
    Quaid I Azam Univ, Islamabad 45320, Pakistan..
    Farag, Mohamed A.
    Cairo Univ, Dept Pharmacognosy, Coll Pharm, Kasr El Aini St,PB 11562, Cairo, Egypt..
    AlAjmi, Mohamed F.
    King Saud Univ, Dept Pharmacognosy, Coll Pharm, POB 2457, Riyadh 11451, Saudi Arabia..
    Palsson, Katinka
    Royal Inst Technol, Sch Chem Sci & Engn, Dept Chem, Ecol Chem Grp,KTH, Stockholm, Sweden..
    Borg-Karlson, Anna-Karin
    Royal Inst Technol, Sch Chem Sci & Engn, Dept Chem, Ecol Chem Grp,KTH, Stockholm, Sweden..
    Essential oils of aromatic Egyptian plants repel nymphs of the tick Ixodes ricinus (Acari: Ixodidae)2017In: Experimental & applied acarology, ISSN 0168-8162, E-ISSN 1572-9702, Vol. 73, no 1, p. 139-157Article in journal (Refereed)
    Abstract [en]

    Due to the role of Ixodes ricinus (L.) (Acari: Ixodidae) in the transmission of many serious pathogens, personal protection against bites of this tick is essential. In the present study the essential oils from 11 aromatic Egyptian plants were isolated and their repellent activity against I. ricinus nymphs was evaluated Three oils (i.e. Conyza dioscoridis L., Artemisia herba-alba Asso and Calendula officinalis L.) elicited high repellent activity in vitro of 94, 84.2 and 82%, respectively. The most active essential oil (C. dioscoridis) was applied in the field at a concentration of 6.5 A mu g/cm(2) and elicited a significant repellent activity against I. ricinus nymphs by 61.1%. The most repellent plants C. dioscoridis, C. officinalis and A. herba-alba yielded essential oils by 0.17, 0.11 and 0.14%, respectively. These oils were further investigated using gas chromatography-mass spectrometry analysis. alpha-Cadinol (10.7%) and hexadecanoic acid (10.5%) were the major components of C. dioscoridis whereas in C. officinalis, alpha-cadinol (21.2%) and carvone (18.2%) were major components. Artemisia herba-alba contained piperitone (26.5%), ethyl cinnamate (9.5%), camphor (7.7%) and hexadecanoic acid (6.9%). Essential oils of these three plants have a potential to be used for personal protection against tick bites.

  • 21.
    El-Seedi, Hesham R.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Burman, Robert
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Mansour, Ahmed
    Turki, Zaki
    Boulos, Loutfy
    Gullbo, Joachim
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Medical Sciences, Cancer Pharmacology and Computational Medicine.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    The traditional medical uses and cytotoxic activities of sixty-one Egyptian plants: Discovery of an active cardiac glycoside from Urginea maritima2013In: Journal of Ethnopharmacology, ISSN 0378-8741, E-ISSN 1872-7573, Vol. 145, no 3, p. 746-757Article in journal (Refereed)
    Abstract [en]

    Ethnopharmacological relevance: Medicinal plants from the Sinai desert are widely used in traditional Bedouin medicine to treat a range of conditions including, cancers, and may thus be useful sources of novel anti-tumor compounds. Information on plants used in this way was obtained through collaboration with Bedouin herbalists. Aim of the study: To document the traditional uses of 61 species from 29 families of Egyptian medicinal plants and to investigate their biological activity using a cytotoxicity assay. Material and methods: MeOH extracts of the 61 plant species investigated were dissolved in 10% DMSO and their cytotoxic activity was evaluated. The extracts were tested in duplicate on three separate occasions at three different concentrations (1, 10 and 100 mu g/ml) against human lymphoma U-937 GTB. The most active extract was subjected to bioassay-guided fractionation using HPLC and LC/ESI-MS to isolate and identify its active components. Results and discussion: The most potent extracts were those from Asclepias sinaica, Urginea maritima, Nerium oleander and Catharanthus roseus, followed by those from Cichorium endivia, Pulicaria undulate and Melia azedarach. Literature reports indicate that several of these plants produce cardiac glycosides. Bioassay-guided fractionation of alcoholic U. maritima extracts led to the isolation of a bioactive bufadienolide that was subsequently shown to be proscillaridin A, as determined by 1D and 2D NMR spectroscopy. This result demonstrates the value of plants used in traditional medicine as sources of medicinally interesting cytotoxic compounds.

  • 22.
    El-Seedi, Hesham R.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy. Univ Malaya, Fac Sci, Dept Chem, Kuala Lumpur 50603, Malaysia.;Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt..
    Gomaa, Mohamed
    Univ Jeddah, Fac Sci & Arts, Dept Biol, Khulais, Saudi Arabia..
    Salem, Mousa Maali
    Univ Jeddah, Fac Sci & Arts, Dept Biol, Khulais, Saudi Arabia..
    Benchoula, Khaled
    Int Islamic Univ Malaysia, Fac Pharm, Dept Pharmaceut Chem, Kuantan 25200, Pahang, Malaysia..
    Keshk, Hager M.
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt..
    Yosri, Nermeen
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt..
    Ayesh, Ahmed
    Univ Jeddah, Fac Sci & Arts, Dept Biol, Khulais, Saudi Arabia..
    Asker, Ahmed M.
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt..
    Soliman, Kawther
    Univ Jeddah, Fac Sci & Arts, Dept Biol, Khulais, Saudi Arabia..
    Hamza, Zeinab
    Natl Res Ctr, Food Toxins & Contaminants Dept, Marine Toxins Lab, Cairo, Egypt..
    Mansour, Hager M.
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt..
    Elkhateeb, Ahmed
    Natl Res Ctr, Phytochem & Plant Systemat Dept, Pharmaceut & Drug Ind Res Div, Cairo, Egypt..
    Khalif, Shaden A. M.
    Karolinska Univ Hosp, Dept Expt Hematol, SE-14186 Stockholm, Sweden.;Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, SE-10691 Stockholm, Sweden..
    Cytotoxic Effects Of The Red Sea Soft Coral Sarcophyton Trocheliophorum2016In: ACTA POLONIAE PHARMACEUTICA, ISSN 0001-6837, Vol. 73, no 6, p. 1587-1592Article in journal (Refereed)
    Abstract [en]

    The present study describes the in vitro cytotoxic effects of soft coral (Sarcophyton trocheliophorum). Soft corals of genus Sarcophyton were reported to contain compounds that arc active against brine shrimp and promote paclitaxel cytotoxicity in the human colon cancer Caco-2 cell line. The a-hexane extract of the soft coral Sarcophyton trocheliophorum induced significant dose-dependent toxicity (LC50 96.7 ppm) compared with ethyl acetate (LC50 120 ppm). We reported the most active cytotoxic level to be correspondence to LC50 values of 20.2, 59.2 ppm and 18.9 and 26 ppm. Accordingly, bio-assay guided fractionation was conducted to identify the bioactive compounds. Arachidonic acid. eicosapentaenoic acid and docosahexaenoic acid were characterized based on GC-MS analyses. Our results demonstrate the value of marine products as a natural source of medicinally interesting cytotoxic compounds.

