ANTIFERTILITY AND HORMONAL PROPERTIES OF CERTAIN CAROTANE SESQUITERPENES OF FERULA-JAESCHKEANA

ANTIFERTILITY AND HORMONAL PROPERTIES OF CERTAIN CAROTANE SESQUITERPENES OF FERULA-JAESCHKEANA
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DOI:
10.1055/s-2006-962526
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发表时间:
1988-12-01
期刊:
影响因子:
2.7
通讯作者:
KAMBOJ, VP
KAMBOJ, VP
中科院分区:
医学3区
文献类型:
--
作者:
SINGH, MM;AGNIHOTRI, A;KAMBOJ, VP

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在评估的阿魏的 7 种胡萝卜素倍半萜中,三种阿魏二醇酯(化合物 3、5 和 6)在大鼠交配后第 1-7 天口服给药时显示出避孕功效。然而,在切除卵巢的未成熟雌性大鼠中,活性化合物表现出雌激素活性,但缺乏抗雌激素活性。使用竞争性蛋白质结合测定,化合物3、5和6对大鼠子宫胞质雌激素受体的17β-雌二醇的相对结合亲和力分别为0.01%、5.75%和0.75%。
Of the 7 carotane sesquiterpenes of Ferula jaeschkeana Vatke evaluated, three jaeschkaeanadiol esters (compounds 3, 5, and 6) showed contraceptive efficacy when administered orally on days 1-7 post coitum in rats. In ovariectomized immature female rats, however, the active compounds exhibited estrogenic activity and were devoid of antiestrogenic activity. Using a competitive protein binding assay, the compounds 3, 5, and 6 showed relative binding affinity of 0.01%, 5.75%, and 0.75% of 17.beta.-estradiol, respectively, for rat uterine cytosol estrogen receptors.