dc.contributor.author | Lauinger, Ina L. | |
dc.contributor.author | Vivas, Livia | |
dc.contributor.author | Perozzo, Remo | |
dc.contributor.author | Stairiker, Christopher | |
dc.contributor.author | Tarun, Alice | |
dc.contributor.author | Zloh, Mire | |
dc.contributor.author | Zhang, Xujie | |
dc.contributor.author | Xu, Hua | |
dc.contributor.author | Tonge, Peter J. | |
dc.contributor.author | Franzblau, Scott G. | |
dc.contributor.author | Pham, Duc-Hung | |
dc.contributor.author | Esguerra, Camila V. | |
dc.contributor.author | Crawford, Alexander D. | |
dc.contributor.author | Maes, Louis | |
dc.contributor.author | Tasdemir, Deniz | |
dc.date.accessioned | 2018-09-20T16:14:05Z | |
dc.date.available | 2018-09-20T16:14:05Z | |
dc.date.issued | 2013-06-28 | |
dc.identifier.citation | Lauinger, Ina L. Vivas, Livia; Perozzo, Remo; Stairiker, Christopher; Tarun, Alice; Zloh, Mire; Zhang, Xujie; Xu, Hua; Tonge, Peter J.; Franzblau, Scott G.; Pham, Duc-Hung; Esguerra, Camila V.; Crawford, Alexander D.; Maes, Louis; Tasdemir, Deniz (2013). Potential of lichen secondary metabolites againstplasmodiumliver stage parasites with fas-ii as the potential target. Journal of Natural Products 76 (6), 1064-1070 | |
dc.identifier.issn | 0163-3864,1520-6025 | |
dc.identifier.uri | http://hdl.handle.net/10379/12389 | |
dc.description.abstract | Chemicals 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 mu M, BS IC50 value 47.3 mu M). The compounds 1 - 3 inhibited one Or more enzymes (Pf FabI, 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., | |
dc.publisher | American Chemical Society (ACS) | |
dc.relation.ispartof | Journal of Natural Products | |
dc.rights | Attribution-NonCommercial-NoDerivs 3.0 Ireland | |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/3.0/ie/ | |
dc.subject | fatty-acid biosynthesis | |
dc.subject | carrier protein reductase | |
dc.subject | enoyl-acp reductase | |
dc.subject | usnic acid | |
dc.subject | in-vitro | |
dc.subject | antimycobacterial activity | |
dc.subject | staphylococcus-aureus | |
dc.subject | antimalarial activity | |
dc.subject | drug discovery | |
dc.subject | falciparum | |
dc.title | Potential of lichen secondary metabolites againstplasmodiumliver stage parasites with fas-ii as the potential target | |
dc.type | Article | |
dc.identifier.doi | 10.1021/np400083k | |
dc.local.publishedsource | http://europepmc.org/articles/pmc4119598?pdf=render | |
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