  • 23.
    El-Seedi, Hesham R.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Univ Malaya, Fac Sci, Dept Chem, Kuala Lumpur, Malaysia; Univ Karachi, Int Ctr Chem Sci, HEJ Res Inst Chem, Karachi, Pakistan; Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm, Egypt.
    Khalifa, Shaden A. M.
    Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, Stockholm, Sweden.
    Taher, Eman A.
    Natl Org Drug Control & Res NODCAR, Cairo, Egypt; KTH, Royal Inst Technol, Dept Chem, Stockholm, Sweden.
    Farag, Mohamed A.
    Cairo Univ, Coll Pharm, Dept Pharmacognosy, Kasr el Aini St, Cairo, Egypt; Amer Univ Cairo, Sch Sci & Engn, Dept Chem, New Cairo, Egypt.
    Saeed, Aamer
    Quaid I Azam Univ, Dept Chem, Islamabad, Pakistan.
    Gamal, Mohamed
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm, Egypt.
    Hegazy, Mohamed-Elamir F.
    Natl Res Ctr, Chem Med Plants Dept, Giza, Egypt; Johannes Gutenberg Univ Mainz, Inst Pharm, Dept Pharmaceut Biol, Mainz, Germany.
    Youssef, Diaa
    King Abdulaziz Univ, Fac Pharm, Jeddah, Saudi Arabia.
    Musharraf, Syed G.
    Univ Karachi, Int Ctr Chem Sci, HEJ Res Inst Chem, Karachi, Pakistan.
    Alajlani, Muaaz M.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Xiao, Jianbo
    Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Control Chinese Med, Macau, Peoples R China.
    Efferth, Thomas
    Johannes Gutenberg Univ Mainz, Inst Pharm, Dept Pharmaceut Biol, Mainz, Germany.
    Cardenolides: Insights from chemical structure and pharmacological utility2019In: Pharmacological Research, ISSN 1043-6618, E-ISSN 1096-1186, Vol. 141, p. 123-175Article, review/survey (Refereed)
    Abstract [en]

    Cardiac glycosides (CGs) are a class of naturally occurring steroid-like compounds, and members of this class have been in clinical use for more than 1500 years. They have been used in folk medicine as arrow poisons, abortifacients, heart tonics, emetics, and diuretics as well as in other applications. The major use of CGs today is based on their ability to inhibit the membrane-bound Na+/K+ -ATPase enzyme, and they are regarded as an effective treatment for congestive heart failure (CHF), cardiac arrhythmia and atrial fibrillation. Furthermore, increasing evidence has indicated the potential cytotoxic effects of CGs against various types of cancer. In this review, we highlight some of the structural features of this class of natural products that are crucial for their efficacy, some methods of isolating these compounds from natural resources, and the structural elucidation tools that have been used. We also describe their physicochemical properties and several modern biotechnological approaches for preparing CGs that do not require plant sources.

  • 24.
    El-Seedi, Hesham R.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Al Rayan Coll, Al Ragan Res & Innovat Ctr, Medina 42541, Saudi Arabia;Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt.
    Khalifa, Shaden A. M.
    Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, SE-10691 Stockholm, Sweden;Karolinska Univ Hosp, Clin Res Ctr, Huddinge, Sweden.
    Yosri, Nermeen
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt.
    Khatib, Alfi
    Int Islamic Univ Malaysia, Dept Pharmaceut Chem, Fac Pharm, Kuantan 25200, Pahang, Malaysia.
    Chen, Lei
    Fujian Agr & Forestry Univ, Coll Food Sci, Fuzhou 350002, Fujian, Peoples R China.
    Saeed, Aamer
    Quaid I Azam Univ, Islamabad 45320, Pakistan.
    Efferth, Thomas
    Johannes Gutenberg Univ Mainz, Dept Pharmaceut Biol, Staudinger Weg 5, D-55128 Mainz, Germany.
    Verpoorte, Rob
    Leiden Univ, IBL, Nat Prod Lab, POB 9505, NL-2300 RA Leiden, Netherlands.
    Plants mentioned in the Islamic Scriptures (Holy Qur'an and Ahadith): Traditional uses and medicinal importance in contemporary times2019In: Journal of Ethnopharmacology, ISSN 0378-8741, E-ISSN 1872-7573, Vol. 243, article id 112007Article, review/survey (Refereed)
    Abstract [en]

    Ethnopharmacological relevance: Over the past thousand years, Islamic physicians have collected cultural, philosophical, sociological and historical backgrounds for understanding diseases and medications. The Prophet Mohammed (Peace Be Upon Him (PBUH) said: "There is no disease that Allah has created, except that Allah also has created its cure." Therefore, Islamic scholars are encouraged to explore and use both traditional and modern forms of medicine. Aim of the study: (1) To identify some of the medicinal plants mentioned in the Holy Qur'an and Ahadith textbooks of the period 700-1500 AD; (2) to compare them with presently used traditional medicines; (3) to evaluate their value based on modern research; and (4) to investigate the contributions of Islamic scholars to the development of the scientific branches, particularly medicine. Materials and methods: A literature search was performed relating to 12 medicinal plants mentioned in the Holy Qur'an and Ahadith using textbooks, Al-Azhar scholars, published articles, the plant list website (http://www.theplantlist.org/), the medicinal plant names services website (http://mpns.kew.org/mpns-portal/) and web databases (PubMed, Science Direct, and Google Scholar). Results and discussion: The Islamic Golden Age was a step towards modern medicine, with unique insights and multi-disciplinary aspects. Traditional Islamic Medicine has had a significant impact on the development of various medical, scientific and educational activities. Innumerable Muslim and non-Muslim physicians have built on the strong foundation of Traditional Islamic Medicine by translating the described natural remedies and effects. The influences of different ancient cultures on the traditional uses of natural products were also documented in Islamic Scriptures in the last part of the second millennium. The divine teachings of Islam combine natural and practical healing and incorporate inherited science and technology. Conclusion: In this review, we discuss Traditional Islamic Medicine with reference to both medical recommendations mentioned in the Holy Qur'an and Prophetic Traditional Medicine (al-Tibb al-Nabawi). Although the molecular mechanisms and functions of some of the listed medicinal plants and their derivatives have been intensively studied, some traditional remedies have yet to be translated into clinical applications.

  • 25.
    El-Seedi, Hesham R.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Khalil, Nasr S.
    Azeem, Muhammad
    Taher, Eman A.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Palsson, Katinka
    Borg-Karlson, Anna-Karin
    Chemical Composition and Repellency of Essential Oils From Four Medicinal Plants Against Ixodes ricinus Nymphs (Acari Ixodidae)2012In: Journal of medical entomology, ISSN 0022-2585, E-ISSN 1938-2928, Vol. 49, no 5, p. 1067-1075Article in journal (Refereed)
    Abstract [en]

    In our search for effective tick repellents from plant origin, we investigated the effect of essential oils of four medicinal and culinary plants belonging to the family Lamiaceae on nymphs of the tick Ixodes ricinus (L.). The essential oils of the dry leaves of Rosmarinus officinalis (Rosemary) (L.), Mentha spicata (Spearmint) (L.), Origanum majorana (Majoram) (L.), and Ocimum basilicum (Basil) (L.) were isolated by steam distillation and 15 mu g/cm(2) concentration of oils was tested against ticks in a laboratory bioassay. The oils of R. officinalis, M. spicata, and O. majorana showed strong repellency against the ticks 100, 93.2, and 84.3%, respectively, whereas O. basilicum only showed 64.5% repellency. When tested in the field, the oils of R. officinalis and M. spicata showed 68.3 and 59.4% repellency at a concentration of 6.5 mu g/cm(2) on the test cloths. The oils were analyzed by gas chromatography mass spectrometry and the major compounds from the most repellent oils were 1,8-cineole, camphor, linalool, 4-terpineol, borneol, and carvone.

  • 26.
    Elshrif, Shimaa S.
    et al.
    Menoufia Univ, Fac Sci, Chem Dept, Shibin Al Kawm 32512, Egypt..
    El Gendy, Abd El-Nasser G.
    Natl Res Ctr, Med & Aromat Plants Res Dept, Cairo 12622, Egypt..
    Elshamy, Abdelsamed I.
    Natl Res Ctr, Nat Compound Chem Dept, El Tahrir St, Giza 12622, Egypt..
    Nassar, Mahmoud I.
    Natl Res Ctr, Nat Compound Chem Dept, El Tahrir St, Giza 12622, Egypt..
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Fac Sci, Chem Dept, Shibin Al Kawm 32512, Egypt..
    Chemical Composition and TLC-DPPH-Radical Scavenging Activity of Cyperus alternifolius Rottb. Essential Oils2017In: Journal of Essential Oil-Bearing Plants (JEOBP), ISSN 0972-060X, E-ISSN 0976-5026, Vol. 20, no 4, p. 1125-1130Article in journal (Refereed)
    Abstract [en]

    The essential oils (EOs) of the tubers and aerial parts of Cyperus alternifolius Rottb. were separately extracted and analyzed by gas chromatography-mass spectroscopy (GC-MS). Seventeen and fifteen volatile compounds were identified from the tubers and aerial parts represented 99.16 % and 100 % of the total mass, respectively. Terpenes (97.82 % and 97.43 %) were the more characteristic content including sesquiterpenes (97.22 % and 3.89 %) and monoterpenes (0.6 % and 93.54 %), respectively. Caryophyllene (50.6 %), caryophyllene oxide (29.84 %), farnesyl acetone (4.65 %) represented the major components of the tubers EO. While D-limonene (63.78 %), theaspirane A (13.36 %), theaspirane B (10.97 %) and gamma-terpinene (3.4 %) were the majors of aerial parts EO. The aerial parts oil showed significant antioxidant activity at all concentrations in relation to rutin by TLC-DPPH radical scavenging activity method. The EO of the tubers exhibited moderate antioxidant activity at 5 mu g/ml and 10 mu g/ml with values 1.33 +/- 0.13 and 1.12 +/- 0.38, respectively. Significant antioxidant activity were exhibited by aerial parts EO at the three concentrations 2.5 mu g/ml, 5 mu g/ml and 10 mu g/ml with activity values 5.83 +/- 0.61, 7.18 +/- 0.81 and 8.48 +/- 1.30, respectively.

