uu.seUppsala University Publications
Change search
Refine search result
12 1 - 50 of 61
CiteExportLink to result list
Permanent link
Cite
Citation style
  • apa
  • ieee
  • modern-language-association
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf
Rows per page
  • 5
  • 10
  • 20
  • 50
  • 100
  • 250
Sort
  • Standard (Relevance)
  • Author A-Ö
  • Author Ö-A
  • Title A-Ö
  • Title Ö-A
  • Publication type A-Ö
  • Publication type Ö-A
  • Issued (Oldest first)
  • Issued (Newest first)
  • Created (Oldest first)
  • Created (Newest first)
  • Last updated (Oldest first)
  • Last updated (Newest first)
  • Disputation date (earliest first)
  • Disputation date (latest first)
  • Standard (Relevance)
  • Author A-Ö
  • Author Ö-A
  • Title A-Ö
  • Title Ö-A
  • Publication type A-Ö
  • Publication type Ö-A
  • Issued (Oldest first)
  • Issued (Newest first)
  • Created (Oldest first)
  • Created (Newest first)
  • Last updated (Oldest first)
  • Last updated (Newest first)
  • Disputation date (earliest first)
  • Disputation date (latest first)
Select
The maximal number of hits you can export is 250. When you want to export more records please use the Create feeds function.
  • 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.
    Adl, Sina M.
    et al.
    Univ Saskatchewan, Dept Soil Sci, Coll Agr & Bioresources, 51 Campus Dr, Saskatoon, SK S7N 5A8, Canada.
    Bass, David
    Nat Hist Museum, Dept Life Sci, Cromwell Rd, London SW7 5BD, England;CEFAS, Barrack Rd, Weymouth DT4 8UB, Dorset, England.
    Lane, Christopher E.
    Univ Rhode Isl, Dept Biol Sci, Kingston, RI 02881 USA.
    Lukes, Julius
    Czech Acad Sci, Biol Ctr, Inst Parasitol, Ceske Budejovice 37005, Czech Republic;Univ South Bohemia, Fac Sci, Ceske Budejovice 37005, Czech Republic.
    Schoch, Conrad L.
    Natl Inst Biotechnol Informat, Natl Lib Med, NIH, Bethesda, MD 20892 USA.
    Smirnov, Alexey
    St Petersburg State Univ, Fac Biol, Dept Invertebrate Zool, St Petersburg 199034, Russia.
    Agatha, Sabine
    Univ Salzburg, Dept Biosci, Hellbrunnerstr 34, A-5020 Salzburg, Austria.
    Berney, Cedric
    CNRS, UMR 7144 AD2M, Grp Evolut Protistes & Ecosyst Pelag, Stn Biol Roscoff, Pl Georges Teissier, F-29680 Roscoff, France.
    Brown, Matthew W.
    Mississippi State Univ, Dept Biol Sci, Starkville, MS 39762 USA;Mississippi State Univ, Inst Genom Biocomp & Biotechnol, Starkville, MS 39762 USA.
    Burki, Fabien
    Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Organismal Biology, Systematic Biology. Uppsala University, Science for Life Laboratory, SciLifeLab.
    Cárdenas, Paco
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Cepicka, Ivan
    Charles Univ Prague, Dept Zool, Fac Sci, Vinicna 7, CR-12844 Prague, Czech Republic.
    Chistyakova, Lyudmila
    St Petersburg State Univ, Core Facil Ctr Culture Collect Microorganisms, St Petersburg 198504, Russia.
    del Campo, Javier
    CSIC, Inst Ciencies Mar, Passeig Maritim Barceloneta 37-49, E-08003 Barcelona, Catalonia, Spain.
    Dunthorn, Micah
    Univ Kaiserslautern, Dept Ecol, Erwin Schroedinger St, D-67663 Kaiserslautern, Germany;Univ Duisburg Essen, Dept Eukaryot Microbiol, Univ Str 5, D-45141 Essen, Germany.
    Edvardsen, Bente
    Univ Oslo, Dept Biosci, POB 1066 Blindern, N-0316 Oslo, Norway.
    Eglit, Yana
    Dalhousie Univ, Dept Biol, Halifax B3H 4R2, NS, Canada.
    Guillou, Laure
    Univ Paris 06, Sorbonne Univ, Paris 6, CNRS,UMR 7144 AD2M,Stn Biol Roscoff, Pl Georges Teissier,,CS90074, F-29688 Roscoff, France.
    Hampl, Vladimir
    Charles Univ Prague, Dept Parasitol, Fac Sci, BIOCEV, Prumyslov 595, Vestec 25242, Czech Republic.
    Heiss, Aaron A.
