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  • Title: In vitro and in vivo antimalarial activity of puberulic acid and its new analogs, viticolins A-C, produced by Penicillium sp. FKI-4410.
    Author: Iwatsuki M, Takada S, Mori M, Ishiyama A, Namatame M, Nishihara-Tsukashima A, Nonaka K, Masuma R, Otoguro K, Shiomi K, Omura S.
    Journal: J Antibiot (Tokyo); 2011 Feb; 64(2):183-8. PubMed ID: 21063422.
    Abstract:
    In the course of screening for antimalarial agents, five tropolone compounds were isolated from the culture broth of Penicillium sp. FKI-4410. Two were known compounds, puberulic acid and stipitatic acid. Three were new analogs of puberulic acid, designated viticolins A-C. Among them, puberulic acid exhibited potent antimalarial inhibition, with IC(50) values of 0.01 μg ml(-1) against chloroquine-sensitive and -resistant Plasmodium falciparum strains in vitro. Furthermore, puberulic acid showed weak cytotoxicity against human MRC-5 cells, with an IC(50) value of 57.2 μg ml(-1). The compound also demonstrated a therapeutic effect in vivo, which compared well against the currently used antimalarial drugs, and thus shows promise as a leading candidate for development into a new antimalarial compound.
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