  • 27.
    Farag, Mohamed A.
    et al.
    Cairo Univ, Coll Pharm, Pharmacognosy Dept, Kasr El Aini St,PB 11562, Cairo, Egypt;Amer Univ Cairo, Sch Sci & Engn, Dept Chem, New Cairo 11835, Egypt.
    El-Kersh, Dina M.
    BUE, Fac Pharm, Pharmacognosy Dept, Cairo 11837, Egypt.
    Ehrlich, Anja
    Leibniz Inst Plant Biochem, Dept Bioorgan Chem, Weinberg 3, D-06120 Halle, Saale, Germany.
    Choucry, Mouchira A.
    Cairo Univ, Coll Pharm, Pharmacognosy Dept, Kasr El Aini St,PB 11562, Cairo, Egypt.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Fac Sci, Dept Chem, Al Minufya, Egypt.
    Frolov, Andrej
    Leibniz Inst Plant Biochem, Dept Bioorgan Chem, Weinberg 3, D-06120 Halle, Saale, Germany;St Petersburg State Univ, Dept Biochem, St Petersburg 199034, Russia.
    Wessjohann, Ludger A.
    Leibniz Inst Plant Biochem, Dept Bioorgan Chem, Weinberg 3, D-06120 Halle, Saale, Germany.
    Variation in Ceratonia siliqua pod metabolome in context of its different geographical origin, ripening stage and roasting process2019In: Food Chemistry, ISSN 0308-8146, E-ISSN 1873-7072, Vol. 283, p. 675-687Article in journal (Refereed)
    Abstract [en]

    Carob is a legume tree of a considerable commercial importance for the flavor and sweet industry. In this context, it is cultivated mostly for its pods, which are known for their nutritive value and multiple health benefits. However, metabolite patterns, underlying these properties are still mostly uncharacterized. In this study, the role of geographical origin, ontogenetic changes and thermal processing on the Ceratonia siliqua pod metabolome was assessed by mass spectrometry (MS)-based metabolomics. Thereby, a total of 70 fruits primary metabolites, represented mainly by carbohydrates, organic and amino acids were detected. Analysis of secondary bioactive metabolites assessed by ultra-high-performance liquid chromatography-electrospray ionization high resolution mass spectrometry (UHPLC-ESI-HR-MS) revealed in total 83 signals. The major signals, most significantly contributing in discrimination of C. siliqua specimens were assigned to tannins and flavonoids. PCA models derived from either UHPLC-MS or GC-MS proved to be powerful tools for discrimination of C. siliqua specimens.

  • 28.
    Gunasekera, Sunithi
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Aboye, Teshome L.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Madian, Walid A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    El-Seedi, Hesham R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Making Ends Meet: Microwave-Accelerated Synthesis of Cyclic and Disulfide Rich Proteins Via In Situ Thioesterification and Native Chemical Ligation2013In: International Journal of Peptide Research and Therapeutics, ISSN 1573-3149, Vol. 19, no 1- SI, p. 43-54Article in journal (Refereed)
    Abstract [en]

    The development of synthetic methodologies for cyclic peptides is driven by the discovery of cyclic peptide drug scaffolds such as the plant-derived cyclotides, sunflower trypsin inhibitor 1 (SFTI-1) and the development of cyclized conotoxins. Currently, the native chemical ligation reaction between an N-terminal cysteine and C-terminal thioester group remains the most robust method to obtain a head-to-tail cyclized peptide. Peptidyl thioesters are effectively generated by Boc SPPS. However, their generation is challenging using Fmoc SPPS because thioester linkers are not stable to repeated piperidine exposure during deprotection. Herein we describe a Fmoc-based protocol for synthesizing cyclic peptides adapted for microwave assisted solid phase peptide synthesis. The protocol relies on the linker Di-Fmoc-3,4-diaminobenzoic acid, and we demonstrate the use of Gly, Ser, Arg and Ile as C-terminal amino acids (using HBTU and HATU as coupling reagents). Following synthesis, an N-acylurea moiety is generated at the C-terminal of the peptide; the resin bound acylurea peptide is then deprotected and cleaved from the resin. The fully deprotected peptide undergoes thiolysis in aqueous buffer, generating the thioester in situ. Ultimately, the head-to-tail cyclized peptide is obtained via native chemical ligation. Two naturally occurring cyclic peptides, the prototypical Mobius cyclotide kalata B1 and SFTI-1 were synthesized efficiently, avoiding potential branching at the diamino linker, using the optimized protocol. In addition, we demonstrate the possibility to use the approach for the synthesis of long and synthetically challenging linear sequences, by the ligation of two truncated fragments of a 50-residue long plant defensin.

  • 29.
    Hussain, Afzal
    et al.
    King Saud Univ, Dept Pharmacognosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    Oves, Mohammad
    King Abdulaziz Univ, Ctr Excellence Environm Studies, Jeddah 21589, Saudi Arabia.
    Alajmi, Mohamed F.
    King Saud Univ, Dept Pharmacognosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    Hussain, Iqbal
    Jubail Ind Coll, Dept Gen Studies, Jubail Ind City 31961, Jubail, Saudi Arabia.
    Amir, Samira
    Alfaisal Univ, Dept Chem, Coll Sci & Gen Studies, Riyadh 11451, Saudi Arabia.
    Ahmed, Jahangeer
    King Saud Univ, Dept Chem, Coll Sci, Riyadh 11451, Saudi Arabia.
    Rehman, Md Tabish
    King Saud Univ, Dept Pharmacognosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Ali, Imran
    Taibah Univ, Dept Chem, Coll Sci, Al Medina Al Munawara 41477, Saudi Arabia;Jamia Millia Islamia, Dept Chem, New Delhi, India.
    Biogenesis of ZnO nanoparticles using Pandanus odorifer leaf extract: anticancer and antimicrobial activities2019In: RSC Advances, ISSN 2046-2069, E-ISSN 2046-2069, Vol. 9, no 27, p. 15357-15369Article in journal (Refereed)
    Abstract [en]

    The continuously increasing incidence rates of cancer and infectious diseases are open threats to the sustainable survival of animals and humans. In the last two decades, the demands of nanomaterials as modern therapeutic agents have increased. In this study, biogenic zinc oxide nanoparticles (ZnO NPs) were developed from aqueous Pandanus odorifer leaf extract (POLE) and characterized using modern methods and tools, such as electron microscopy, X-ray diffraction, energy dispersive X-ray spectroscopy (EDX), Fourier transform infrared spectroscopy and UV-vis spectroscopy, which indicated the formation of very pure, spherical NPs approximately 90 nm in size. The anticancer activity of the ZnO NPs was evaluated by MTT and neutral red uptake (NRU) assays in MCF-7, HepG2 and A-549 cells at different doses (1, 2, 5, 10, 25, 50, 100 g ml(-1)). Moreover, the morphology of the treated cancer cells was examined by phase contrast microscopy. The results suggest that the synthesized ZnO NPs inhibited the growth of the cells when applied a concentration from 50-100 g ml(-1). Moreover, the biogenic ZnO NPs were analysed as an antimicrobial agent against pathogenic bacteria. The highest antibacterial activity was observed against Gram-positive Bacillus subtilis (26 nm) and Gram-negative Escherichia coli (24 mm) at 50 g per well. Complete bacterial growth (100%) vanished 100% upon treatment with ZnO NPs at 85 g ml(-1). Overall, POLE mediated derived biogenic ZnO NPs could serve as a significant anticancer and antimicrobial agent and be used in the development of novel drugs and skin care products.

