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榕叶榕(桑科)提取物的雌激素样作用及其缓解Wistar大鼠卵巢切除诱导的某些更年期症状的能力。

Estrogenic effects of Ficus umbellata Vahl. (Moraceae) extracts and their ability to alleviate some menopausal symptoms induced by ovariectomy in Wistar rats.

作者信息

Zingue Stéphane, Michel Thomas, Tchatchou Jules, Chantal Beatrice Magne Nde, Winter Evelyn, Monchot André, Awounfack Charline Florence, Djiogue Sefirin, Clyne Colin, Fernandez Xavier, Creczynski-Pasa Tânia Beatriz, Njamen Dieudonné

机构信息

Department of Life and Earth Sciences, Higher Teachers' Training College, University of Maroua, P.O. Box 55, Maroua, Cameroon; Department of Animal Biology and Physiology, Faculty of Science, University of Yaounde I, P.O. Box 812, Yaounde, Cameroon.

Institute of Chemistry of Nice, Faculty of Science, University Nice Sophia-Antipolis, UMR CNRS 7272, Valrose Park, F-06108 Nice Cedex 2, Nice, France.

出版信息

J Ethnopharmacol. 2016 Feb 17;179:332-44. doi: 10.1016/j.jep.2016.01.004. Epub 2016 Jan 4.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Ficus umbellata Vahl. (Moraceae) is a medicinal plant used in Cameroon to treat amenorrhea as well as other physiological disorders related to menopause.

AIM OF STUDY

In order to justify scientifically its traditional use, the estrogen-like properties of the aqueous (AE) and methanol (MeOH) extracts of F. umbellata were investigated.

MATERIAL AND METHODS

In vitro, the ability of different extracts of F. umbellata to activate estrogen receptors α (ERα) and β (ERβ) in cell-based reporter gene assays using human embryonic kidney (HEK293T) cells transfected with ERs was tested. In vivo, a 3-day uterotrophic assay and the capacity of the extracts to alleviate hot flushes in ovariectomized adult rats were tested. Using a bioassay-guided fractionation the major compound of F. umbellata was isolated and tested in vitro on HEK293T-ERα and ERβ cells.

RESULTS

AE and MeOH extracts significantly altered ERα as well as ERβ activities. In vivo, both extracts significantly increase the uterine and vaginal epithelium thickness, and uterine total protein levels in a dose dependent manner. Interestingly, both extracts of F. umbellata at the dose of 100 mg/kg BW significantly decreased the total number, average duration as well as frequency of hot flushes in experimental rats compared to age-matched OVX controls. Finally, 7-methylumbelliferone, a coumarin was characterized as the major compound of F. umbellata; however this compound did not transactivate ERα as well ERβ in vitro.

CONCLUSION

These aforementioned results suggest that F. umbellata extracts as used by the traditional practitioner have estrogen-like effects and may alleviate some menopausal problems such as vaginal dryness and hot flushes.

摘要

民族药理学相关性

伞花榕(桑科)是喀麦隆一种用于治疗闭经以及其他与更年期相关生理紊乱的药用植物。

研究目的

为了科学地证明其传统用途,对伞花榕水提取物(AE)和甲醇提取物(MeOH)的雌激素样特性进行了研究。

材料与方法

在体外,使用转染了雌激素受体的人胚肾(HEK293T)细胞,通过基于细胞的报告基因检测来测试伞花榕不同提取物激活雌激素受体α(ERα)和β(ERβ)的能力。在体内,进行了为期3天的子宫增重试验,并测试了提取物减轻去卵巢成年大鼠潮热的能力。通过生物测定引导的分级分离法分离出伞花榕的主要化合物,并在体外对HEK293T - ERα和ERβ细胞进行测试。

结果

AE和MeOH提取物显著改变了ERα以及ERβ的活性。在体内,两种提取物均以剂量依赖性方式显著增加子宫和阴道上皮厚度以及子宫总蛋白水平。有趣的是,与年龄匹配的去卵巢对照组相比,伞花榕两种提取物在100 mg/kg体重剂量下均显著降低了实验大鼠潮热的总数、平均持续时间以及频率。最后,香豆素7 - 甲基伞形酮被鉴定为伞花榕的主要化合物;然而,该化合物在体外并未激活ERα和ERβ。

结论

上述结果表明,传统从业者使用的伞花榕提取物具有雌激素样作用,可能缓解一些更年期问题,如阴道干燥和潮热。

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