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Isolation, Structure, and HIV‐1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum
Author(s) -
Singh Sheo B.,
Zink Deborah L.,
Guan Ziqiang,
Collado Javier,
Pelaez Fernando,
Felock Peter J.,
Hazuda Daria J.
Publication year - 2003
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.200390281
Subject(s) - penicillium chrysogenum , chemistry , integrase , integrase inhibitor , isolation (microbiology) , stereochemistry , penicillium , inhibitory postsynaptic potential , human immunodeficiency virus (hiv) , microbiology and biotechnology , biochemistry , virology , dna , food science , viral load , antiretroviral therapy , biology , neuroscience
HIV‐1 Integrase is a critical enzyme for replication of HIV, and its inhibition is one of the most promising new drug targets for anti‐retroviral therapy with potentially significant advantages over existing therapies. Xanthoviridicatins E ( 1 ) and F ( 2 ) are two novel polyketide natural products that were isolated from a fermentation broth of an endophytic strain of Penicillium chrysogenum isolated from the living leaves collected in Peru. These compounds are new members of the unsymmetrical xanthoviridicatin family represented by the broader xanthomegnin family. Xanthoviridicatins E and F inhibited the cleavage reaction of HIV‐1 integrase with an IC 50 of 6 and 5 μ M , respectively. The bioassay‐directed isolation, structure elucidation, and HIV‐1 inhibitory activity of these compounds are described.