  • 30.
    Kanwal, Nayab
    et al.
    Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan.
    Siddiqui, Amna Jabbar
    Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan.
    Ul Haq, Faraz
    Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan.
    El-Seedi, Hesham R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Musharraf, Syed Ghulam
    Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan.
    Two-stage mass spectrometry approach for the analysis of triterpenoid glycosides in Fagonia indica2018In: RSC Advances, ISSN 2046-2069, E-ISSN 2046-2069, Vol. 8, no 71, p. 41023-41031Article in journal (Refereed)
    Abstract [en]

    Triterpenoid glycosides are molecules widely distributed in plants and have shown a wide range of biological activities against various diseases. This paper describes the qualitative and quantitative analysis of triterpenoid glycoside (saponins) using a two-stage mass spectrometry approach in five samples of Fagonia indica collected from various parts of the country. In the first stage, triterpenoid glycosides were identified using liquid chromatography high-resolution mass spectrometry using UHPLC-QTOF-MS system. In the second stage, compounds were quantified using a multiple reaction monitoring (MRM) approach using an UHPLC-QQQ-MS system. Fagonia indica has shown a wide range of biological activities and found to be rich in saponin or triterpenoid glycoside constituents. A total of thirteen triterpenoid saponins were identified based on high-resolution analysis, MS/MS and database comparison, while six of them were simultaneously quantified using the multiple reaction monitoring (MRM) approach. The results indicate that the samples share a similar UHPLC pattern, however, the amount of these saponins in samples varies greatly. Compound 4i.e. nayabin D was the major constituent (1.4-3.8 g g(-1)) among the six analyzed compounds. The results demonstrated that the developed multi-compound determination in combination with a fingerprint analysis method is rapid, accurate, precise and sensitive and can be utilized for quality control and high-throughput quantification of various saponins in Fagonia indica may be extended to other plant species.

  • 31. Khalifa, Shaden A. M.
    et al.
    de Medina, Philippe
    Erlandsson, Anna
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Public Health and Caring Sciences.
    El-Seedi, Hesham R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Silvente-Poirot, Sandrine
    Poirot, Marc
    The novel steroidal alkaloids dendrogenin A and B promote proliferation of adult neural stem cells2014In: Biochemical and Biophysical Research Communications - BBRC, ISSN 0006-291X, E-ISSN 1090-2104, Vol. 446, no 3, p. 681-686Article in journal (Refereed)
    Abstract [en]

    Dendrogenin A (DDA) and dendrogenin B (DDB) are new aminoalkyl oxysterols which display re-differentiation of tumor cells of neuronal origin at nanomolar concentrations. We analyzed the influence of dendrogenins on adult mice neural stem cell proliferation, sphere formation and differentiation. DDA and DDB were found to have potent proliferative effects in neural stem cells. Additionally, they induce neuronal outgrowth from neurospheres during in vitro cultivation. Taken together, our results demonstrate a novel role for dendrogenins A and B in neural stem cell proliferation and differentiation which further increases their likely importance to compensate for neuronal cell loss in the brain. (C) 2014 Elsevier Inc. All rights reserved.

  • 32.
    Khalifa, Shaden A. M.
    et al.
    Karolinska Univ Hosp, Clin Res Ctr, S-14157 Stockholm, Sweden;Stockholm Univ, Dept Mol Biosci, Wenner Gren Inst, SE-10691 Stockholm, Sweden.
    Elias, Nizar
    Univ Kalamoon, Dept Lab Med, Fac Med, POB 222, Dayr Atiyah, Syria.
    Farag, Mohamed A.
    Cairo Univ, Coll Pharm, Pharmacognosy Dept, Kasr El Aini St,PB 11562, Cairo, Egypt;Amer Univ Cairo, Dept Chem, Sch Sci & Engn, New Cairo 11835, Egypt.
    Chen, Lei
    Fujian Agr & Forestry Univ, Coll Food Sci, Fuzhou 350002, Fujian, Peoples R China.
    Saeed, Aamer
    Quaid I Azam Univ, Dept Chemitry, Islamabad 45320, Pakistan.
    Hegazy, Mohamed-Elamir F.
    Johannes Gutenberg Univ Mainz, Inst Pharm & Biochem, Dept Pharmaceut Biol, Staudingerweg 5, D-55128 Mainz, Germany;Natl Res Ctr, Chem Med Plants Dept, 33 El Bohouth St, Giza 12622, Egypt.
    Moustafa, Moustafa S.
    Kuwait Univ, Dept Chem, Fac Sci, Safat 13060, Kuwait.
    Abd El-Wahed, Aida
    Kuwait Univ, Dept Chem, Fac Sci, Safat 13060, Kuwait.
    Al-Mousawi, Saleh M.
    Kuwait Univ, Dept Chem, Fac Sci, Safat 13060, Kuwait.
    Musharraf, Syed G.
    Univ Karachi, Int Ctr Chem & Biol Sci ICCBS, HEJ Inst Chem Res, Karachi 75270, Pakistan.
    Chang, Fang-Rong
    Kaohsiung Med Univ, Grad Inst Nat Prod, Kaohsiung 807, Taiwan.
    Iwasaki, Arihiro
    Keio Univ, Fac Sci & Technol, Dept Chem, Kohoku Ku, 3-14-1 Hiyoshi, Yokohama, Kanagawa 2238522, Japan.
    Suenaga, Kiyotake
    Keio Univ, Fac Sci & Technol, Dept Chem, Kohoku Ku, 3-14-1 Hiyoshi, Yokohama, Kanagawa 2238522, Japan;Univ HalleWittenberg, Dept Pharmaceut Biol Pharmacognosy, Inst Pharm, Hoher Weg 8, DE-06120 Halle, Saale, Germany.
    Alajlani, Muaaz M.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt;Jiangsu Univ, Coll Food & Biol Engn, Zhenjiang 212013, Jiangsu, Peoples R China;Al Rayan Coll, Al Rayan Res & Innovat Ctr, Medina 42541, Saudi Arabia.
    Marine Natural Products: A Source of Novel Anticancer Drugs2019In: Marine Drugs, ISSN 1660-3397, E-ISSN 1660-3397, Vol. 17, no 9, article id 491Article, review/survey (Refereed)
    Abstract [en]

    Cancer remains one of the most lethal diseases worldwide. There is an urgent need for new drugs with novel modes of action and thus considerable research has been conducted for new anticancer drugs from natural sources, especially plants, microbes and marine organisms. Marine populations represent reservoirs of novel bioactive metabolites with diverse groups of chemical structures. This review highlights the impact of marine organisms, with particular emphasis on marine plants, algae, bacteria, actinomycetes, fungi, sponges and soft corals. Anti-cancer effects of marine natural products in in vitro and in vivo studies were first introduced; their activity in the prevention of tumor formation and the related compound-induced apoptosis and cytotoxicities were tackled. The possible molecular mechanisms behind the biological effects are also presented. The review highlights the diversity of marine organisms, novel chemical structures, and chemical property space. Finally, therapeutic strategies and the present use of marine-derived components, its future direction and limitations are discussed.

  • 33.
    Khalifa, Shaden A. M.
    et al.
    Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, SE-10691 Stockholm, Sweden;Karolinska Univ, Karolinska Inst Huddinge, Clin Res Ctr, Dept Lab Med, Solna, Sweden.
    Farag, Mohamed A.
    Cairo Univ, Coll Pharm, Pharmacognosy Dept, Kasr El Aini St, Cairo 11562, Egypt;Amer Univ Cairo, Sch Sci & Engn, Dept Chem, New Cairo 11835, Egypt.
    Yosri, Nermeen
    Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt.
    Sabir, Jamal S. M.
    KAU, Ctr Excellence Bionosci Res, Jeddah 21589, Saudi Arabia;KAU, Fac Sci, Dept Biol Sci, Biotechnol Res Grp, Jeddah 21589, Saudi Arabia.
    Saeed, Aamer
    Quaid I Azam Univ, Islamabad 45320, Pakistan.
    Al-Mousawi, Saleh Mohammed
    Univ Kuwait, Fac Sci, Dept Chem, POB 5969, Safat 13060, Kuwait;Univ Karachi, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
    Taha, Wafaa
    Minist Hlth, Reg Colab, Pesticides Residues Food & Water Dept, Menoufia, Egypt.
    Musharraf, Syed Ghulam
    Patel, Seema
    San Diego State Univ, Bioinformat & Med Informat Res Ctr, San Diego, CA 92182 USA.
    El-Seedi, Hesham R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Fac Sci, Dept Chem, Shibin Al Kawm 32512, Egypt;Al Rayon Coll, Al Rayon Res & Innovat Ctr, Medina 42541, Saudi Arabia;Jiangsu Univ, Coll Food & Biol Engn, Zhenjiang 212013, Jiangsu, Peoples R China.
    Truffles: From Islamic culture to chemistry, pharmacology, and food trends in recent times2019In: Trends in Food Science & Technology, ISSN 0924-2244, E-ISSN 1879-3053, Vol. 91, p. 193-218Article, review/survey (Refereed)
    Abstract [en]

