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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.
    Abdillahi, Suado M.
    et al.
    Lund Univ, Div Infect Med, Dept Clin Sci, Tornavagen 10, S-22184 Lund, Sweden.
    Maass, Tobias
    Univ Cologne, Fac Med, Ctr Biochem, Ctr Mol Med Cologne, D-50931 Cologne, Germany.
    Kasetty, Gopinath
    Lund Univ, Div Resp Med & Allergol, Dept Clin Sci, S-22184 Lund, Sweden.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Baumgarten, Maria
    Lund Univ, Div Infect Med, Dept Clin Sci, Tornavagen 10, S-22184 Lund, Sweden.
    Tati, Ramesh
    Lund Univ, Div Infect Med, Dept Clin Sci, Tornavagen 10, S-22184 Lund, Sweden.
    Nordin, Sara L.
    Lund Univ, Div Infect Med, Dept Clin Sci, Tornavagen 10, S-22184 Lund, Sweden.
    Walse, Björn
    Sarom Biostruct AB, S-22363 Lund, Sweden.
    Wagener, Raimund
    Univ Cologne, Fac Med, Ctr Biochem, Ctr Mol Med Cologne, D-50931 Cologne, Germany.
    Schmidtchen, Artur
    Lund Univ, Div Dermatol & Venereol, Dept Clin Sci, S-22184 Lund, Sweden;Univ Copenhagen, Bispebjerg Hosp, Dept Biomed Sci, Copenhagen Wound Healing Ctr, DK-2400 Copenhagen, Denmark.
    Mörgelin, Matthias
    Lund Univ, Div Infect Med, Dept Clin Sci, Tornavagen 10, S-22184 Lund, Sweden;Colzyx AB, S-22381 Lund, Sweden.
    Collagen VI Contains Multiple Host Defense Peptides with Potent In Vivo Activity2018In: Journal of Immunology, ISSN 0022-1767, E-ISSN 1550-6606, Vol. 201, no 3, p. 1007-1020Article in journal (Refereed)
    Abstract [en]

    Collagen VI is a ubiquitous extracellular matrix component that forms extensive microfibrillar networks in most connective tissues. In this study, we describe for the first time, to our knowledge, that the collagen VI von Willebrand factor type A like domains exhibit a broad-spectrum antimicrobial activity against Gram-positive and Gram-negative bacteria in human skin infections in vivo. In silico sequence and structural analysis of VWA domains revealed that they contain cationic and amphipathic peptide sequence motifs, which might explain the antimicrobial nature of collagen VI. In vitro and in vivo studies show that these peptides exhibited significant antibacterial activity against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa through membrane disruption. Our findings shed new light on the role of collagen VI derived peptides in innate host defense and provide templates for development of peptide-based antibacterial therapies.

  • 4.
    Ahnfelt, Nils-Otto
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Uppsala University, Disciplinary Domain of Humanities and Social Sciences, Faculty of Arts, Department of History of Science and Ideas.
    Fors, Hjalmar
    Uppsala University, Disciplinary Domain of Humanities and Social Sciences, Faculty of Arts, Department of History of Science and Ideas. Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Hagströmer Library, Stockholm, Sweden..
    Reconstructing early modern pharmacy through "Elixir amarum Hiaernei" and its Theriac ancestor2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 5.
    Alajlani, M.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Karl Franzens Univ Graz, Inst Pharmaceut Sci, Dept Pharmacognosy, Univ Pl 4, A-8010 Graz, Austria..
    Backlund, Anders
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Predicting the mechanism of action of antituberculosis agents using chemical global positioning system - natural product2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 6.
    Andersson, H. S.
    et al.
    Linnaeus Univ, Ctr Biomat Chem, Dept Chem & Biomed Sci, Norra Vagen 49, S-39234 Kalmar, Sweden..
    Jacobsson, Erik
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Eriksson, Camilla
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Hedstrom, M.
    Lund Univ, Dept Biotechnol, Box 118, S-22100 Lund, Sweden..
    Seth, H.
    Univ Gothenburg, Dept Biol & Environm Sci, Box 463, S-40530 Gothenburg, Sweden..
    Sundberg, P.
    Univ Gothenburg, Dept Biol & Environm Sci, Box 463, S-40530 Gothenburg, Sweden..
    Rosengren, K. J.
    Univ Queensland, Sch Biomed Sci, Brisbane, Qld 4072, Australia..
    Strand, M.
    Univ Gothenburg, Dept Biol & Environm Sci, Box 463, S-40530 Gothenburg, Sweden.;Swedish Univ Agr Sci, Swedish Species Informat Ctr, Backlosavagen 10, S-75651 Uppsala, Sweden..
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    The toxicity of ribbon worms: Alpha-nemertides or tetrodotoxin, or both?2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 7.
    Anwar, J.
    et al.
    Univ Agr, Dept Agr Chem, Peshawar 25100, Pakistan..
    Muhammad, Taj
    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.
    Iqbal, Z.
    Univ Agr, Dept Agr Chem, Peshawar 25100, Pakistan..
    Fungi as a source for antibacterial compounds2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 8.
    Backlund, Anders
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Bioactivity mapping of chemical property space - possible applications in natural products research2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 9.
    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.

  • 10.
    Cárdenas, Paco
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Organismal Biology, Systematic Biology.
    Moore, Jon A.
    Wilkes Honors College, Florida Atlantic University.
    First records of Geodia demosponges from the New England seamounts, an opportunity to test the use of DNA mini-barcodes on museum specimens2017In: Marine Biodiversity, ISSN 1867-1616, E-ISSN 1867-1624Article in journal (Refereed)
    Abstract [en]

    We report the first records of the sponge genus Geodia (Demospongiae, Tetractinellida, Geodiidae) from the New England Seamounts and Muir Seamount, at lower bathyal depths. Nine specimens collected between 2000 and 2005 belong to two boreal species (Geodia macandrewii and Geodia barretti) and a temperate species (Geodia megastrella). These records extend the distributions of these deep-sea amphi-Atlantic species to the west. Most of these specimens were originally fixed in formalin, which substantially degraded the DNA. We nonetheless managed to sequence two cytochrome c oxidase subunit I (COI) mini-barcodes: the universal mini-barcode at the 5′ end of the Folmer barcode (130 bp) and a newly proposed mini-barcode at the 3′ end of the Folmer barcode (296 bp). These mini-barcodes unambiguously confirmed our identifications. As an additional test, we also successfully sequenced these two mini-barcodes from the holotype of G. barretti, collected in 1855. We conclude by advocating the use of mini-barcodes on formalin-fixed or old specimens with degraded DNA.

