Show simple item record

dc.contributor.authorLauinger, Ina L
dc.contributor.authorVivas, Livia
dc.contributor.authorPerozzo, Remo
dc.contributor.authorStairiker, Christopher
dc.contributor.authorTarun, Alice
dc.contributor.authorZloh, Mire
dc.contributor.authorZhang, Xujie
dc.contributor.authorXu, Hua
dc.contributor.authorTonge, Peter J.
dc.contributor.authorFranzblau, Scott G.
dc.contributor.authorPham, Duc-Hung
dc.contributor.authorEsguerra, Camila V.
dc.contributor.authorCrawford, Alexander D.
dc.contributor.authorMaes, Louis
dc.contributor.authorTasdemir, Deniz
dc.date.accessioned2013-07-25T14:02:41Z
dc.date.available2013-07-25T14:02:41Z
dc.date.issued2013-06-28
dc.identifier.citationLauinger , I L , Vivas , L , Perozzo , R , Stairiker , C , Tarun , A , Zloh , M , Zhang , X , Xu , H , Tonge , P J , Franzblau , S G , Pham , D-H , Esguerra , C V , Crawford , A D , Maes , L & Tasdemir , D 2013 , ' Potential of Lichen Secondary Metabolites against Plasmodium Liver Stage Parasites with FAS-II as the Potential Target ' , Journal of Natural Products , vol. 76 , no. 6 , pp. 1064-70 . https://doi.org/10.1021/np400083k
dc.identifier.issn1520-6025
dc.identifier.otherPURE: 2092512
dc.identifier.otherPURE UUID: 3300d058-2b95-4eaa-853c-82857222eaa2
dc.identifier.otherPubMed: 23806111
dc.identifier.otherScopus: 84879641321
dc.identifier.urihttp://hdl.handle.net/2299/11193
dc.description.abstractChemicals targeting the liver stage (LS) of the malaria parasite are useful for causal prophylaxis of malaria. In this study, four lichen metabolites, evernic acid (1), vulpic acid (2), psoromic acid (3), and (+)-usnic acid (4), were evaluated against LS parasites of Plasmodium berghei. Inhibition of P. falciparum blood stage (BS) parasites was also assessed to determine stage specificity. Compound 4 displayed the highest LS activity and stage specificity (LS IC50 value 2.3 μM, BS IC50 value 47.3 μM). The compounds 1-3 inhibited one or more enzymes (PfFabI, PfFabG, and PfFabZ) from the plasmodial fatty acid biosynthesis (FAS-II) pathway, a potential drug target for LS activity. To determine species specificity and to clarify the mechanism of reported antibacterial effects, 1-4 were also evaluated against FabI homologues and whole cells of various pathogens (S. aureus, E. coli, M. tuberculosis). Molecular modeling studies suggest that lichen acids act indirectly via binding to allosteric sites on the protein surface of the FAS-II enzymes. Potential toxicity of compounds was assessed in human hepatocyte and cancer cells (in vitro) as well as in a zebrafish model (in vivo). This study indicates the therapeutic and prophylactic potential of lichen metabolites as antibacterial and antiplasmodial agents.en
dc.format.extent7
dc.language.isoeng
dc.relation.ispartofJournal of Natural Products
dc.titlePotential of Lichen Secondary Metabolites against Plasmodium Liver Stage Parasites with FAS-II as the Potential Targeten
dc.contributor.institutionDepartment of Pharmacy
dc.contributor.institutionMedicinal and Analytical Chemistry
dc.contributor.institutionSchool of Life and Medical Sciences
dc.contributor.institutionHealth & Human Sciences Research Institute
dc.description.statusPeer reviewed
dc.relation.schoolSchool of Life and Medical Sciences
dcterms.dateAccepted2013-06-28
rioxxterms.versionofrecordhttps://doi.org/10.1021/np400083k
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record