    Amer Museum Nat Hist, Dept Invertebrate Zool, New York, NY 10024 USA.
    Hoppenrath, Mona
    DZMB German Ctr Marine Biodivers Res, D-26382 Wilhelmshaven, Germany.
    James, Timothy Y.
    Univ Michigan, Dept Ecol & Evolutionary Biol, Ann Arbor, MI 48109 USA.
    Karnkowska, Anna
    Univ Warsaw, Dept Mol Phylogenet & Evolut, PL-02089 Warsaw, Poland.
    Karpov, Sergey
    St Petersburg State Univ, Fac Biol, Dept Invertebrate Zool, St Petersburg 199034, Russia;RAS, Lab Parasit Worms & Protistol, Zool Inst, St Petersburg 199034, Russia.
    Kim, Eunsoo
    Amer Museum Nat Hist, Dept Invertebrate Zool, New York, NY 10024 USA.
    Kolisko, Martin
    Czech Acad Sci, Biol Ctr, Inst Parasitol, Ceske Budejovice 37005, Czech Republic.
    Kudryavtsev, Alexander
    St Petersburg State Univ, Fac Biol, Dept Invertebrate Zool, St Petersburg 199034, Russia;RAS, Lab Parasit Worms & Protistol, Zool Inst, St Petersburg 199034, Russia.
    Lahr, Daniel J. G.
    Univ Sao Paulo, Dept Zool, Inst Biosci, Matao Travessa 14 Cidade Univ, BR-05508090 Sao Paulo, SP, Brazil.
    Lara, Enrique
    Univ Neuchatel, Lab Soil Biodivers, Rue Emile Argand 11, CH-2000 Neuchatel, Switzerland;CSIC, Real Jardim Bot,Plaza Murillo 2, E-28014 Madrid, Spain.
    Le Gall, Line
    Sorbonne Univ, Museum Natl Hist Nat, Inst Systemat Evolut Biodiversit, 57 Rue Cuvier,CP 39, F-75005 Paris, France.
    Lynn, Denis H.
    Univ Guelph, Dept Integrat Biol, Summerlee Sci Complex, Guelph, ON N1G 2W1, Canada;Univ British Columbia, Dept Zool, 4200-6270 Univ Blvd, Vancouver, BC V6T 1Z4, Canada.
    Mann, David G.
    Royal Bot Garden, Edinburgh EH3 5LR, Midlothian, Scotland;Inst Agrifood Res & Technol, C Poble Nou Km 5-5, E-43540 San Carlos de la Rapita, Spain.
    Massana, Ramon
    CSIC, Inst Ciencies Mar, Passeig Maritim Barceloneta 37-49, E-08003 Barcelona, Catalonia, Spain.
    Mitchell, Edward A. D.
    Univ Neuchatel, Lab Soil Biodivers, Rue Emile Argand 11, CH-2000 Neuchatel, Switzerland;Jardin Bot Neuchatel,Chemin Perthuis du Salut 58, CH-2000 Neuchatel, Switzerland.
    Morrow, Christine
    Natl Museums Northern Ireland, Dept Nat Sci, 153 Bangor Rd, Holywood BT18 0EU, England.
    Park, Jong Soo
    Kyungpook Natl Univ, Sch Earth Syst Sci, Dept Oceanog, Daegu, South Korea;Kyungpook Natl Univ, Sch Earth Syst Sci, Kyungpook Inst Oceanog, Daegu, South Korea.
    Pawlowski, Jan W.
    Univ Geneva, Dept Genet & Evolut, CH-1211 Geneva 4, Switzerland.
    Powell, Martha J.
    Univ Alabama, Dept Biol Sci, Tuscaloosa, AL 35487 USA.
    Richter, Daniel J.
    Univ Pompeu Fabra, CSIC, Inst Biol Evolut, Passeig Maritim Barceloneta 37-49, Barcelona 08003, Spain.
    Rueckert, Sonja
    Edinburgh Napier Univ, Sch Appl Sci, Edinburgh EH11 4BN, Midlothian, Scotland.
    Shadwick, Lora
    Univ Arkansas, Dept Biol Sci, Fayetteville, AR 72701 USA.
    Shimano, Satoshi
    Hosei Univ, Sci Res Ctr, Chiyoda Ku, 2-17-1 Fujimi, Tokyo, Japan.
    Spiegel, Frederick W.
    Univ Arkansas, Dept Biol Sci, Fayetteville, AR 72701 USA.
    Torruella, Guifre
    Univ Paris XI, Lab Evolut & Systemat, F-91405 Orsay, France.
    Youssef, Noha
    Oklahoma State Univ, Dept Microbiol & Mol Genet, Stillwater, OK 74074 USA.
    Zlatogursky, Vasily V.
    Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Organismal Biology, Systematic Biology. St Petersburg State Univ, Fac Biol, Dept Invertebrate Zool, St Petersburg 199034, Russia.
    Zhang, Qianqian
    Chinese Acad Sci, Yantai Inst Coastal Zone Res, Yantai 264003, Peoples R China.
    Revisions to the Classification, Nomenclature, and Diversity of Eukaryotes2019In: Journal of Eukaryotic Microbiology, ISSN 1066-5234, E-ISSN 1550-7408, Vol. 66, no 1, p. 4-119Article in journal (Refereed)
    Abstract [en]