  • 11.
    Cárdenas, Paco
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Institut Méditerranéen de Biodiversité et d’Ecologie marine et continentale, CNRS, Aix Marseille Univ., IRD, Avignon Univ., Station Marine d’Endoume, Marseille, France.
    Vacelet, Jean
    Institut Méditerranéen de Biodiversité et d’Ecologie marine et continentale, CNRS, Aix Marseille Univ., IRD, Avignon Univ., Station Marine d’Endoume, Marseille, France. .
    Chevaldonné, Pierre
    Institut Méditerranéen de Biodiversité et d’Ecologie marine et continentale, CNRS, Aix Marseille Univ., IRD, Avignon Univ., Station Marine d’Endoume, Marseille, France. .
    Pérez, Thierry
    Institut Méditerranéen de Biodiversité et d’Ecologie marine et continentale, CNRS, Aix Marseille Univ., IRD, Avignon Univ., Station Marine d’Endoume, Marseille, France. .
    Xavier, Joana R.
    Department of Biological Sciences and K.G. Jebsen Centre for Deep-Sea Research, University of Bergen, Bergen, Norway.
    From marine caves to the deep sea, a new look at Caminella (Demospongiae, Geodiidae) in the Atlanto-Mediterranean region2018In: Zootaxa, ISSN 1175-5326, E-ISSN 1175-5334, Vol. 4466, no 1, p. 174-196Article in journal (Refereed)
    Abstract [en]

    Caminella Lendenfeld, 1894 is a poorly known Geodiidae genus with unclear phylogenetic relationships. In order to find new lines of evidence that could shed light on the evolutionary history of Caminella, we decided to revise type material and museum material, as well as examine new material from underwater caves and deep-sea ecosystems. In doing so, we formally show that Isops maculosus Vosmaer, 1894 and Caminella loricata Lendenfeld, 1894 are junior synonyms of Caminella intuta (Topsent, 1892). We discuss different spicule morphological phenotypes in C. intuta, which may be linked to silica availability. We also discovered two new species of deep-sea Caminella: 1) from Cape Verde (Caminella caboverdensis sp. nov.) and 2) from seamounts located south of the Azores archipelago and the North of Spain (Caminella pustula sp. nov.). We reveal that Caminella sterrasters have complex surface microstructures, unique amongst the Geodiidae, where actin tips are linked to each other. Molecular markers (COI, 28S (C1-D2) and 18S) sequenced for some specimens led to new phylogenetic analyses, which continue to suggest a close relationship of Caminella with the Erylinae and Calthropella; these affinities are discussed in light of morphological characters.

  • 12.
    de Boer, Hugo
    et al.
    Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Organismal Biology, Systematic Biology. Univ Oslo, Nat Hist Museum, POB 1172 Blindern, Oslo, Norway.
    Newman, Mark
    Royal Bot Garden Edinburgh, Edinburgh, Midlothian, Scotland.
    Poulsen, Axel Dalberg
    Univ Oslo, Nat Hist Museum, POB 1172 Blindern, Oslo, Norway; Royal Bot Garden Edinburgh, Edinburgh, Midlothian, Scotland.
    Droop, A. Jane
    Royal Bot Garden Edinburgh, Edinburgh, Midlothian, Scotland.
    Fer, Tomas
    Charles Univ Prague, Fac Sci, Dept Bot, Prague, Czech Republic.
    Hien, Le Thi Thu
    Vietnam Acad Sci & Technol, Inst Genome Res, Hanoi, Vietnam.
    Hlavata, Kristyna
    Charles Univ Prague, Fac Sci, Dept Bot, Prague, Czech Republic.
    Lamxay, Vichith
    Natl Univ Laos, Fac Nat Sci, Dept Biol, Dong Dok, Vientiane, Laos.
    Richardson, James E.
    Royal Bot Garden Edinburgh, Edinburgh, Midlothian, Scotland; Univ Rosario, Programa Biol, Carrera, Bogota, Colombia.
    Steffen, Karin
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Leong-Skornickova, Jana
    Singapore Bot Gardens, Natl Parks Board, Herbarium, Singapore, Singapore.
    Convergent morphology in Alpinieae (Zingiberaceae): Recircumscribing Amomum as a monophyletic genus2018In: Taxon, ISSN 0040-0262, E-ISSN 1996-8175, Vol. 67, no 1, p. 6-36Article in journal (Refereed)
    Abstract [en]

    The tropical ginger genus Amomum (Zingiberaceae) has always posed challenges for classification based on morphological characters. Previous molecular phylogenetic studies showed Amomum to be paraphyletic but limited sampling and absence of the data of the type Amomum subulatum made it impossible to resolve the paraphyly and make nomenclatural changes. Here, Amomum is further investigated in a multi-marker phylogenetic framework using matK and nrITS including multiple accessions of the type, the genus Elettaria and additional accessions of Amomum, Alpinia, Elettariopsis, Geocharis, Geostachys and Hornstedtia. Amomum is shown to consist of nine clades and Alpinia of six. The genera Elettaria, Elettariopsis, Plagiostachys, and species in Hornstedtia are nested within these clades. Morphological studies of species previously subsumed in Amomum support recognition of new genera that correspond to well-delimited clades in the phylogenetic framework presented here. Recircumscription of the paraphyletic genus Amomum facilitates identification and creates nomenclatural stability. Three genera, Conamomum, Meistera and Wurfbainia, are resurrected, and three new genera Epiamomum, Lanxangia and Sundamomum are described, together with a key to the genera and a nomenclatural synopsis placing 384 specific names (incl. all synonyms) into the new generic framework. Of these 129 represent new combinations and 3 are replacement names. Types of Geocharis and Geostachys are designated. Further studies and specific sampling will be needed to resolve other branches of Alpinioideae containing other polyphyletic genera.

  • 13.
    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.

  • 14.
    Enmark, Martin
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Karlstad Univ, Dept Engn & Chem Sci, SE-65188 Karlstad, Sweden.
    Glenne, Emelie
    Karlstad Univ, Dept Engn & Chem Sci, SE-65188 Karlstad, Sweden.
    Lesko, Marek
    Karlstad Univ, Dept Engn & Chem Sci, SE-65188 Karlstad, Sweden;Rzeszow Univ Technol, Dept Chem & Proc Engn, PL-35959 Rzeszow, Poland.
    Weinmann, Annika Langborg
    AstraZeneca, IMED Biotech Unit, Early Product Dev, Pharmaceut Sci, Gothenburg, Sweden.
    Leek, Tomas
    AstraZeneca, IMED Biotech Unit, Inflammat & Autoimmun, Med Chem,Resp, Gothenburg, Sweden.
    Kaczmarski, Krzysztof
    Rzeszow Univ Technol, Dept Chem & Proc Engn, PL-35959 Rzeszow, Poland.
    Klarqvist, Magnus
    AstraZeneca, IMED Biotech Unit, Early Product Dev, Pharmaceut Sci, Gothenburg, Sweden.
    Samuelsson, Jorgen
    Karlstad Univ, Dept Engn & Chem Sci, SE-65188 Karlstad, Sweden.
    Fornstedt, Torgny
    Karlstad Univ, Dept Engn & Chem Sci, SE-65188 Karlstad, Sweden.
    Investigation of robustness for supercritical fluid chromatography separation of peptides: Isocratic vs gradient mode2018In: Journal of Chromatography A, ISSN 0021-9673, E-ISSN 1873-3778, Vol. 1568, p. 177-187Article in journal (Refereed)
    Abstract [en]

