| Literature DB >> 24411124 |
Hsin-Yi Hung1, Kyoko Nakagawa-Goto2, Harukuni Tokuda3, Akira Iida4, Nobutaka Suzuki3, Ibrahim D Bori5, Keduo Qian6, Kuo-Hsiung Lee7.
Abstract
Ten new 3,4-seco betulinic acid (BA) derivatives were designed and synthesized. Among them, compounds 7-15 exhibited enhanced chemopreventive ability in an in vitro short-term 12-O-tetradecanoylphorbol-13-acetate (TPA) induced Epstein-Barr virus early antigen (EBV-EA) activation assay in Raji cells. Specifically, analogs with a free C-28 carboxylic acid, including 7, 8, 11, and 13, inhibited EBV-EA activation significantly. The most potent compound 8 displayed 100% inhibition at 1×10(3) mol ratio/TPA and 73.4%, 35.9%, and 8.4% inhibition at 5×10(2), 1×10(2), and 1×10 mol ratio/TPA, respectively, comparable with curcumin at high concentration and better than curcumin at low concentration. The potent chemopreventive activity of novel seco A-ring BAs (8 and 11) was further confirmed in an in vivo mouse skin carcinogenesis assay.Entities:
Keywords: Betulinic acid; Chemopreventive; EBV-EA; seco A-ring
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Year: 2013 PMID： 24411124 PMCID： PMC3936349 DOI： 10.1016/j.bmcl.2013.12.041
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823