    This revision of the classification of eukaryotes follows that of Adl et al., 2012 [J. Euk. Microbiol. 59(5)] and retains an emphasis on protists. Changes since have improved the resolution of many nodes in phylogenetic analyses. For some clades even families are being clearly resolved. As we had predicted, environmental sampling in the intervening years has massively increased the genetic information at hand. Consequently, we have discovered novel clades, exciting new genera and uncovered a massive species level diversity beyond the morphological species descriptions. Several clades known from environmental samples only have now found their home. Sampling soils, deeper marine waters and the deep sea will continue to fill us with surprises. The main changes in this revision are the confirmation that eukaryotes form at least two domains, the loss of monophyly in the Excavata, robust support for the Haptista and Cryptista. We provide suggested primer sets for DNA sequences from environmental samples that are effective for each clade. We have provided a guide to trophic functional guilds in an appendix, to facilitate the interpretation of environmental samples, and a standardized taxonomic guide for East Asian users.

  • 5.
    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)
  • 6.
    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)
  • 7.
    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)
  • 8.
    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.

  • 9.
    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)
  • 10.
    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)
  • 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.
    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 specimens2019In: Marine Biodiversity, ISSN 1867-1616, E-ISSN 1867-1624, Vol. 49, no 1, p. 163-174Article 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.

  • 14.
    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.

  • 15.
    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.

  • 16.
    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.

  • 17.
    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.

  • 18.
    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.

  • 19.
    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.

  • 20.
    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)
  • 21.
    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.

  • 22.
    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.

  • 23.
    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)
  • 24.
    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.

  • 25.
    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.

  • 26.
    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)
  • 27.
    Göransson, Ulf
    et al.
    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.
    Strand, Malin
    Swedish Univ Agr Sci, Swedish Species Informat Ctr, Uppsala, Sweden.
    Andersson, Hakan S.
    Linnaeus Univ, Ctr Biomat Chem, Dept Chem & Biomed Sci, Kalmar, Sweden.
    The Toxins of Nemertean Worms2019In: Toxins, ISSN 2072-6651, E-ISSN 2072-6651, Vol. 11, no 2, article id 120Article, review/survey (Refereed)
    Abstract [en]

    Most ribbon worms (phylum: Nemertea) are found in marine environments, where they act as predators and scavengers. They are characterized by an eversible proboscis that is used to hunt for prey and thick mucus covering their skin. Both proboscis and epidermal mucus mediate toxicity to predators and preys. Research into the chemical nature of the substances that render toxicity has not been extensive, but it has nevertheless led to the identification of several compounds of potential medicinal use or for application in biotechnology. This review provides a complete account of the current status of research into nemertean toxins.

  • 28.
    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)
  • 29.
    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)
  • 30.
    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.

  • 31.
    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.