    We investigated and compared the robustness of supercritical fluid chromatography (SFC) separations of the peptide gramicidin, using either isocratic or gradient elution. This was done using design of experiments in a design space of co-solvent fraction, water mass fraction in co-solvent, pressure, and temperature. The density of the eluent (CO2-MeOH-H2O) was experimentally determined using a Coriolis mass flow meter to calculate the volumetric flow rate required by the design. For both retention models, the most important factor was the total co-solvent fraction and water mass fraction in co-solvent. Comparing the elution modes, we found that gradient elution was more than three times more robust than isocratic elution. We also observed a relationship between the sensitivity to changes and the gradient steepness and used this to draw general conclusions beyond the studied experimental system. To test the robustness in a practical context, both the isocratic and gradient separations were transferred to another laboratory. The gradient elution was highly reproducible between laboratories, whereas the isocratic system was not. Using measurements of the actual operational conditions (not the set system conditions), the isocratic deviation was quantitatively explained using the retention model. The findings indicate the benefits of using gradient elution in SFC as well as the importance of measuring the actual operational conditions to be able to explain observed differences between laboratories when conducting method transfer.

  • 15.
    Eriksson, Camilla
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Gunasekera, Sunithi
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Cerqueira, C.
    Karolinska Inst, Karolinska Univ Hosp, Dept Med, Rheumatol Unit, Stockholm, Sweden..
    Jacobsson, P. J.
    Karolinska Inst, Karolinska Univ Hosp, Dept Med, Rheumatol Unit, Stockholm, Sweden..
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Synthesis of cyclic citrullinated peptides targeting rheumatoid arthritis autoantibodies based on sunflower trypsin inhibitors2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 16.
    Forde, Eanna
    et al.
    Royal Coll Surgeons Ireland, Dept Chem, 123 St Stephens Green, Dublin 2, Ireland;Royal Coll Surgeons Ireland, Dept Clin Microbiol, Dublin 9, Ireland.
    Shafiy, Ghady
    Royal Coll Surgeons Ireland, Dept Chem, 123 St Stephens Green, Dublin 2, Ireland;Royal Coll Surgeons Ireland, Dept Clin Microbiol, Dublin 9, Ireland.
    Fitzgerald-Hughes, Deirdre
    Royal Coll Surgeons Ireland, Dept Clin Microbiol, Dublin 9, Ireland.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Devocelle, Marc
    Royal Coll Surgeons Ireland, Dept Chem, 123 St Stephens Green, Dublin 2, Ireland.
    Action of antimicrobial peptides and their prodrugs on model and biological membranes2018In: Journal of Peptide Science, ISSN 1075-2617, E-ISSN 1099-1387, Vol. 24, no 7, article id e3086Article in journal (Refereed)
    Abstract [en]

    Antimicrobial peptides (AMPs) are promising broad-spectrum antibiotic candidates in the wake of multi-drug resistant pathogens. Their clinical use still requires a solution based on lead optimisation and/ or formulation to overcome certain limitations, such as unwanted cytotoxicity. A prodrug approach could overcome this safety barrier and can be achieved through reversible reduction or neutralisation of the AMPs' net cationic charge. By prodrug activation through pathogen associated enzymes, this approach could increase the therapeutic index of membrane active peptides. P18, a cecropin/ magainin hybrid, and WMR, a myxinidin analogue from hagfish, were used as templates for the design strategy. The membrane permeabilizing activities of these AMPs and their prodrugs are reported here for liposomes of either Escherichia coli polar lipid extract or a human model lipid system of phosphatidylcholine and cholesterol. These results are compared with their antibacterial and haemolytic activities. Overall, correlation between liposome permeabilization and the corresponding bioactivity is observed and indicate that the broad-spectrum antibacterial effect exerted by these peptides is associated with membrane disruption. Furthermore, the prodrug modification had a general negative influence on membrane disruption and bioactivity, notably as much on bacterial as on human membranes. This prodrug strategy is particularly successful when complete neutralisation of the AMP's net charge occurs. Thus, on-target selectivity between bacterial and human membranes can be improved, which may be used to prevent the unnecessary exposure of host cells and commensal bacteria to active AMPs.

  • 17.
    Gunasekera, Sunithi
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Fernandes-Cerqueira, C.
    Karolinska Inst, Dept Med, Rheumatol Unit, S-17176 Solna, Sweden..
    Eriksson, Camilla
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Jakobsson, P. J.
    Karolinska Inst, Dept Med, Rheumatol Unit, S-17176 Solna, Sweden..
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Circular disulfide-rich peptide scaffolds as anti-citrullinated peptide antibody inhibitors2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 18.
    Gunasekera, Sunithi
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Fernandes-Cerqueira, Catia
    Karolinska Inst, Karolinska Univ Hosp, Dept Med Solna, Rheumatol Unit, Rheumatol Clin D2 01, S-17176 Stockholm, Sweden.
    Wennmalm, Stefan
    Royal Inst Technol KTH, Scilifelab, Appl Phys, Expt Biomol Phys, Tomtebodavagen 23, S-17165 Stockholm, Sweden.
    Wahamaa, Heidi
    Karolinska Inst, Karolinska Univ Hosp, Dept Med Solna, Rheumatol Unit, Rheumatol Clin D2 01, S-17176 Stockholm, Sweden.
    Sommarin, Yngve
    Eurodiagnost AB, S-21224 Malmo, Sweden.
    Catrina, Anca, I
    Karolinska Inst, Karolinska Univ Hosp, Dept Med Solna, Rheumatol Unit, Rheumatol Clin D2 01, S-17176 Stockholm, Sweden.
    Jakobsson, Per-Johan
    Karolinska Inst, Karolinska Univ Hosp, Dept Med Solna, Rheumatol Unit, Rheumatol Clin D2 01, S-17176 Stockholm, Sweden.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Stabilized Cyclic Peptides as Scavengers of Autoantibodies: Neutralization of Anticitrullinated Protein/Peptide Antibodies in Rheumatoid Arthritis2018In: ACS Chemical Biology, ISSN 1554-8929, E-ISSN 1554-8937, Vol. 13, no 6, p. 1525-1535Article in journal (Refereed)
    Abstract [en]

    The occurrence of autoantibodies is a hallmark of rheumatoid arthritis, specifically those autoantibodies targeting proteins containing the arginine-derived amino acid citrulline. There is strong evidence showing that the occurrence of anticitrullinated protein/peptide antibodies (ACPA) are involved in disease progression, and ACPA was recently shown to induce pain in animals. Here, we explore a novel concept useful for research, diagnostics, and possibly therapy of autoimmune diseases, namely, to directly target and neutralize autoantibodies using peptide binders. A high-affinity peptide-based scavenger of ACPA was developed by grafting a citrullinated epitope derived from human fibrinogen into a naturally occurring stable peptide scaffold. The best scavenger comprises the truncated epitope alpha-fibrinogen, [Cit573]fib(566-580), grafted into the scaffold sunflower trypsin inhibitor-1, SFTI-1. The final peptide demonstrates low nanomolar apparent affinity and superior stability.

