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紫堇属植物化学成分的内分泌作用研究 2. 化合物与雌激素受体的体外结合。

Studies on the endocrine effects of the contents of Cimicifuga racemosa 2. In vitro binding of compounds to estrogen receptors.

机构信息

Schaper & Brümmer GmbH & Co KG, Postfach 611160, D-3320 Salzgitter 61.

出版信息

Planta Med. 1985 Aug;51(4):316-9. doi: 10.1055/s-2007-969500.

Abstract

The endocrine activity of compounds of the rhizome of CIMICIFUGA RACEMOSA can be demonstrated in the IN VIVO model of the ovariectomized rat as well as in the IN VITRO system of the estrogen receptor assay. A reduction of the serum levels of luteinizing hormone in ovariectomized rats takes place upon application of a methanol-extract. This extract contains substances, which are able to bind to estrogen receptors of rat uteri. Using the estrogen receptor assay as a pharmacological testsystem to determine the activity of different fractions, the chromatographic separation of the methanol-extract resulted in at least three different endocrine active compounds. One of these could be identified as the isoflavon Formononetine. The endocrine activity of this isoflavon was characterized in both described testsystems. It can be shown that Formononetine is a competitor in the estrogen receptor assay, but failed to reduce the serum levels of luteinizing hormone in overiectomized rats.

摘要

升麻根茎化合物的内分泌活性可以在去卵巢大鼠的体内模型以及雌激素受体测定的体外系统中得到证明。甲醇提取物可使去卵巢大鼠的血清黄体生成素水平降低。该提取物含有能够与大鼠子宫雌激素受体结合的物质。使用雌激素受体测定作为药理学测试系统来确定不同馏分的活性,甲醇提取物的色谱分离导致至少三种不同的内分泌活性化合物。其中之一可以鉴定为异黄酮芒柄花素。在这两个描述的测试系统中都对这种异黄酮的内分泌活性进行了表征。可以表明芒柄花素是雌激素受体测定中的竞争性抑制剂,但不能降低去卵巢大鼠的血清黄体生成素水平。

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