Glutathione S-Transferase Inhibiting Chemical Constituents of Caesalpinia bonduc

スポンサーリンク

概要

• 論文の詳細を見る

• 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-3α-ol (2), 13,14-seco-stigmasta-9 (11), 14-dien-3α-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 IC_<50> values of these compounds and their derivatives ranged from 57-380μм and were compared to the inhibitory effects due to sodium taurocholate, an isoprenederived GST inhibitor (IC_<50>=398μм). A plausible biosynthesis of 13, 14-seco-steroids has also been proposed.

• 公益社団法人日本薬学会の論文
• 2007-03-01

著者

• Samarasekera Radhika

  Natural Products Development Group Industrial Technology Institute

• UDENIGWE Chibuike

  Department of Chemistry, The University of Winnipeg

• ATA Athar

  Department of Chemistry, The University of Winnipeg

• Ata Athar

  Department Of Chemistry The University Of Winnipeg

• Udenigwe Chibuike

  Department Of Chemistry The University Of Winnipeg:department Of Chemistry The University Of Manitob

関連論文

• Glutathione S-Transferase Inhibiting Chemical Constituents of Caesalpinia bonduc
• Novel Microbial Transformations of Sclareolide
• Mucoralactone A: An Unusual Steroid from the Liquid Culture of Mucor plumbeus

スポンサーリンク