  • 19.
    Gunasekera, Sunithi
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Muhammad, Taj
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Rosengren, K. Johan
    Univ Queensland, Sch Biomed Sci, Brisbane, Qld 4072, Australia.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Alanine and Lysine Scans of the LL-37-Derived Peptide Fragment KR-12 Reveal Key Residues for Antimicrobial Activity2018In: ChemBioChem (Print), ISSN 1439-4227, E-ISSN 1439-7633, Vol. 19, no 9, p. 931-939Article in journal (Refereed)
    Abstract [en]

    The human host defence peptide LL-37 is a broad-spectrum antibiotic with immunomodulatory functions. Residues 18-29 in LL-37 have previously been identified as a minimal peptide (KR-12) that retains antibacterial activity with decreased cytotoxicity. In this study, analogues of KR-12 were generated by Ala and Lys scans to identify key elements for activity. These were tested against a panel of human pathogens and for membrane permeabilisation on liposomes. Replacements of hydrophobic and cationic residues with Ala were detrimental for antibiotic potency. Substitutions by Lys increased activity, as long as the increase in cationic density did not disrupt the amphiphilic disposition of the helical structure. Importantly, substitutions showed differential effects against different organisms. Replacement of Gln5 with Lys and Asp9 with Ala or Lys improved the broad-spectrum activity most, each resulting in up to an eightfold increase in potency against Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans. The improved analogues displayed no significant toxicity against human cells, and thus, KR-12 is a tuneable template for antibiotic development.

  • 20.
    Göransson, Ulf
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Gunasekera, Sunithi
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Malik, S.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Park, S.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Slazak, Blazej
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Jacobsson, Erik
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Eriksson, Camilla
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Andersson, H.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Peptide biodiscovery from plants and animals: structure to function2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 21.
    Henz, Astrid
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Buonfiglio, R.
    AstraZeneca R&D, Discovery Sci, Chem Innovat Ctr, Computat Chem, S-43183 Molndal, Sweden..
    Kogej, T.
    AstraZeneca R&D, Discovery Sci, Chem Innovat Ctr, Computat Chem, S-43183 Molndal, Sweden..
    Backlund, Anders
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Phylogenetic relationships through the lens of chemoinformatic methods2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 22.
    Jacobsson, Erik
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Andersson, H. S.
    Linnaeus Univ, Dept Chem & Biomed Sci, Ctr Biomat Chem, Kalmar, Sweden..
    Strand, M.
    Swedish Univ Agr Sci, Swedish Species Informat Ctr, Uppsala, Sweden..
    Lebbe, E.
    Univ Leuven KU Leuven, Toxicol & Pharmacol, O&N 2,POB 992,Herestr 49, B-3000 Leuven, Belgium..
    Eriksson, Camilla
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Peigneur, S.
    Univ Leuven KU Leuven, Toxicol & Pharmacol, O&N 2,POB 992,Herestr 49, B-3000 Leuven, Belgium..
    Rosengren, J.
    Univ Queensland, Sch Biomed Sci, Brisbane, Qld 4072, Australia..
    Tytgat, J.
    Univ Leuven KU Leuven, Toxicol & Pharmacol, O&N 2,POB 992,Herestr 49, B-3000 Leuven, Belgium..
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Peptide toxins from the longest animal on earth2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 23.
    Jacobsson, Erik
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Andersson, Håkan S.
    Linnaeus Univ, Ctr Biomat Chem, Dept Chem & Biomed Sci, Kalmar, Sweden..
    Strand, Malin
    Swedish Univ Agr Sci, Swedish Species Informat Ctr, Uppsala, Sweden..
    Peigneur, Steve
    Univ Leuven, KU Leuven, Toxicol & Pharmacol, O&N 2,POB 992,Herestr 49, B-3000 Leuven, Belgium..
    Eriksson, Camilla
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Lodén, Henrik
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences. Uppsala University, Science for Life Laboratory, SciLifeLab.
    Shariatgorji, Mohammadreza
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences. Uppsala University, Science for Life Laboratory, SciLifeLab.
    Andrén, Per E.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences. Uppsala University, Science for Life Laboratory, SciLifeLab.
    Lebbe, Eline K. M.
    Univ Leuven, KU Leuven, Toxicol & Pharmacol, O&N 2,POB 992,Herestr 49, B-3000 Leuven, Belgium..
    Rosengren, K. Johan
    Univ Queensland, Sch Biomed Sci, Brisbane, Qld 4072, Australia..
    Tytgat, Jan
    Univ Leuven, KU Leuven, Toxicol & Pharmacol, O&N 2,POB 992,Herestr 49, B-3000 Leuven, Belgium..
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Peptide ion channel toxins from the bootlace worm, the longest animal on Earth2018In: Scientific Reports, ISSN 2045-2322, E-ISSN 2045-2322, Vol. 8, article id 4596Article in journal (Refereed)
    Abstract [en]

    Polypeptides from animal venoms have found important uses as drugs, pharmacological tools, and within biotechnological and agricultural applications. We here report a novel family of cystine knot peptides from nemertean worms, with potent activity on voltage-gated sodium channels. These toxins, named the alpha-nemertides, were discovered in the epidermal mucus of Lineus longissimus, the 'bootlace worm' known as the longest animal on earth. The most abundant peptide, the 31-residue long alpha-1, was isolated, synthesized, and its 3D NMR structure determined. Transcriptome analysis including 17 species revealed eight alpha-nemertides, mainly distributed in the genus Lineus. alpha-1 caused paralysis and death in green crabs (Carcinus maenas) at 1 mu g/kg (similar to 300 pmol/kg). It showed profound effect on invertebrate voltage-gated sodium channels (e.g. Blattella germanica Na(v)1) at low nanomolar concentrations. Strong selectivity for insect over human sodium channels indicates that a-nemertides can be promising candidates for development of bioinsecticidal agents.