    Background: Many years back, during Islamic civilization, truffle (Kama'ah) was mentioned by Prophet Muhammed (PBUH) to be well recognized as a therapeutic for eye diseases. ("In the Sahihain, it is narrated that the Prophet said: "The Kama'ah (truffle) is among the manna (which is a food mentioned in the Qura'n, Surah alBagarah), and its water (extract or juice) cures the eye diseases"). Truffles represent a large group of soil fungi belonging to Ascomycota, Basidiomycota, and Zygomycota. Because of their exceptionally profitable protein, fat, polysaccharide, carbohydrate, ash, mineral, phenolic and other organic molecule contents, truffles have been appreciated as food, nutritional and therapeutic sources for many years. Scope and approach: The main aim of this review is to highlight a comprehensive compile of truffles traditional uses, mycochemistry, pharmacological properties and nutritional value with special focus on desert truffles. Such review represents a good candidate reference for future truffle research. Key findings and conclusions: In this review, we discuss the traditional aspects of truffles with reference to Prophetic Traditional Medicine (al-Tibb al-Nabawi) to cure aliments such as trachoma. The use of truffles is justified by many recent research findings with regards to their anti-inflammatory, anti-bacterial, anti-oxidant, and anti-cancer properties. Although the molecular mechanism and functions of the different truffle species have been intensively studied, we look forward to translating these traditional remedies into preclinical and clinical applications.

  • 34.
    Larik, Fayaz Ali
    et al.
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan..
    Saeed, Aamer
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan..
    Shahzad, Danish
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan..
    Faisal, Muhammad
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan..
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Mehfooz, Haroon
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan..
    Channar, Pervaiz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan..
    Synthetic approaches towards the multi target drug spironolactone and its potent analogues/derivatives2017In: Steroids, ISSN 0039-128X, E-ISSN 1878-5867, Vol. 118, p. 76-92Article, review/survey (Refereed)
    Abstract [en]

    Spironolactone is a well-known multi-target drug and is specifically used for the treatment of high blood pressure and heart failure. It is also used for the treatment of edema, cirrhosis of the liver, malignant, pediatric, nephrosis and primary hyperaldosteronism. Spironolactone in association with thiazide diuretics treats hypertension and in association with furosemide treats bronchopulmonary dyspepsia. The therapeutic mechanism of action of spironolactone involves binding to intracellular mineralocorticoids receptors (MRs) in kidney epithelial cells, thereby inhibiting the binding of aldosterone. Since its first synthesis in 1957 there are several synthetic approaches have been reported throughout the years, Synthetic community has devoted efforts to improve the synthesis of spironolactone and to synthesize its analogues and derivatives. This review aims to provide comprehensive insight for the synthetic endeavors devoted towards the synthesis of a versatile drug spironolactone and its analogues/derivatives.

  • 35.
    Miao, Lingchao
    et al.
    Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Control Chinese Med, Taipa, Macao, Peoples R China.
    Tao, Hongxun
    Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Control Chinese Med, Taipa, Macao, Peoples R China.
    Peng, Yu
    Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Control Chinese Med, Taipa, Macao, Peoples R China.
    Wang, Shengpeng
    Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Control Chinese Med, Taipa, Macao, Peoples R China.
    Zhong, Zhangfeng
    Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Control Chinese Med, Taipa, Macao, Peoples R China.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Dragan, Simona
    Univ Med & Farm Timisoara, 2 Eftimie Murgu Sq, Timisoara 300041, Romania.
    Zengin, Gokhan
    Selcuk Univ, Sci Fac, Dept Biol, Konya, Turkey.
    Cheang, Wai San
    Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Control Chinese Med, Taipa, Macao, Peoples R China.
    Wang, Yitao
    Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Control Chinese Med, Taipa, Macao, Peoples R China.
    Xiao, Jianbo
    Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Control Chinese Med, Taipa, Macao, Peoples R China.
    The anti-inflammatory potential of Portulaca oleracea L. (purslane) extract by partial suppression on NF-kappa B and MAPK activation2019In: Food Chemistry, ISSN 0308-8146, E-ISSN 1873-7072, Vol. 290, p. 239-245Article in journal (Refereed)
    Abstract [en]

    Portulaca oleracea L. (Purslane) has great potential as food and traditional drugs in several countries. The purpose of this study was to evaluate the anti-inflammatory effects of purslane extract on lipopolysaccharide (LPS)stimulated RAW 264.7 cells. Purslane extracts significantly reduced LPS-induced synthesis of NO in a dose-dependent manner, as well as the expression levels of iNOS and COX-2. The productions of TNF-alpha and IL-6 were also significantly reduced at the higher dose of 400 mu g/ml. Meanwhile, the expression levels of P65, p-P65, p-MEK and p-I kappa B-alpha were inhibited dose-dependently. The nuclear translocation of P65 was partially prevented by the extract, which explained the inhibition of NF-kappa B pathway. In addition, three reported flavonoids, named luteolin, kaempferol and quercitrin, were identified in the extract, which might be responsible for its anti-inflammatory effects. Above all, our research has partially proved that purslane could be considered as a natural anti-inflammatory agent in further applications.

  • 36.
    Moustafa, Moustafa Sherief
    et al.
    Univ Kuwait, Dept Chem, Fac Sci, POB 5969, Safat 13060, Kuwait.
    Al-Mousawi, Saleh Mohammed
    Univ Kuwait, Dept Chem, Fac Sci, POB 5969, Safat 13060, Kuwait.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Univ Karachi, Res Inst Chem, ICCBS, Karachi 75270, Pakistan;Menoufia Univ, Chem Dept, Fac Sci, Menoufia, Egypt.
    Elnagdi, Mohamed Hilmy
    Cairo Univ, Dept Chem, Fac Sci, POB 12613, Giza, Egypt.
    Chemistry of Heterocyclic Five and Six Membered Enamino Nitriles and Enamino Esters2018In: Mini-Reviews in medical chemistry, ISSN 1389-5575, E-ISSN 1875-5607, Vol. 18, no 12, p. 992-1007Article, review/survey (Refereed)
    Abstract [en]

    Progress in the chemistry of cyclic enamino-nitriles based on the advanced synthetic methodologies is reported. Due to the recent accomplishment, it becomes possible to reactivate these molecules toward electrophiles, nucleophiles and as electron rich dienes in 2+3 dipolar additions and in 4+2 cycloadditions reactions. Synthesizing the poly functionalized 4H-pyrans and their fused derivatives is a fascinating field with a multitude of biological implications such as antitumor, cardiotonic, hepatoprotective, antihypertensive, antibronchitis, as well antifungal activity. This work was conducted with particular emphasis on reviewing the work done on the cyclic enamines since 1990 up till now in order to highlight in more details the synthetic pathways, interactions and the biological activities, Furthermore; we referred to the recent original data of our group contributions within this field.

  • 37.
    Moustafa, Moustafa Sherief
    et al.
    Univ Kuwait, Fac Sci, Dept Chem, Safat Kuwait, Kuwait.
    Al-Mousawi, Saleh Mohammed
    Univ Kuwait, Fac Sci, Dept Chem, Safat Kuwait, Kuwait.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Elnagdi, Mohamed Hilmy
    Cairo Univ, Fac Sci, Dept Chem, Giza, Egypt.
    Tales of the Unexpected in Synthesis of Polyfunctional Heteroaromatics2018In: Current Organic Synthesis, ISSN 1570-1794, E-ISSN 1875-6271, Vol. 15, no 5, p. 587-602Article, review/survey (Refereed)
    Abstract [en]

    Background: Our research group has a longstanding interest in the synthesis of novel functionalized heteroaromatic compounds, and the development of new methods for this purpose. During our ongoing investigations, we recently had an instance to check the reproducibility of some published results concerning the chemistry of arylhydrazonals, enamines and other functionally substituted carbonyl compounds. This work has led to the discovery of some new rearrangements, and the revision of the structures originally assigned to several molecules.

