College of Pharmacy, Sookmyung Women's University, Seoul, Republic of Korea.
Phytother Res. 2010 Feb;24(2):295-300. doi: 10.1002/ptr.2966.
Caffeic acid phenethyl ester (CAPE) is an active ingredient of beehive propolis with a structure similar to phenolic acid. The estrogenic effects of propolis were previously demonstrated through the activation of an estrogen receptor. To identify the estrogenic properties of propolis, CAPE was evaluated using in vitro and in vivo methods. CAPE showed selective binding affinity to human estrogen receptor beta (hERbeta) rather than hERalpha. CAPE also reduced ERalpha expression in MCF-7 and MDA 231 cells. In the yeast estrogen receptor transcription assay, CAPE produced the transcriptional activity of estrogen-responsive element with EC(50) values of 3.72 x 10(-6) M. CAPE did not increase the growth of MCF-7 estrogen receptor-positive breast cancer cells in doses ranging from 10(-7) to 10(-5) M. In order to understand how CAPE acts in animals, CAPE was tested by a uterotrophic bioassay. Treatment with CAPE (100, 500 mg/kg) did not increase the uterine weight relative to 3 microg/kg 17beta-estradiol treatment. The results indicate that CAPE, which is a selective agonist to hERbeta, but does not show any estrogenic effect on estrogen receptor-positive breast cancer cells and in immature rat uterine tissue, is a potential selective estrogen receptor modulator.
咖啡酸苯乙酯（CAPE）是一种具有与酚酸相似结构的蜂胶活性成分。蜂胶的雌激素作用先前是通过激活雌激素受体来证明的。为了确定蜂胶的雌激素特性，使用体外和体内方法评估了 CAPE。CAPE 对人雌激素受体β（hERβ）具有选择性结合亲和力，而不是 hERα。CAPE 还降低了 MCF-7 和 MDA 231 细胞中 ERα 的表达。在酵母雌激素受体转录测定中，CAPE 产生雌激素反应元件的转录活性，EC（50）值为 3.72 x 10（-6）M。CAPE 在 10（-7）至 10（-5）M 的剂量范围内不会增加 MCF-7 雌激素受体阳性乳腺癌细胞的生长。为了了解 CAPE 在动物中的作用方式，通过子宫增重生物测定对 CAPE 进行了测试。与 3μg/kg 17β-雌二醇处理相比，CAPE（100、500mg/kg）处理并未增加子宫重量。结果表明，CAPE 是 hERβ 的选择性激动剂，但对雌激素受体阳性乳腺癌细胞和未成熟大鼠子宫组织没有任何雌激素作用，是一种潜在的选择性雌激素受体调节剂。
