金柚提取物对雌激素受体调节作用的研究

摘要

Objective To study the effects of extracts from golden-pomelo ( Citrus grandis L .) on estrogen receptors ( ERs) and i-dentify the active constitutents .Methods The estrogenic activities of the extracts and HPLC isolated fractions were evaluated by the mamma -lian cell hybrid technology .The active constitutents had been identified by comparing with the UV-absorption spectrum and HPLC results of the standard substance .Their estrogenic activities were compared with that of estradiol and genistein .Results The extracts from golden-pomelo selectively were increased the activity of ERβwithout effecting on ERα.Naringin and naringenin were identified as two ERβagonists in the extracts.The relative estrogenic potency of the substances was estradiol>genistein>naringenin>naringin.Conclusions Golden-pomelo have the active constitutents for ERβand is promising in the related therapeutics and health care products .%目的：研究金柚提取物对雌激素受体（ER）的调节作用，并鉴定其功效成分。方法利用哺乳动物报告基因系统检测金柚总提取物及高效液相色谱（ HPLC）分离的单一化学成分对ERα和ERβ的调节作用。通过与标准品的紫外可见吸收光谱及 HPLC 图谱鉴定其活性成分，并与雌二醇、染料木苷等ER激活剂比较活性。结果金柚提取物能特异性激活 ERβ，对ERα无影响，活性成分主要为柚皮素和柚皮苷（部分激活剂），与雌二醇、染料木苷活性比较：雌二醇＞染料木苷＞柚皮素＞柚皮苷。结论金柚含有ERβ特异性激活成分，能用作ERβ相关的药物治疗及保健品。