    Objective: This review surveys some correction of several erroneous reports that have appeared in the literature, and presents some interesting new rearrangements discovered in the course of investigating older reports.

    Results: The crystallographic studies revealed that the condensation of arylhydrazonals with active methylenenitriles yields arylazoniconates rather than pyridazenones as previously reported. Additionally, phenathylthiocyanate reacts with malononitrile to afford thiazoles rather than the previously reported condensation with the carbonyl group. In another example, the reaction of phenethylmalononitrile with hydrazine yields pyrazolopyridazenes rather than phenacylpyrazol-3,5-diamine. In yet another case, several interesting Dimrothtype rearrangements were observed when malononitrile was condensed with enaminones, contradicting earlier reports. Unexpectedly, these enaminones underwent self-trimerization to yield 1,3,5-trisubstituted benzenes under certain conditions. Enaminonitriles also undergo interesting and novel Dimroth rearrangements when reacted with cyclohexanedione or dehydroacetic acid derivatives.

    Conclusion: We have shown that the structures of several complex heterocyclic compounds that have been reported in the literature over the last 50 years were incorrectly assigned, possibly because the authors who originally reported them were using substandard or outdated analytical equipments.

  • 38.
    Murugesu, Suganya
    et al.
    Kulliyyah Pharm Int Islamic Univ Malaysia, Dept Pharmaceut Chem, Kuantan 25200, Pahang Darul Ma, Malaysia.
    Ibrahim, Zalikha
    Kulliyyah Pharm Int Islamic Univ Malaysia, Dept Pharmaceut Chem, Kuantan 25200, Pahang Darul Ma, Malaysia.
    Ahmed, Qamar-Uddin
    Kulliyyah Pharm Int Islamic Univ Malaysia, Dept Pharmaceut Chem, Kuantan 25200, Pahang Darul Ma, Malaysia.
    Yusoff, Nik-Idris Nik
    Kulliyyah Pharm Int Islamic Univ Malaysia, Dept Pharmaceut Chem, Kuantan 25200, Pahang Darul Ma, Malaysia.
    Uzir, Bisha-Fathamah
    Kulliyyah Pharm Int Islamic Univ Malaysia, Dept Pharmaceut Chem, Kuantan 25200, Pahang Darul Ma, Malaysia.
    Perumal, Vikneswari
    Univ Kuala Lumpur, Royal Coll Med Perak, Fac Pharm & Hlth Sci, Ipoh 30450, Perak Darul Rid, Malaysia.
    Abas, Faridah
    Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43300, Selangor Darul, Malaysia.
    Saari, Khozirah
    Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43300, Selangor Darul, Malaysia.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
    Khatib, Alfi
    Kulliyyah Pharm Int Islamic Univ Malaysia, Dept Pharmaceut Chem, Kuantan 25200, Pahang Darul Ma, Malaysia;Univ Putra Malaysia, Lab Nat Prod, Inst Biosci, Serdang 43300, Selangor Darul, Malaysia.
    Characterization of alpha-Glucosidase Inhibitors from Clinacanthus nutans Lindau Leaves by Gas Chromatography-Mass Spectrometry-Based Metabolomics and Molecular Docking Simulation2018In: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 23, no 9, article id 2402Article in journal (Refereed)
    Abstract [en]

    Background: Clinacanthus nutans (C. nutans) is an Acanthaceae herbal shrub traditionally consumed to treat various diseases including diabetes in Malaysia. This study was designed to evaluate the alpha-glucosidase inhibitory activity of C. nutans leaves extracts, and to identify the metabolites responsible for the bioactivity. Methods: Crude extract obtained from the dried leaves using 80% methanolic solution was further partitioned using different polarity solvents. The resultant extracts were investigated for their alpha-glucosidase inhibitory potential followed by metabolites profiling using the gas chromatography tandem with mass spectrometry (GC-MS). Results: Multivariate data analysis was developed by correlating the bioactivity, and GC-MS data generated a suitable partial least square (PLS) model resulting in 11 bioactive compounds, namely, palmitic acid, phytol, hexadecanoic acid (methyl ester), 1-monopalmitin, stigmast-5-ene, pentadecanoic acid, heptadecanoic acid, 1-linolenoylglycerol, glycerol monostearate, alpha-tocospiro B, and stigmasterol. In-silico study via molecular docking was carried out using the crystal structure Saccharomyces cerevisiae isomaltase (PDB code: 3A4A). Interactions between the inhibitors and the protein were predicted involving residues, namely LYS156, THR310, PRO312, LEU313, GLU411, and ASN415 with hydrogen bond, while PHE314 and ARG315 with hydrophobic bonding. Conclusion: The study provides informative data on the potential alpha-glucosidase inhibitors identified in C. nutans leaves, indicating the plant's therapeutic effect to manage hyperglycemia.

  • 39.
    Patel, Seema
    et al.
    San Diego State Univ, Bioinformat & Med Informat Res Ctr, 5500 Campanile Dr, San Diego, CA 92182 USA.
    Homaei, Ahmad
    Univ Hormozgan, Fac Marine Sci & Technol, Dept Marine Biol, Bandar Abbas, Iran;Univ Hormozgan, Dept Biol, Fac Sci, Bandar Abbas, Iran.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. KTH, Sch Chem Sci & Engn, Dept Chem, Ecol Chem Grp, Stockholm, Sweden.
    Akhtar, Nadeem
    Univ Guelph, Dept Anim Biosci, Guelph, ON N1G 2W1, Canada.
    Cathepsins: Proteases that are vital for survival but can also be fatal2018In: Biomedicine and Pharmacotherapy, ISSN 0753-3322, E-ISSN 1950-6007, Vol. 105, p. 526-532Article in journal (Refereed)
    Abstract [en]

    The state of enzymes in the human body determines the normal physiology or pathology, so all the six classes of enzymes are crucial. Proteases, the hydrolases, can be of several types based on the nucleophilic amino acid or the metal cofactor needed for their activity. Cathepsins are proteases with serine, cysteine, or aspartic acid residues as the nucleophiles, which are vital for digestion, coagulation, immune response, adipogenesis, hormone liberation, peptide synthesis, among a litany of other functions. But inflammatory state radically affects their normal roles. Released from the lysosomes, they degrade extracellular matrix proteins such as collagen and elastin, mediating parasite infection, autoimmune diseases, tumor metastasis, cardiovascular issues, and neural degeneration, among other health hazards. Over the years, the different types and isoforms of cathepsin, their optimal pH and functions have been studied, yet much information is still elusive. By taming and harnessing cathepsins, by inhibitors and judicious lifestyle, a gamut of malignancies can be resolved. This review discusses these aspects, which can be of clinical relevance.

  • 40.
    Saeed, A.
    et al.
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Larik, F. A.
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Jabeen, F.
    Laurentian Univ, Cardiovasc & Metab Res Unit, 935 Ramsey Lake Rd, Sudbury, ON P3E 2C6, Canada.
    Mehfooz, H.
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Ghumro, S. A.
    Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
    El-Seedi, Hesham R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Ali, M.
    Quaid I Azam Univ, Dept Biol Sci, Islamabad 45320, Pakistan.
    Channar, P. A.
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Ashraf, H.
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Synthesis, Antibacterial and Antileishmanial Activity, Cytotoxicity, and Molecular Docking of New Heteroleptic Copper(I) Complexes with Thiourea Ligands and Triphenylphosphine2018In: Russian journal of general chemistry, ISSN 1070-3632, E-ISSN 1608-3350, Vol. 88, no 3, p. 541-550Article in journal (Refereed)
    Abstract [en]

    A series of copper(I) complexes with triphenylphosphine and N-acyl-N'-arylthioureas were synthesized and characterized by elemental analysis and IR and NMR (H-1, C-13, P-31) spectroscopy. The thiourea ligands and their copper(I) triphenylphosphine complexes were screened for antibacterial and antileishmanial activities and cytotoxicity. The synthesized compounds showed much better activity as compared to glucantime and Kanamycin used as reference drugs. The thiourea ligands showed better activity than their Cu(I) complexes. The molecular docking technique was utilized to ascertain the mechanism of action toward molecular targets (GP63 and 16S-rRNA A-site). It was found that the ligands and complexes were stabilized at the active site by electrostatic and hydrophobic forces, consistent with the corresponding experimental results. The in silico study of the binding pattern predicted that one of the synthesized ligands, N-(5-chloro-2-nitrophenyl)-N'-pentanoylthiourea, can serve as a potential surrogate for hit-to-lead generation and design of novel antibacterial and antileishmanial agents.

