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Title: DNA topoisomerase IIα inhibitory and anti-HIV-1 flavones from leaves and twigs of Gardenia carinata
Authors: Naowarat Kongkum
Patoomratana Tuchinda
Manat Pohmakotr
Vichai Reutrakul
Pawinee Piyachaturawat
Surawat Jariyawat
Kanoknetr Suksen
Chalobon Yoosook
Jitra Kasisit
Chanita Napaswad
Mahidol University
Keywords: Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Mar-2012
Citation: Fitoterapia. Vol.83, No.2 (2012), 368-372
Abstract: Four new flavones, 5,2′-dihydroxy-7,3′,4′,5′- tetramethoxyflavone (1), 5,2′,5′-trihydroxy-7,3′,4′- trimethoxyflavone (2), 5,7,2′,5′-tetrahydroxy-6,3′,4′- trimethoxyflavone (3) and 5,2′,5′-trihydroxy-6,7,3′,4′- tetramethoxyflavone (4), along with the known 5,3′-dihydroxy-6,7,4′, 5′-tetramethoxyflavone (5), 5,7,3′,5′-tetrahydroxy-6,4′- dimethoxyflavone (6), syringaldehyde, vanillic acid and scopoletin were isolated from the leaves and twigs of Gardenia carinata (Rubiaceae). Their structures were determined by spectroscopic methods. Flavone 2 exhibited cytotoxic activity against P-388 and MCF-7 cell lines, while 3, 5 and 6 were active only in P-388 cell line. All active compounds were found to inhibit DNA topoisomerase IIα activity, which may be responsible for the observed cytotoxicity. Flavones 1-3, 5 and 6 also exhibited anti-HIV-1 activity in the anti-syncytium assay using δTat/rev MC99 virus and 1A2 cell line system; 2 was most potent. Only flavones 1 and 6 showed considerably activity against HIV-1 reverse transcriptase. © 2011 Elsevier B.V. All rights reserve.
ISSN: 18736971
Appears in Collections:Scopus 2011-2015

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