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Isolation, Structure, and HIV-1 Integrase Inhibitory Activity of Cytosporic Acid, a Fungal Metabolite Produced by a Cytospora sp.

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posted on 21.03.2003, 00:00 by Hiranthi Jayasuriya, Ziqiang Guan, Jon D. Polishook, Anne W. Dombrowski, Peter J. Felock, Daria J. Hazuda, Sheo B. Singh
HIV-1 integrase is a critical enzyme for replication of HIV, and its inhibition has the potential to lead to an anti-retroviral therapy that has advantages over existing therapies. Cytosporic acid (1) is a polyketide-derived novel natural product that was isolated from a fermentation broth of the filamentous fungus Cytospora sp. collected from Puerto Rico. It inhibited strand transfer reaction of HIV-1 integrase with an IC50 of 20 μM. The isolation, structure elucidation, relative stereochemistry, and activity of 1 are described.

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