期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 55, 期 3, 页码 442-445出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.55.442
关键词
Caesalpinia bonduc; glutathione S-transferase; 13,14-seco-sterol; pipataline; caesaldekarin J
Glutathione S-transferase inhibition assay-guided fractionations on the ethanolic extract of the bark of Caesalpinia bonduc resulted in the isolation of a new sterol, 17-hydroxy-campesta-4,6-dien-3-one (1) along with four known compounds, 13,14-seco-stigmasta-5,14-dien-alpha-ol (2), 13,14-seco-stigmasta-9(11),14-dien-3 alpha-ol (3), caesaldekarin J (4) and pipataline (5) as active constituents. Structures of compounds 1-5 were established on the basis of extensive NMR spectroscopic studies. The compounds (1-5) were isolated on the basis of their inhibitory activity against glutathione S-transferase, an enzyme that has been implicated in resistances during treatment of cancer and parasitic infections. Efforts to study structure-activity relationships of compounds 2 and 3 were also made by modifying their structures. The IC50 values of these compounds and their derivatives ranged from 57-380 mu m and were compared to the inhibitory effects due to sodium taurocholate, an isoprene-derived GST inhibitor (IC30 = 398 mu m). A plausible biosynthesis of 13,14-seco-steroids has also been proposed.
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