  • 41.
    Saeed, Aamer
    et al.
    Quaid I Azam Univ, Dept Chem, Islamabad, Pakistan.
    Faisal, Muhammad
    Quaid I Azam Univ, Dept Chem, Islamabad, Pakistan.
    Larik, Fayaz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad, Pakistan.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Channar, Pervaiz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad , Pakistan.
    Shahzad, Danish
    Quaid I Azam Univ, Dept Chem, Islamabad, Pakistan.
    Recent Progress in Pyridine Containing Heterocycles as High Performance Host Materials for Blue PHOLEDs2018In: Mini-Reviews in Organic Chemistry, ISSN 1570-193X, E-ISSN 1875-6298, Vol. 15, no 4, p. 261-273Article, review/survey (Refereed)
    Abstract [en]

    Phosphorescent Organic Light-Emitting Diodes (PHOLEDs) have an advantage of stability for a lifetime in comparison with the conventional Organic Light-Emitting Diodes (OLEDs). Green and red OLEDs have already achieved success, but for the last decade, blue OLEDs have observed a surge in the attention towards them from academia as well as the industry. There are incessant efforts devoted towards the improvement of external quantum efficiency from 25-30%. The host materials (or host compounds), hole transporting and electron transporting are the preeminent factors for the enhancement of External Quantum Efficiency (EQE). This review aims at highlighting the role of pyridine as an efficient Electron Transporting Material (ETM) for blue PHOLEDs. Pyridine having electron withdrawing nature can serve as valuable host compounds for electron transport material in PHOLEDs of a blue color. The presence of nitrogen atom in pyridine facilitates in lowering HOMO/LUMO energy levels compared to benzene ring and this assists in adding phenyl rings at the periphery of pyridine ring.

  • 42.
    Shahid, Shereena
    et al.
    Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
    Faisal, Muhammad
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Saeed, Aamer
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Ghumro, Sarfaraz Ali
    Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Rasheed, Samina
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Abbas, Nadir
    Univ Hail, Dept Chem Engn, Hail, Saudi Arabia.
    Larik, Fayaz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Channar, Pervaiz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Fattah, Tanzeela Abdul
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Ashraf, Zaman
    Allama Iqbal Open Univ, Dept Chem, Islamabad 44000, Pakistan.
    Solangi, Zulfiqar Ali
    Shah Abdul Latif Univ, Dept Chem, Khairpur, Pakistan.
    A Review on the Scope of TFDO-Mediated Oxidation in Organic Synthesis-Reactivity and Selectivity2018In: Current Organic Synthesis, ISSN 1570-1794, E-ISSN 1875-6271, Vol. 15, no 8, p. 1091-1108Article, review/survey (Refereed)
    Abstract [en]

    Dioxiranes are three-membered strained ring peroxides that are typical archetype examples of electrophilic entities. A dioxirane-based oxidant named 3-methyl(trifluoromethyl)dioxirane (TFDO) is a fluorinated analogue of the extremely valuable oxidant dimethyldioxirane (DMDO). Owing to the strained three-membered ring and presence of electron-withdrawing trifluoromethyl group, TFDO is several times more reactive than DMDO and acts as a significant chemical reagent. Moreover, TFDO exhibits high regio-, chemo- and stereo-selectivity even under unusual reaction conditions, i.e. at pH values close to neutrality and at sub-ambient temperatures. The TFDO transfers an oxygen atom to "unactivated" carbon-hydrogen bonds of alkanes as well as to the double bonds of alkenes and also helps in oxidation of compounds containing heteroatoms having a lone pair of electrons, such as sulfides and amines. TFDO-mediated oxidation is considered to be one of the main procedures in the 21st century for the synthesis of oxygen-containing organic molecules. This review throws light on the applications of TFDO in organic syntheses to provide an insight into the future research and gives a comprehensive summary of the selective functionalization of activated and non-activated organic compounds.

  • 43.
    Shahzad, Danish
    et al.
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Saeed, Aamer
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Larik, Fayaz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Channar, Pervaiz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Abbas, Qamar
    Univ Sindh, Dept Physiol, Jamshoro 76080, Pakistan.
    Alajmi, Mohamed F.
    King Saud Univ, Dept Pharmacognosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    Arshad, M. Ifzan
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Erben, Mauricio F.
    UNLP, CONICET, CEQUINOR, Dept Quim,Fac Ciencias Exactas,CCT La Plata, Blvd 120 E-60 & 64 1465, RA-1900 La Plata, Argentina.
    Hassan, Mubashir
    Kongju Natl Univ, Coll Nat Sci, Dept Biol Sci, 56 Gongjudehak Ro, Gongju 32588, Chungnam, South Korea.
    Raza, Hussain
    Kongju Natl Univ, Coll Nat Sci, Dept Biol Sci, 56 Gongjudehak Ro, Gongju 32588, Chungnam, South Korea.
    Seo, Sung-Yum
    Kongju Natl Univ, Coll Nat Sci, Dept Biol Sci, 56 Gongjudehak Ro, Gongju 32588, Chungnam, South Korea.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Novel C-2 Symmetric Molecules as -Glucosidase and -Amylase Inhibitors: Design, Synthesis, Kinetic Evaluation, Molecular Docking and Pharmacokinetics2019In: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 24, no 8, article id 1511Article in journal (Refereed)
    Abstract [en]

    A series of symmetrical salicylaldehyde-bishydrazine azo molecules, 5a-5h, have been synthesized, characterized by H-1-NMR and C-13-NMR, and evaluated for their in vitro -glucosidase and -amylase inhibitory activities. All the synthesized compounds efficiently inhibited both enzymes. Compound 5g was the most potent derivative in the series, and powerfully inhibited both -glucosidase and -amylase. The IC50 of 5g against -glucosidase was 0.35917 +/- 0.0189 mu M (standard acarbose IC50 = 6.109 +/- 0.329 mu M), and the IC50 value of 5g against -amylase was 0.4379 +/- 0.0423 mu M (standard acarbose IC50 = 33.178 +/- 2.392 mu M). The Lineweaver-Burk plot indicated that compound 5g is a competitive inhibitor of -glucosidase. The binding interactions of the most active analogues were confirmed through molecular docking studies. Docking studies showed that 5g interacts with the residues Trp690, Asp548, Arg425, and Glu426, which form hydrogen bonds to 5g with distances of 2.05, 2.20, 2.10 and 2.18 angstrom, respectively. All compounds showed high mutagenic and tumorigenic behaviors, and only 5e showed irritant properties. In addition, all the derivatives showed good antioxidant activities. The pharmacokinetic evaluation also revealed promising results

  • 44.
    Svahn, K. Stefan
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Goransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Bohlin, Lars
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Larsson, D. G. J.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
    Olsen, Björn
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
    Chryssanthou, E.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
    The search for new antibiotic substances from filamentous fungi2012In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 78, no 11, p. 1162-1162Article in journal (Other academic)
  • 45.
    Svahn, Stefan
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Bohlin, Lars
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
    Larsson, Joakim
    Olsen, Björn
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Medical Sciences, Infectious Diseases.
    Chryssanthou, Erja
    Antimicrobial activity of filamentous fungi isolated from highly antibiotic-contaminated river sediment2012In: Infection ecology & epidemiology, ISSN 2000-8686, Vol. 2, p. 11591-Article in journal (Refereed)
    Abstract [en]

    Background:

    Filamentous fungi are well known for their production of substances with antimicrobial activities, several of which have formed the basis for the development of new clinically important antimicrobial agents. Recently, environments polluted with extraordinarily high levels of antibiotics have been documented, leading to strong selection pressure on local sentinel bacterial communities. In such microbial ecosystems, where multidrug-resistant bacteria are likely to thrive, it is possible that certain fungal antibiotics have become less efficient, thus encouraging alternative strategies for fungi to compete with bacteria.

    Methods:

    In this study, sediment of a highly antibiotic-contaminated Indian river was sampled in order to investigate the presence of cultivable filamentous fungi and their ability to produce substances with antimicrobial activity.

