| Literature DB >> 21696970 |
Zhenyu Lu1, Yuanqing Ding, Xing-Cong Li, Daignon R Djigbenou, Brian T Grimberg, Daneel Ferreira, Chris M Ireland, Ryan M Van Wagoner.
Abstract
A new fascaplysin analogue, 3-bromohomofascaplysin A (1), along with two known analogues, homofascaplysin A (2) and fascaplysin (3), were isolated from a Fijian Didemnum sp. ascidian. The absolute configurations of 3-bromohomofascaplysin A (1) and homofascaplysin A (2) were determined via experimental and theoretically calculated ECD spectra. The differential activities of 1-3 against different blood-borne life stages of the malaria pathogen Plasmodium falciparum were assessed. Homofascaplysin A (2) displayed an IC(50) of 0.55±0.11 nM against ring stage parasites and 105±38 nM against all live parasites. Given the stronger resistance of ring stage parasites against most current antimalarials relative to the other blood stages, homofascaplysin A (2) represents a promising agent for treatment of drug resistant malaria.Entities:
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Year: 2011 PMID： 21696970 PMCID： PMC3205246 DOI： 10.1016/j.bmc.2011.05.046
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641