苦参根中薰衣草基黄酮苦参酮的雌激素和抗癌特性。

Estrogenic and anticarcinogenic properties of kurarinone, a lavandulyl flavanone from the roots of Sophora flavescens.

作者信息

De Naeyer An, Vanden Berghe Wim, Pocock Victoria, Milligan Stuart, Haegeman Guy, De Keukeleire Denis

机构信息

Laboratory of Pharmacognosy and Phytochemistry, Faculty of Pharmaceutical Sciences, Ghent University, Harelbekestraat 72, B-9000 Ghent, Belgium.

出版信息

J Nat Prod. 2004 Nov;67(11):1829-32. doi: 10.1021/np040069a.

DOI:10.1021/np040069a

PMID:15568770

Abstract

Kurarinone, a lavandulyl flavanone, was isolated from a polyphenolic extract of the roots of Sophora flavescens using fractionation guided by estrogenic activity, which was determined by recombinant yeast and Ishikawa Var-I bioassays. Kurarinone showed weak estrogenic activity both in the yeast screen and in the Ishikawa Var-I assay with EC(50) values of 4.6 and 1.66 microM, respectively. Furthermore, kurarinone was found to have potent cytotoxic activity (IC(50) value = 22.2 microM) against human MCF-7/6 breast cancer cells in the sulforhodamine-B assay.

摘要

苦参酮是一种薰衣草基黄酮，从苦参根的多酚提取物中分离得到，分离过程采用雌激素活性导向分级法，雌激素活性通过重组酵母和石川Var-I生物测定法测定。苦参酮在酵母筛选实验和石川Var-I实验中均显示出较弱的雌激素活性，其半数有效浓度（EC50）值分别为4.6微摩尔和1.66微摩尔。此外，在磺酰罗丹明B实验中发现，苦参酮对人MCF-7/6乳腺癌细胞具有较强的细胞毒性活性（半数抑制浓度（IC50）值 = 22.2微摩尔）。