  • 32.
    Kelly, Michelle
    et al.
    Natl Inst Water & Atmospher Res, Coasts & Oceans Natl Ctr, POB 109-695, Auckland, New Zealand.
    Cardenas, Paco
    Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Farmakognosi.
    Rush, Nicola
    Natl Inst Water & Atmospher Res, Coasts & Oceans Natl Ctr, POB 109-695, Auckland, New Zealand.
    Sim-Smith, Carina
    Natl Inst Water & Atmospher Res, Coasts & Oceans Natl Ctr, POB 109-695, Auckland, New Zealand.
    Macpherson, Diana
    Natl Inst Water & Atmospher Res, Coasts & Oceans Natl Ctr, Private Bag 14901, Wellington, New Zealand.
    Page, Mike
    Natl Inst Water & Atmospher Res, Coasts & Oceans Natl Ctr, POB 893, Nelson, New Zealand.
    Bell, Lori J.
    Coral Reef Res Fdn, Box 1765, Koror 96940, Palau.
    Molecular study supports the position of the New Zealand endemic genus Lamellomorpha in the family Vulcanellidae (Porifera, Demospongiae, Tetractinellida), with the description of three new species2019In: European journal of taxonomy, ISSN 2118-9773, Vol. 506, p. 1-25Article in journal (Refereed)
    Abstract [en]

    Due to the possession of huge contort strongyles, and a lack of triaenes in an otherwise 'astrophorine' spicule complement, the phylogenetic position of the endemic, monospecific New Zealand sponge genus, Lamellomorpha Bergquist, 1968, has remained enigmatic. The genus was established within Jaspidae de Laubenfels, 1968 (in the abandoned order Epipolasida Sollas, 1888), but it was not until 2002 that the genus was transferred formally to Astrophorina Sollas, 1887, albeit incertae sedis, by Hooper & Maldonado (2002). In this study, we recognise specimens of Lamellomorpha from the Subantarctic New Zealand region and Chatham Rise, considered by Bergquist to be conspecific with the type species, L. strongylata Bergquist, 1968, first described from the Three Kings-Spirits Bay region of Northland, as the new species, L. australis Kelly & Cardenas sp. nov. These two species of Lamellomorpha have differences in external morphology and colour, skeletal architecture and spicules, natural products, geographical distribution, and depth ranges. Sequencing of the COI Folmer barcode/mini-barcode and of 28S (C1-C2 domains) of these two species suggests phylogenetic affinities of Lamellomorpha with the tetractinellid suborder Astrophorina and the family Vulcanellidae Cardenas et al., 2011. Two Subantarctic New Zealand species of the vulcanellid genus Poecillastra Sollas, 1888, P. ducitriaena Kelly & Cardenas sp. nov. and P. macquariensis Kelly & Cardenas sp. nov., provide further support for the close relationship of Lamellomorpha and Poecillastra.

  • 33.
    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)
  • 34.
    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).

  • 35.
    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.

  • 36.
    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)
  • 37.
    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.

  • 38.
    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.

  • 39.
    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)
  • 40.
    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.

  • 41.
    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 peptides2018In: Biomacromolecules, ISSN 1525-7797, E-ISSN 1526-4602, Vol. 19, no 12, p. 4691-4702Article in journal (Refereed)
    Abstract [en]

    Herein, we report on the formation of cross-linked antimicrobial peptide-loaded microgel multilayers. Poly(ethyl acrylate- co-methacrylic acid) microgels were synthesized and functionalized with biotin to enable the formation of microgel multilayers cross-linked with avidin. Microgel functionalization and avidin cross-linking were verified with infrared spectroscopy, dynamic light scattering, and z-potential measurements, while multilayer formation (up to four layers) was studied with null ellipsometry and quartz crystal microbalance with dissipation (QCM-D). Incorporation of the antimicrobial peptide KYE28 (KYEITTIHNLFRKLTHRLFRRNFGYTLR) into the microgel multilayers was achieved either in one shot after multilayer formation or through addition after each microgel layer deposition. The latter was found to strongly promote peptide incorporation. Further, antimicrobial properties of the peptide-loaded microgel multilayers against Escherichia coli were investigated and compared to those of a peptide-loaded microgel monolayer. Results showed a more pronounced suppression in bacterial viability in suspension for the microgel multilayers. Correspondingly, LIVE/DEAD staining showed promoted disruption of adhered bacteria for the KYE28-loaded multilayers. Taken together, cross-linked microgel multilayers thus show promise as high load surface coatings for antimicrobial peptides.

  • 42.
    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)
  • 43.
    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