Estrogen-like effect of a Cimicifuga racemosa extract sub-fraction as assessed by in vivo, ex vivo and in vitro assays
Estrogen-like effect of a Cimicifuga racemosa extract sub-fraction as assessed by in vivo, ex vivo and in vitro assays
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DOI：
10.1016/j.jsbmb.2007.03.044
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发表时间：
2007-11-01
影响因子：
4.1
通讯作者：
Evandri, M. G.
中科院分区：
文献类型：
--
作者：
Bolle, P.;Mastrangelo, S.;Evandri, M. G.
黑升麻（Cimicifuga racemosa）用于治疗痛经和更年期症状。关于活性化合物的性质和作用机制的数据仍然存在争议，主要是关于其雌激素活性。本研究旨在通过体内、离体和体外实验，评估总状花干醇提取物及其亲水和亲脂亚组分可能的雌激素活性。在酵母雌激素筛选中，只有亲脂亚组分能够激活人类雌激素受体α，其效力较低，但与17 -雌二醇的功效相当。总提取物和亲脂亚组分均未显示出21日龄大鼠体内子宫萎缩作用。与戊酸雌二醇处理的大鼠相比，总状假单胞菌处理动物的离体子宫组织对催产素、前列腺素F-2 α和缓激素的敏感性一般要低得多。相反，亲脂亚组分对28日龄大鼠子宫角的催产素、前列腺素F-2 α和缓激素的体外反应具有剂量依赖性的抑制活性，其效价接近17 β -雌二醇的1:30。报道的结果证实了总状念珠菌在月经困扰中的有效性，并进一步强调了亲脂性成分与尚未确定的雌激素受体结合的可能性，可能与炎症负相关。(c) 2007 Elsevier Ltd.版权所有。
Black cohosh (Cimicifuga racemosa) is used in the treatment of painful menstruation and menopausal symptoms. Data about the nature of the active compounds and mechanism(s) of action are still controversial, chiefly with respect to its estrogenic activity.This work aimed to assess the possible estrogenic activity of a commercial dry hydro-alcoholic extract of C. racemosa and its hydrophilic and lipophilic sub-fractions on in vivo, ex vivo, and in vitro assays.In a yeast estrogen screen, only the lipophilic sub-fraction was able to activate the human estrogen receptor alpha, with a lower potency but comparable efficacy to that of 17 beta-estradiol.Neither the total extract nor the lipophilic sub-fraction showed an in vivo uterotrophic effect in 21-day-old rats. Uterine tissues obtained ex vivo from C. racemosa treated animals were generally much less sensitive to oxytocin, prostaglandin F-2 alpha, and bradykinin than tissues obtained from estradiol valerate treated rats.The Lipophilic sub-fraction, instead, induced a dose-dependent inhibitory activity on the in vitro response to oxytocin, prostaglandin F-2 alpha, and bradykinin of uterine horns from naive 28-day-old rats, with a potency rate close to 1:30 of that of 17 beta-estradiol.Reported results confirm the effectiveness of C. racemosa in menstrual distress and further emphasize the possibility that lipophilic constituents bind to an as yet not identified estrogen receptor, likely inversely involved in inflammation.(c) 2007 Elsevier Ltd. All rights reserved.