  • 24.
    Lai, K. H.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
    Lu, M. C.
    Natl Dong Hwa Univ, Grad Inst Marine Biotechnol, Pingtung 944, Taiwan.;Natl Museum Marine Biol & Aquarium, Pingtung 944, Taiwan..
    Chang, F. R.
    Kaohsiung Med Univ, Grad Inst Nat Prod, Coll Pharm, Kaohsiung 807, Taiwan.;Kaohsiung Med Univ Hosp, Ctr Canc, Kaohsiung 80708, Taiwan.;Kaohsiung Med Univ, Res Ctr Nat Prod & New Drug, Kaohsiung 80708, Taiwan..
    Su, J. H.
    Natl Dong Hwa Univ, Grad Inst Marine Biotechnol, Pingtung 944, Taiwan.;Natl Museum Marine Biol & Aquarium, Pingtung 944, Taiwan..
    El-Shazly, M.
    Kaohsiung Med Univ, Grad Inst Nat Prod, Coll Pharm, Kaohsiung 807, Taiwan.;Ain Shams Univ, Fac Pharm, Dept Pharmacognosy & Nat Prod Chem, Org African Unity St, Cairo 11566, Egypt..
    Du, Y. C.
    Kaohsiung Med Univ, Grad Inst Nat Prod, Coll Pharm, Kaohsiung 807, Taiwan..
    Wu, T. Y.
    Kaohsiung Med Univ, Grad Inst Nat Prod, Coll Pharm, Kaohsiung 807, Taiwan..
    Hsu, Y. M.
    Kaohsiung Med Univ, Grad Inst Nat Prod, Coll Pharm, Kaohsiung 807, Taiwan..
    Backlund, Anders
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Wu, Y. C.
    Kaohsiung Med Univ, Grad Inst Nat Prod, Coll Pharm, Kaohsiung 807, Taiwan.;China Med Univ, Sch Pharm, Coll Pharm, Taichung 40402, Taiwan.;China Med Univ Hosp, Chinese Med Res & Dev Ctr, Taichung 40447, Taiwan.;China Med Univ Hosp, Ctr Mol Med, Taichung 40447, Taiwan..
    Antileukemic sesterterpenoids from a marine sponge, Luffariella sp.2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 25.
    Liu, Xiaojie
    et al.
    Leiden Univ, Inst Biol, Nat Prod Lab, NL-2333 BE Leiden, Netherlands..
    Ahlgren, Samantha
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Leiden Univ, Inst Biol, Nat Prod Lab, NL-2333 BE Leiden, Netherlands.
    Korthout, Henrie A. A. J.
    Fytagoras BV, NL-2333 BE Leiden, Netherlands..
    Salome-Abarca, Luis F.
    Leiden Univ, Inst Biol, Nat Prod Lab, NL-2333 BE Leiden, Netherlands..
    Bayona, Lina M.
    Leiden Univ, Inst Biol, Nat Prod Lab, NL-2333 BE Leiden, Netherlands..
    Verpoorte, Robert
    Leiden Univ, Inst Biol, Nat Prod Lab, NL-2333 BE Leiden, Netherlands..
    Choi, Young Hae
    Leiden Univ, Inst Biol, Nat Prod Lab, NL-2333 BE Leiden, Netherlands.;Kyung Hee Univ, Coll Pharm, Seoul 02447, South Korea..
    Broad range chemical profiling of natural deep eutectic solvent extracts using a high performance thin layer chromatography-based method2018In: Journal of Chromatography A, ISSN 0021-9673, E-ISSN 1873-3778, Vol. 1532, p. 198-207Article in journal (Refereed)
    Abstract [en]

    Natural deep eutectic solvents (NADES) made mainly with abundant primary metabolites are being increasingly applied in green chemistry. The advantages of NADES as green solvents have led to their use in novel green products for the food, cosmetics and pharma markets. However, one of the main difficulties encountered in the development of novel products and their quality control arises from their low vapour pressure and high viscosity. These features create the need for the development of new analytical methods suited to this type of sample. In this study, such a method was developed and applied to analyse the efficiency of a diverse set of NADES for the extraction of compounds of interest from two model plants, Ginkgo biloba and Panax ginseng. The method uses high-performance thin-layer chromatography (HPTLC) coupled with multivariate data analysis (MVDA). It was successfully applied to the comparative quali- and quantitative analysis of very chemically diverse metabolites (e.g., phenolics, terpenoids, phenolic acids and saponins) that are present in the extracts obtained from the plants using six different NADES. The composition of each NADES was a combination of two or three compounds mixed in defined molar ratios; malic acid-choline chloride (1:1), malic acid-glucose (1:1), choline chloride-glucose (5:2), malic acid-proline (1:1), glucose-fructose-sucrose (1:1:1) and glycerol-proline-sucrose (9:4:1). Of these mixtures, malic acid-choline chloride (1:1) and glycerol-proline-sucrose (1:1:1) for G. biloba leaves, and malic acid-choline chloride (1:1) and malic acid-glucose (1:1) for P. ginseng leaves and stems showed the highest yields of the target compounds. Interestingly, none of the NADES extracted ginkgolic acids as much as the conventional organic solvents. As these compounds are considered to be toxic, the fact that these NADES produce virtually ginkgolic acid-free extracts is extremely useful. The effect of adding different volumes of water to the most efficient NADES was also evaluated and the results revealed that there is a great influence exerted by the water content, with maximum yields of ginkgolides, phenolics and ginsenosides being obtained with approximately 20% water (w/w).

  • 26.
    Luis Carballo, Jose
    et al.
    Univ Nacl Autonoma Mexico, Inst Ciencias Mar & Limnol, Unidad Acad Mazatlan, Ave Joel Montes Camarena S-N,POB 811, Mazatlan 82000, Sin, Mexico.
    Bautista-Guerrero, Eric
    Univ Guadalajara, Ctr Invest Costeras, Ctr Univ Costa, Lab Ecol Marina, Ave Univ 2013 Del, Puerto Vallarta 48280, Jalisco, Mexico.
    Cárdenas, Paco
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Antonio Cruz-Barraza, Jose
    Univ Nacl Autonoma Mexico, Inst Ciencias Mar & Limnol, Unidad Acad Mazatlan, Ave Joel Montes Camarena S-N,POB 811, Mazatlan 82000, Sin, Mexico.
    Maria Aguilar-Camacho, Jose
    Natl Univ Ireland Galway, Sch Nat, Sci, Zool,Ryan Inst, Univ Rd, Galway, Ireland.
    Molecular and morphological data from Thoosidae in favour of the creation of a new suborder of Tetractinellida2018In: Systematics and Biodiversity, ISSN 1477-2000, E-ISSN 1478-0933, Vol. 16, no 5, p. 512-521Article in journal (Refereed)
    Abstract [en]

