A quantitative structure - Activity relationship for the modulation effects of flavonoids on P-glycoprotein-mediated transport

Ming Thau Sheu, Yi Bo Liou, Yu Han Kao, Ying Ku Lin, Hsiu O. Ho

研究成果: 雜誌貢獻文章

33 引文 斯高帕斯(Scopus)

摘要

P-Glycoprotein accounts for multidrug resistance in chemotherapy patients and contributes to reduced oral bioavailability and distribution of drugs in the brain. The aim of this study was to establish the qualitative and quantitative structure - activity relationships (QSAR) of flavonoid modulation effects on P-glycoprotein (P-gp)'s function. Using human colorectal adenocarcinoma (HCT15) cells as an in vitro model and fexofenadine as a P-gp substrate, the modulation effects on P-gp at three concentration levels of 22 representative compounds from four flavonoid families were evaluated. Results showed that the modulation (enhanced or inhibitory) effects could be divided into three ranges designated as enhanced (217%) as compared to verapamil. An optimal QSAR was constructed for Y1 (adjusted R2=0.4798), Y2 (adjusted R 2=0.6809), and Y3 (adjusted R2=0.5902), respectively. This was further con-firmed by a highly correlated plot of the predicted percent inhibition against observed values from a respective QSAR equation.

原文英語
頁(從 - 到)1187-1194
頁數8
期刊Chemical and Pharmaceutical Bulletin
58
發行號9
DOIs
出版狀態已發佈 - 九月 2010

ASJC Scopus subject areas

  • Drug Discovery
  • Chemistry(all)

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