3-bromohomofascaplysin A, a fascaplysin analogue from a Fijian Didemnum sp. ascidian |
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Authors: | Lu Zhenyu Ding Yuanqing Li Xing-Cong Djigbenou Daignon R Grimberg Brian T Ferreira Daneel Ireland Chris M Van Wagoner Ryan M |
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Institution: | Department of Medicinal Chemistry, University of Utah, Salt Lake City, UT 84112, USA. |
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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. |
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