    The Thoosidae (Porifera, Demospongiae, Tetractinellida) currently includes the genera Thoosa, Alectona, and Delectona. To this date, molecular data are only available for Alectona. In this study, the phylogenetic affinities of the genera Thoosa and Alectona have been investigated with the species T. mismalolli, T. calpulli, and T. purpurea from the Mexican Pacific using morphology and three molecular loci: the mitochondrial cytochrome oxidase subunit 1 (CO1 mtDNA), 28S rRNA (fragment D2), and 18S rRNA. Morphology and embryology showed that these genera are quite different from the rest of the tetractinellids because larvae of Alectona and Thoosa have unique features in sponges, such as the presence of monaxonic discs in Thoosa and tetraxonic discs in Alectona which disappear in the adult stages. A phylogenetic analysis using selected species from the order Tetractinellida revealed that Thoosa groups with Alectona thus confirming morphological studies. The peculiarities in spiculation and embryology of the Thoosa and Alectona larvae, which are markedly different from species belonging to the suborders Astrophorina and Spirophorina and their distant phylogenetic position (based on three molecular loci), suggest that Thoosidae could be placed in the new suborder Thoosina.

  • 27.
    Mohotti, S.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Univ Colombo, Fac Sci, Dept Chem, Thurstan Rd, Colombo 00300, Sri Lanka..
    Rajendran, S.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Muhammad, Taj
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Burman, R.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Hellman, Björn
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
    de Silva, E. D.
    Univ Colombo, Fac Sci, Dept Chem, Thurstan Rd, Colombo 00300, Sri Lanka..
    Goransson, U.
    Univ Colombo, Fac Sci, Dept Chem, Thurstan Rd, Colombo 00300, Sri Lanka..
    Hettiarachchi, C. M.
    Univ Colombo, Fac Sci, Dept Chem, Thurstan Rd, Colombo 00300, Sri Lanka..
    Gunasekera, Sunithi
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    A bioactivity-guided screening of Sri Lankan plants in the search for novel antibacterial and anticancer agents2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 28.
    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.

  • 29.
    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.

  • 30.
    Muhammad, Taj
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Gunasekera, Sunithi
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Strömstedt, Adam A.
    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.
    Engineering of KR-12: A minimalized domain derived from human host defense peptide LL-37 into a potent antimicrobial drug lead2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 31.
    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.

  • 32.
    Nyström, Lina
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
    Al-Rammahi, Noor
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
    Malekkhaiat Häffner, Sara
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Browning, Kathryn L.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
    Malmsten, Martin
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
    Avidin-biotin cross-linked microgel multilayers as carriers for antimicrobial peptidesIn: Article in journal (Refereed)
  • 33.
    Nyström, Lina
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
    Nordström, Randi
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Saunders, Brian
    Univ Manchester, Manchester, Lancs, England.
    Alvarez-Asencio, Ruben
    KTH, Div Surface Corros Chem, Stockholm, Sweden.
    Rutland, Mark
    KTH, Div Surface Corros Chem, Stockholm, Sweden.
    Malmsten, Martin
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
    Peptide-loaded microgels as antimicrobial surface coatings2018In: Abstract of Papers of the American Chemical Society, ISSN 0065-7727, Vol. 255Article in journal (Other academic)
  • 34.
    Nyström, Lina
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Schmidtchen, Artur
    Lund University, Lund, Sweden; University of Copenhagen, Copenhagen, Denmark.
    Malmsten, Martin
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. University of Copenhagen, Copenhagen, Denmark.
    Peptide-Loaded Microgels as Antimicrobial and Anti-Inflammatory Surface Coatings2018In: Biomacromolecules, ISSN 1525-7797, E-ISSN 1526-4602, Vol. 19, no 8, p. 3456-3466Article in journal (Refereed)
    Abstract [en]

    Here we report on covalently immobilized poly(ethyl acrylate- co-methacrylic acid) microgels loaded with the host defense peptide KYE28 (KYEITTIHNLFRKLTHRLFRRNFGYTLR), which is derived from human heparin cofactor II, as well as its poly(ethylene glycol)-conjugated (PEGylated) version, KYE28PEG. Peptide loading and release, as well as the consequences of these processes on the microgel and peptide properties, were studied by in situ ellipsometry, confocal microscopy, zeta potential measurements, and circular dichroism spectroscopy. The results show that the microgel-peptide interactions are electrostatically dominated, thus promoted at higher microgel charge density, while PEGylation suppresses peptide binding. PEGylation also enhances the α-helix induction observed for KYE28 upon microgel incorporation. Additionally, peptide release is facilitated at physiological salt concentration, particularly so for KYE28PEG, which illustrates the importance of electrostatic interactions. In vitro studies on Escherichia coli show that the microgel-modified surfaces display potent antifouling properties in both the absence and presence of the incorporated peptide. While contact killing dominates at low ionic strength for the peptide-loaded microgels, released peptides also provide antimicrobial activity in bulk at a high ionic strength. Additionally, KYE28- and KYE28PEG-loaded microgels display anti-inflammatory effects on human monocytes. Taken together, these results not only show that surface-bound microgels offer an interesting approach for local drug delivery of host defense peptides but also illustrate the need to achieve high surface loads of peptides for efficient biological effects.

    The full text will be freely available from 2019-08-30 15:44
  • 35.
    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.

  • 36.
    Rasheed, Dalia M.
    et al.
    October 6 Univ, Fac Pharm, Pharmacognosy Dept, Cairo, Egypt..
    Porzel, Andrea
    Leibniz Inst Plant Biochem, Dept Bioorgan Chem, Weinberg 3, D-06120 Halle An Der Saale, Germany..
    Frolov, Andrei
    Leibniz Inst Plant Biochem, Dept Bioorgan Chem, Weinberg 3, D-06120 Halle An Der Saale, Germany..
    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..
    Wessjohann, Ludger A.
    Leibniz Inst Plant Biochem, Dept Bioorgan Chem, Weinberg 3, D-06120 Halle An Der Saale, Germany..
    Farag, Mohamed A.
    Cairo Univ, Coll Pharm, Pharmacognosy Dept, Cairo 11562, Egypt.;Amer Univ Cairo, Sch Sci & Engn, Dept Chem, New Cairo 11835, Egypt..
    Comparative analysis of Hibiscus sabdariffa (roselle) hot and cold extracts in respect to their potential for alpha-glucosidase inhibition2018In: Food Chemistry, ISSN 0308-8146, E-ISSN 1873-7072, Vol. 250, p. 236-244Article in journal (Refereed)
    Abstract [en]

    Roselle (Hibiscus sabdariffa) is a functional food with potential health benefits, consumed either as hot or cold beverage. To ensure quality control of its various products, accurate measurement of active metabolites is warranted. Herein, we propose a combination of ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS) and nuclear magnetic resonance (NMR) analytical platforms for the untargeted characterization of metabolites in two roselle cultivars, Aswan and Sudan-1. The analyses revealed 33 metabolites, including sugars, flavonoids, anthocyanins, phenolic and aliphatic organic acids. Their relative contents in cultivars were assessed via principle component analysis (PCA) and orthogonal projection to latent structures analysis (OPLS). Impact of the different extraction methods (decoction, infusion and maceration) was compared by quantitative H-1 NMR spectroscopy, revealing cold maceration to be optimal for preserving anthocyanins, whereas infusion was more suited for recovering organic acids. The metabolite pattern revealed by the different extraction methods was found in good correlation for their ability to inhibit alpha-glucosidase enzyme.

