New antimalarial dimeric diketopiperazines, piperasagamines A and B, produced by a deep-sea-derived fungus
Karin Hamada1, Yoshihiro Watanabe1,2, Hiroki Kojima1,2
1Graduate School of Infection Control Sciences, Kitasato University, Minato-ku, Tokyo, Japan.
Abstract:
Two new dimeric diketopiperazines, piperasagamines A (1) and B (2), were discovered from the cultured material of a deep-sea-derived Aspergillus sp. FKJ-0404 strain. The planar structures of 1 and 2 were elucidated by spectroscopic analysis as dimeric diketopiperazines featuring an α, β-dehydroproline moiety. The absolute configurations of 1 and 2 were determined by advanced Marfey's analysis combined with the analysis of their reduced derivatives. Among them, 2 showed moderate antimalarial activity with an IC50 value of 9.9 µg ml-1 against Plasmodium falciparum FCR3 strain.
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