Estrogenic activity of triterpene glycosides in yeast two-hybrid assay
Estrogenic activity of triterpene glycosides in yeast two-hybrid assay
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DOI：
10.1016/j.jsbmb.2006.06.022
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发表时间：
2006-11-01
影响因子：
4.1
通讯作者：
Aminin, D. L.
中科院分区：
文献类型：
--
作者：
Kovalchuk, S. N.;Kozhemyako, V. B.;Aminin, D. L.
以人雌激素受体基因HERα、共激活因子TIF2和LacZ为报告基因，用酵母双杂交系统检测了天然产物和半合成人参皂苷Rh-2的6种三萜苷：海参皂苷A、全毒素A(1)、前叶皂苷A、黄瓜皂苷A(2)-2和人参皂苷C的雌激素活性。只有人参皂苷-Rh在10(-7)-10(-6)M的浓度范围内表现出显著的中等雌激素样活性，其作用约为在半效浓度下应用17β-雌二醇活性的30%。这表明人参皂苷-Rh-2是一种弱的植物雌激素。海参三萜苷、海参糖苷A、全毒素A(1)、黄瓜皂苷A(2)-2、海参皂苷A(2)-2、海参皂苷C没有明显的雌激素样活性。酵母双杂交实验得到的数据反映了被测化合物和17β-雌二醇之间的构效关系。只有人参皂苷-Rh在化学结构上与17β-雌二醇有一些相似之处，这可能解释了这种糖苷与HERα受体的亲和力。(C)2006爱思唯尔有限公司。保留所有权利。
Estrogenic potency of six triterpene glycosides, Holothurin A, Holotoxin A(1), Frondoside A, Cucumarioside A(2)-2 and Cauloside C, that are natural products and semi-synthesized Ginsenoside-Rh-2, were examined with yeast two-hybfid system, including expressed genes of human estrogen receptor, hER alpha, the co-activator TIF2 and lacZ as a reporter gene. Only Ginsenoside-Rh, exhibited significant moderate estrogenic activity in the concentration range of 10(-7) to 10(-6) M. Its effect was approximately 30% of the activity of 17 beta-estradiol applied at half-effective concentration. This indicates Ginsenosides-Rh-2 is a weak phytoestrogen. The sea cucumber triterpene glycosides, Holothurin A, Holotoxin A(1), Cucumarioside A(2)-2 and Frondoside A, and plant glycoside Cauloside C had no appreciable estrogenic activity. Data obtained by yeast two-hybrid assay reflect structure-activity relationship between tested compounds and 17 beta-estradiol. Only Ginsenoside-Rh, has some similarity in chemical structure with 17 beta-estradiol that might explain affinity of this glycoside to the hER alpha receptor. (c) 2006 Elsevier Ltd. All rights reserved.