作者: Chibuike C. Udenigwe , Athar Ata , Radhika Samarasekera
DOI: 10.1248/CPB.55.442
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摘要: Glutathione S-transferase inhibition assay-guided fractionations on the ethanolic extract of bark Caesalpinia bonduc resulted in isolation a new sterol, 17-hydroxy-campesta-4,6-dien-3-one (1) along with four known compounds, 13,14-seco-stigmasta-5,14-dien-3alpha-ol (2), 13,14-seco-stigmasta-9(11),14-dien-3alpha-ol (3), caesaldekarin J (4) and pipataline (5) as active constituents. Structures compounds 1-5 were established basis extensive NMR spectroscopic studies. The (1-5) isolated their inhibitory activity against glutathione S-transferase, an enzyme that has been implicated resistances during treatment cancer parasitic infections. Efforts to study structure-activity relationships 2 3 also made by modifying structures. IC50 values these derivatives ranged from 57-380 microM compared effects due sodium taurocholate, isoprene-derived GST inhibitor (IC50=398 microM). A plausible biosynthesis 13,14-seco-steroids proposed.