Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp.

Journal Article (Journal Article)

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 IC(50) of 20 microM. The isolation, structure elucidation, relative stereochemistry, and activity of 1 are described.

Full Text

Duke Authors

Cited Authors

  • Jayasuriya, H; Guan, Z; Polishook, JD; Dombrowski, AW; Felock, PJ; Hazuda, DJ; Singh, SB

Published Date

  • April 2003

Published In

Volume / Issue

  • 66 / 4

Start / End Page

  • 551 - 553

PubMed ID

  • 12713414

International Standard Serial Number (ISSN)

  • 0163-3864

Digital Object Identifier (DOI)

  • 10.1021/np020533g


  • eng

Conference Location

  • United States