Yap S P, Shen P, Li J, Lee L S, Yong E L
Department of Obstetrics & Gynecology, National University Hospital, Yong Loo Lin School of Medicine, National University of Singapore, Singapore.
J Ethnopharmacol. 2007 Sep 5;113(2):218-24. doi: 10.1016/j.jep.2007.05.029. Epub 2007 Jun 2.
The Chinese medicinal herb, Epimedium, used traditionally for bone health exerts estrogenic activity (EA) in vitro. A genetically characterized Epimedium brevicornum (EB) extract induced biphasic responses in the mRNA and protein expression of the estrogen-regulated progesterone receptor gene in breast cancer (MCF-7) cells. These changes were mirrored changes in estrogenic receptor (ERalpha) content. In male Sprague-Dawley rats, administration of the estrogenic prodrug, estradiol valerate increased area-under-curve of serum effects for ERalpha (AUC difference: 18,900EA(ERalpha) min; 95% CI: 0-37,800; p = 0.05) and breast cancer cell (MCF-7) growth (AUC difference: 30,200EA(MCF-7) min; 95% CI: 24,200-36,200; p<0.001), compared to placebo. Oral administration of Epimedium brevicornum increased ERalpha activity (1320EA(ERalpha) min, p<0.01). Our data indicate that estrogen-responsive bioassays can measure the pharmacokinetic/pharmacodynamics of estrogenic activity in serum. Epimedium brevicornum extract increases estrogenic activity in serum and human studies are required to evaluate whether Epimedium extracts have utility for estrogen replacement therapy.
传统上用于骨骼健康的中药淫羊藿在体外具有雌激素活性（EA）。一种经过基因鉴定的短角淫羊藿（EB）提取物在乳腺癌（MCF-7）细胞中诱导了雌激素调节的孕激素受体基因的mRNA和蛋白质表达的双相反应。这些变化反映在雌激素受体（ERα）含量的变化上。在雄性Sprague-Dawley大鼠中，与安慰剂相比，给予雌激素前体药物戊酸雌二醇可增加血清中ERα效应的曲线下面积（AUC差异：18,900EA(ERα)分钟；95%置信区间：0-37,800；p = 0.05）以及乳腺癌细胞（MCF-7）的生长（AUC差异：30,200EA(MCF-7)分钟；95%置信区间：24,200-36,200；p<0.001）。口服短角淫羊藿可增加ERα活性（1320EA(ERα)分钟，p<0.01）。我们的数据表明，雌激素反应性生物测定法可测量血清中雌激素活性的药代动力学/药效学。短角淫羊藿提取物可增加血清中的雌激素活性，需要进行人体研究以评估淫羊藿提取物是否可用于雌激素替代疗法。
