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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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Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, and West Point, Pennsylvania 19486
Cite this: J. Nat. Prod. 2003, 66, 4, 551–553
Publication Date (Web):March 21, 2003
Copyright © 2003 American Chemical Society and American Society of Pharmacognosy

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    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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    A copy of 1H and 13C NMR spectra of 1, Table 1 containing full 1H and 13C NMR assignments including HMBC data, and Figure 1 showing a ChemDraw 3D model and NOESY data. This material is available free of charge via the Internet at

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