  • 37.
    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.

  • 38.
    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.

  • 39.
    Saeed, Aamer
    et al.
    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..
    Larik, Fayaz Ali
    Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan..
    El-Seedi, Hesham R.
    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 45320, Pakistan..
    Developments in the synthesis of the antiplatelet and antithrombotic drug (S)-clopidogrel2017In: Chirality, ISSN 0899-0042, E-ISSN 1520-636X, Vol. 29, no 11, p. 684-707Article, review/survey (Refereed)
    Abstract [en]

    S-(+)-Methyl 2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)acetate, also known as (S)-clopidogrel, is marketed under the trade names Plavix and Iscover. It is a potent thienopyridine-class of antithrombotic and antiplatelet drug (antiaggregant). Among the two available stereoisomers of clopidogrel, for pharmaceutical activities only the S-enantiomer is applicable, as no antithrombotic activity is observed in the R-enantiomer and causes political upheavals and social turmoil in animal experiments. Worldwide sales of Plavix amounted to $6.4 billion yearly, which ranks second. Attributed to the increased demand of (S)-clopidogrel drug, it provoked the synthetic community to devise facile synthetic approaches. This review aims to summarize the synthetic methods of (S)-clopidogrel drug reported in the literature. The present review discusses the pros and cons of each synthetic methodology, which would be beneficial to the scientific community for further developments in the synthetic methodologies for (S)-clopidogrel. In addition, the compilation approach of literature-reported synthetic strategies of (S)-clopidogrel in one platform is advantageous, supportive, and crucial for the synthetic community to elect the best synthetic methodology of (S)-clopidogrel and to create new synthesis ideas.

  • 40.
    Shcherbakova, A.
    et al.
    Friedrich Wilhelms Univ Bonn, Med Clin 3, UKB, Sigmund Freudstr 25, D-53127 Bonn, Germany.;Dept Forestry, Ploshchad Lenina 3, Yoshkar Ola 424000, Mari El Republi, Russia..
    Nyugen, L.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Friedrich Wilhelms Univ Bonn, Med Clin 3, UKB, Sigmund Freudstr 25, D-53127 Bonn, Germany..
    Koptina, A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Backlund, Anders
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Shurgin, A.
    Dept Forestry, Ploshchad Lenina 3, Yoshkar Ola 424000, Mari El Republi, Russia..
    Romanov, E.
    Dept Forestry, Ploshchad Lenina 3, Yoshkar Ola 424000, Mari El Republi, Russia..
    Ulrich-Merzenich, G.
    Friedrich Wilhelms Univ Bonn, Med Clin 3, UKB, Sigmund Freudstr 25, D-53127 Bonn, Germany..
    Screening of compounds of Evernia prunastri (L.) for their antiproliferative activity in glioblastoma cells2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 41.
    Slazak, Blazej
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Polish Acad Sci, W Szafer Inst Bot, Krakow, Poland.
    Kapusta, Malgorzata
    Univ Gdansk, Fac Biol, Dept Plant Cytol & Embryol, Gdansk, Poland.
    Strömstedt, Adam A.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Slomka, Aneta
    Jagiellonian Univ, Inst Bot, Dept Plant Cytol & Embryol, Gdansk, Poland.
    Krychowiak, Marta
    Univ Gdansk, Intercollegiate Fac Biotechnol, Lab Biol Act Cpds, Gdansk, Poland;Med Univ Gdansk, Gdansk, Poland.
    Shariatgorji, Mohammadreza
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences. Uppsala University, Science for Life Laboratory, SciLifeLab.
    Andrén, Per E.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences. Uppsala University, Science for Life Laboratory, SciLifeLab.
    Bohdanowicz, Jerzy
    Univ Gdansk, Fac Biol, Dept Plant Cytol & Embryol, Gdansk, Poland.
    Kuta, Elzbieta
    Jagiellonian Univ, Inst Bot, Dept Plant Cytol & Embryol, Gdansk, Poland.
    Göransson, Ulf
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    How Does the Sweet Violet (Viola odorata L.) Fight Pathogens and Pests - Cyclotides as a Comprehensive Plant Host Defense System2018In: Frontiers in Plant Science, ISSN 1664-462X, E-ISSN 1664-462X, Vol. 9, article id 1296Article in journal (Refereed)
    Abstract [en]

    Cyclotides are cyclic plant polypeptides of 27-37 amino acid residues. They have been extensively studied in bioengineering and drug development contexts. However, less is known about the relevance of cyclotides for the plants producing them. The anti-insect larvae effects of kB1 and antibacterial activity of cyO2 suggest that cyclotides are a part of plant host defense. The sweet violet (Viola odorata L.) produces a wide array of cyclotides, including kB1 (kalata B1) and cyO2 (cycloviolacin O2), with distinct presumed biological roles. Here, we evaluate V. odorata cyclotides' potency against plant pathogens and their mode of action using bioassays, liposome experiments and immunogold labeling for transmission electron microscopy (TEM). We explore the link between the biological activity and distribution in plant generative, vegetative tissues and seeds, depicted by immunohistochemistry and matrix assisted laser desorption ionization mass spectrometry imaging (MALDI-MSI). Cyclotides cyO2, cyO3, cyO13, and cyO19 are shown to have potent activity against model fungal plant pathogens (Fusarium oxysporum, F. graminearum, F. culmorum, Mycosphaerella fragariae, Botrytis cinerea) and fungi isolated from violets (Colletotrichum utrechtense and Alternaria alternata), with minimal inhibitory concentrations (MICs) ranging from 0.8 to 25 mu M. Inhibition of phytopathogenic bacteria - Pseudomonas syringae pv. syringae, Dickeya dadantii and Pectobacterium atrosepticum - is also observed with MIC = 25-100 mu M. A membrane-disrupting antifungal mode of action is shown. Finding cyO2 inside the fungal spore cells in TEM images may indicate that other, intracellular targets may be involved in the mechanism of toxicity. Fungi can not break down cyclotides in the course of days. varv A (kalata S) and kB1 show little potency against pathogenic fungi when compared with the tested cycloviolacins. cyO2, cyO3, cyO19 and kB1 are differentially distributed and found in tissues vulnerable to pathogen (epidermis, rizodermis, vascular bundles, protodermis, procambium, ovary walls, outer integuments) and pest ( ground tissues of leaf and petiole) attacks, respectively, indicating a link between the cyclotides' sites of accumulation and biological role. Cyclotides emerge as a comprehensive defense system in V. odorata, in which different types of peptides have specific targets that determine their distribution in plant tissues.