    Results:

    Sixty one strains of filamentous fungi, predominantly various Aspergillus spp. were identified. The majority of the Aspergillus strains displayed antimicrobial activity against methicillin-resistant Staphylococcus aureus, extended-spectrum beta-lactamase-producing Escherichia coli, vancomycin-resistant Enterococcus faecalis and Candida albicans. Bioassay-guided isolation of the secondary metabolites of A. fumigatus led to the identification of gliotoxin.

    Conclusion:

    This study demonstrated proof of principle of using bioassay-guided isolation for finding bioactive molecules

  • 46.
    Ujan, Rabail
    et al.
    Univ Sindh, Dr MA Kazi Inst Chem, Jamshoro 76080, Pakistan.
    Saeed, Aamer
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Channar, Pervaiz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Larik, Fayaz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Abbas, Qamar
    Univ Sindh, Dept Physiol, Jamshoro 76080, Pakistan.
    Alajmi, Mohamed F.
    King Saud Univ, Dept Pharmacognosy, Coll Pharm, Riyadh 11451, Saudi Arabia.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Rind, Mahboob Ali
    Univ Sindh, Dr MA Kazi Inst Chem, Jamshoro 76080, Pakistan.
    Hassan, Mubashir
    Kongju Natl Univ, Coll Nat Sci, Dept Biol Sci, Gongju 314701, Chungnam, South Korea.
    Raza, Hussain
    Kongju Natl Univ, Coll Nat Sci, Dept Biol Sci, Gongju 314701, Chungnam, South Korea.
    Seo, Sung-Yum
    Kongju Natl Univ, Coll Nat Sci, Dept Biol Sci, Gongju 314701, Chungnam, South Korea.
    Drug-1,3,4-Thiadiazole Conjugates as Novel Mixed-Type Inhibitors of Acetylcholinesterase: Synthesis, Molecular Docking, Pharmacokinetics, and ADMET Evaluation2019In: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 24, no 5, article id 860Article in journal (Refereed)
    Abstract [en]

    A small library of new drug-1,3,4-thiazidazole hybrid compounds (3a-3i) was synthesized, characterized, and assessed for their acetyl cholinesterase enzyme (AChE) inhibitory and free radical scavenging activities. The newly synthesized derivatives showed promising activities against AChE, especially compound 3b (IC50 18.1 +/- 0.9 nM), which was the most promising molecule in the series, and was substantially more active than the reference drug (neostigmine methyl sulfate; IC50 2186.5 +/- 98.0 nM). Kinetic studies were performed to elucidate the mode of inhibition of the enzyme, and the compounds showed mixed-type mechanisms for inhibiting AChE. The Ki of 3b (0.0031 mu M) indicates that it can be very effective, even at low concentrations. Compounds 3a-3i all complied with Lipinski's Rule of Five, and showed high drug-likeness scores. The pharmacokinetic parameters revealed notable lead-like properties with insignificant liver and skin-penetrating effects. The structure-activity relationship (SAR) analysis indicated pi-pi interactions with key amino acid residues related to Tyr124, Trp286, and Tyr341.

  • 47.
    Zahra, Maram Hussein
    et al.
    Okayama Univ, Grad Sch Nat Sci & Technol, Div Chem & Biotechnol, Okayama 7008530, Japan.
    Salem, Tarek A. R.
    Qassim Univ, Dept Biochem, Coll Med, Al Qassim 51452, Saudi Arabia;Univ Sadat City, Genet Engn & Biotechnol Inst, Dept Mol Biol, Sadat City 32958, Egypt.
    El-Aarag, Bishoy
    Okayama Univ, Grad Sch Nat Sci & Technol, Div Chem & Biotechnol, Okayama 7008530, Japan;Menoufia Univ, Div Biochem, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt.
    Yosri, Nermeen
    Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt.
    EL-Ghlban, Samah
    Menoufia Univ, Div Biochem, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt.
    Zaki, Kholoud
    Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt.
    Marei, Amel H.
    Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt.
    Abd El-Wahed, Aida
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt;Agr Res Ctr, Plant Protect Res Inst, Dept Bee Res, Giza 12627, Egypt.
    Saeed, Aamer
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan.
    Khatib, Alfi
    Int Islamic Univ Malaysia, Dept Pharmaceut Chem, Fac Pharm, Kuantan 25200, Pahang, Malaysia.
    AlAjmi, Mohamed F.
    King Saud Univ, Coll Pharm, Pharmacognosy Grp, Riyadh 11451, Saudi Arabia.
    Shathili, Abdulrahman M.
    Al Rayan Coll, Al Rayan Res & Innovat Ctr, Medina 42541, Saudi Arabia.
    Xiao, Jianbo
    Univ Macau, Inst Chinese Med Sci, Taipa 999078, Macau, Peoples R China.
    Khalifa, Shaden A. M.
    Karolinska Univ Hosp, Clin Res Ctr, S-14186 Huddinge, Sweden;Stockholm Univ, Wenner Gren Inst, Dept Mol Biosci, SE-10691 Stockholm, Sweden.
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Menoufia Univ, Dept Chem, Fac Sci, Shibin Al Kawm 32512, Egypt;Al Rayan Coll, Al Rayan Res & Innovat Ctr, Medina 42541, Saudi Arabia;Jiangsu Univ, Coll Food & Biol Engn, Zhenjiang 212013, Jiangsu, Peoples R China.
    Alpinia zerumbet (Pers.): Food and Medicinal Plant with Potential In Vitro and In Vivo Anti-Cancer Activities2019In: Molecules, ISSN 1420-3049, E-ISSN 1420-3049, Vol. 24, no 13, article id 2495Article in journal (Refereed)
    Abstract [en]

    Background/Aim: Plants play an important role in anti-cancer drug discovery, therefore, the current study aimed to evaluate the biological activity of Alpinia zerumbet (A. zerumbet) flowers.

    Methods: The phytochemical and biological criteria of A. zerumbet were in vitro investigated as well as in mouse xenograft model.

    Results: A. zerumbet extracts, specially CH2Cl2 and MeOH extracts, exhibited the highest potent anti-tumor activity against Ehrlich ascites carcinoma (EAC) cells. The most active CH2Cl2 extract was subjected to bioassay-guided fractionation leading to isolatation of the naturally occurring 5,6-dehydrokawain (DK) which was characterized by IR, MS, H-1-NMR and C-13-NMR. A. zerumbet extracts, specially MeOH and CH2Cl2 extracts, exhibited significant inhibitory activity towards tumor volume (TV). Furthermore, A. zerumbet extracts declined the high level of malonaldehyde (MDA) as well as elevated the levels of superoxide dismutase (SOD) and catalase (CAT) in liver tissue homogenate. Moreover, DK showed anti-proliferative action on different human cancer cell lines. The recorded IC50 values against breast carcinoma (MCF-7), liver carcinoma (Hep-G2) and larynx carcinoma cells (HEP-2) were 3.08, 6.8, and 8.7 mu g/mL, respectively.

    Conclusion: Taken together, these findings open the door for further investigations in order to explore the potential medicinal properties of A. zerumbet.

  • 48. Zahran, Moustafa
    et al.
    El-Kemary, Maged
    Khalifa, Shaden
    El-Seedi, Hesham
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Spectral studies of silver nanoparticles biosynthesized by Origanum majorana2018In: Green Processing and Synthesis, ISSN 2191-9542, E-ISSN 2191-9550, Vol. 7, no 2, p. 100-105Article in journal (Refereed)
    Abstract [en]

    Silver nanoparticles (AgNPs) were biologically synthesized in an eco-friendly manner using aqueous leaf extract of Origanum majorana plant and silver nitrate (AgNO 3) solution. Size, shape, and crystallinity of the biosynthesized AgNPs were determined by using a transmission electron microscope (TEM). Zeta potential analyzer was used to prove the stability of the metallic nanoparticles, while Fourier transform infrared spectroscopy was used to identify the bioreducing and capping agents. AgNPs were electrochemically investigated using cyclic voltammetry (CV), while the optical properties of the metallic nanoparticles were studied using UV-Vis and fluorescence spectroscopies. According to TEM images, AgNPs are spherical with an average size of 35 nm. TEM also refers to the presence of mono and polycrystalline AgNPs. The value of zeta potential (-39 mV) proved the stability of AgNPs caused by capping molecules of O. majorana plant. CV studies showed that AgNPs were electrochemically investigated at 0.39 mV. AgNPs showed a surface plasmon resonance peak at 440 nm, while the emission peak was detected at 466 nm. These nanoparticles are promising for many industrial and medical applications.

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