  • 42.
    Strömstedt, Adam A.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Vikeved, Elisabet
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Cárdenas, Paco
    Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Organismal Biology, Systematic Biology. Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Alsmark, UCM
    Uppsala University.
    Chen, Yung Hsuan
    National Museum of Marine Biology and Aquarium, .
    Backlund, Anders
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Aaptamines from Haliclona and bromopyrroles from Agelas — marine sponge alkaloids with distinct modes of action against bacteria and protozoaManuscript (preprint) (Other academic)
  • 43.
    Vacelet, Jean
    et al.
    IMBE, CNRS, Aix Marseille Univ, Univ Avignon, IRD, Station Marine d’Endoume, Marseille, France.
    Cárdenas, Paco
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. IMBE, CNRS, Aix Marseille Univ, Univ Avignon, IRD, Station Marine d’Endoume, Marseille, France.
    When is an aster not an aster? A new deep-sea Discorhabdella (Demospongiae, Poecilosclerida) with asters, from the Mozambique Channel2018In: Zootaxa, ISSN 1175-5326, E-ISSN 1175-5334, Vol. 4466, no 1, p. 197-204Article in journal (Refereed)
    Abstract [en]

    Discorhabdella pseudaster n. sp. is an incrusting sponge from the upper bathyal zone of the 'Banc du Geyser', north of Madagascar, Mozambique Channel. This new species is described only from a single specimen but it is remarkable by the presence of spicules similar to euasters, a type of microsclere unknown in Poecilosclerida. These spicules are in fact a new example of homoplasy, being derivatives of the typical Discorhabdella pseudoastrose acanthostyles, which are here reduced to the aster-like tyles. The isochelae with a large lamella on the shaft are also quite unique in Poeciloclerida.

  • 44.
    Vikeved, Elisabet
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Alsmark, UCM
    Uppsala University.
    Sköld, Christian
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
    Prediction of anti-leishmanial drug targets using metabolite-based target fishingManuscript (preprint) (Other academic)
  • 45.
    Vikeved, Elisabet
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Buonfiglio, R.
    AstraZeneca R&D Gothenburg, Chem Innovat Ctr, Discovery Sci, SE-43183 Molndal, Sweden..
    Kogej, T.
    AstraZeneca R&D Gothenburg, Chem Innovat Ctr, Discovery Sci, SE-43183 Molndal, Sweden..
    Backlund, Anders
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Mapping metabolic pathways in chemical property space paves the way for new leishmanicidals2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 46.
    Vikeved, Elisabet
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Sköld, Christian
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
    Alsmark, UCM
    Uppsala University.
    Multi-targeting the folate pathway is a promising strategy against Leishmania tropicaManuscript (preprint) (Other academic)
  • 47.
    Xu, Jing-Hao
    et al.
    Natl Dong Hwa Univ, Grad Inst Marine Biol, Pingtung 94450, Taiwan;Natl Museum Marine Biol & Aquarium, Planning & Res Div, Pingtung 94450, Taiwan.
    Lai, Kuei-Hung
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. Natl Museum Marine Biol & Aquarium, Planning & Res Div, Pingtung 94450, Taiwan.
    Su, Yin-Di
    Natl Museum Marine Biol & Aquarium, Planning & Res Div, Pingtung 94450, Taiwan;Ind Technol Res Inst, Greenhouse Syst Technol Ctr, Cent Reg Campus, Nantou 54041, Taiwan.
    Chang, Yu-Chia
    Natl Museum Marine Biol & Aquarium, Planning & Res Div, Pingtung 94450, Taiwan;Ind Technol Res Inst, Greenhouse Syst Technol Ctr, Cent Reg Campus, Nantou 54041, Taiwan;Natl Sun Yat Sen Univ, Dept Marine Biotechnol & Resources, Kaohsiung 80424, Taiwan.
    Peng, Bo-Rong
    Natl Museum Marine Biol & Aquarium, Planning & Res Div, Pingtung 94450, Taiwan;Natl Sun Yat Sen Univ, Doctoral Degree Program Marine Biotechnol, Kaohsiung 80424, Taiwan;Acad Sinica, Doctoral Degree Program Marine Biotechnol, Taipei 11529, Taiwan.
    Backlund, Anders
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Wen, Zhi-Hong
    Natl Sun Yat Sen Univ, Dept Marine Biotechnol & Resources, Kaohsiung 80424, Taiwan.
    Sung, Ping-Jyun
    Natl Dong Hwa Univ, Grad Inst Marine Biol, Pingtung 94450, Taiwan;Natl Museum Marine Biol & Aquarium, Planning & Res Div, Pingtung 94450, Taiwan;Natl Sun Yat Sen Univ, Dept Marine Biotechnol & Resources, Kaohsiung 80424, Taiwan;China Med Univ Hosp, Chinese Med Res & Dev Ctr, Taichung 40447, Taiwan;Kaohsiung Med Univ, Grad Inst Nat Prod, Kaohsiung 80708, Taiwan.
    Briaviolides K-N, New Briarane-Type Diterpenoids from Cultured Octocoral Briareum violaceum2018In: Marine Drugs, ISSN 1660-3397, E-ISSN 1660-3397, Vol. 16, no 3, article id 75Article in journal (Refereed)
    Abstract [en]

    Four new briarane diterpenoids, briaviolides K-N (1-4), have been obtained from the cultured-type octocoral Briareum violaceum. Using a spectroscopic approach, the structures of briaranes 1-4 were identified. This study employed an in vitro model of lipopolysaccharide (LPS)-induced inflammation in the murine macrophage RAW264.7 cell line, and found that among the four briaranes, briarane 2 possessed anti-inflammatory activity against inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein expressions in cells. In addition, principal component analysis using the chemical global positioning system (ChemGPS) for natural products (ChemGPS-NP) was employed in order to analyze the structure-activity relationship (SAR), and the results indicated that the ring conformation of the compound has a leading role in suppressing the expressions of pro-inflammatory iNOS and COX-2 proteins in macrophages.

  • 48.
    Yang, L.
    et al.
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi. China Pharmaceut Univ, Dept Complex Prescript TCM, Jiangsu Prov Key Lab TCM Evaluat & Translat Res, Nanjing, Jiangsu, Peoples R China..
    Henz, Astrid
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Backlund, Anders
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Predicting inhibitors of HSP27 phosphorylation using ChemGPS-NP2016In: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 82Article in journal (Other academic)
  • 49. Zahran, Moustafa
    et al.