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大叶千斤拔诱导其雌激素活性的潜在机制解析

Elucidation of Underlying Mechanisms by Which Millettia macrophylla Benth Induces Its Estrogenic Activity.

作者信息

Zingue Stéphane, Magne Nde Chantal Beatrice, Clyne Colin, Njamen Dieudonné

机构信息

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

MIMR-PHI Institute of Medical Research, Departments of Molecular and Translational Sciences, Monash University, 246 Clayton Road, Level 4, VIC 3168, Melbourne, Australia.

出版信息

Int Sch Res Notices. 2014 Aug 10;2014:763781. doi: 10.1155/2014/763781. eCollection 2014.

DOI:10.1155/2014/763781
PMID:27433539
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4897398/
Abstract

Millettia macrophylla is used traditionally to treat menopause related symptoms. This plant was shown to exhibit estrogenic effects in vitro on human embryonic kidney cells and in vivo on ovariectomized rats. The present study aimed at elucidating underlying mechanisms by which M. macrophylla induced its estrogenic effects. To accomplish our goal, kidney Hek293T cells transiently transfected with estrogen alpha or beta receptor expression plasmids were cotreated with a pure antiestrogen ICI 182,780 and the dichloromethane or methanol soluble fractions of M. macrophylla. To follow up, we cotreated ovariectomized rats with both extracts and ICI 182,780 for 3 days in the classical uterotrophic assay. Animals were then sacrificed and the uterine wet weight, total protein levels in uteri, uterine, and vaginal epithelial heights, and mammary gland were assessed. In vitro, the results suggested that the induction of the estrogenic activity by M. macrophylla is due to the binding of its secondary metabolites to ERα and ERβ. In vivo, the cotreatment of extracts and ICI 182,780 significantly abrogated the biological responses induced by the extracts alone. Taken together, these results indicate that the active principles of M. macrophylla induce their beneficial effects on menopausal symptoms by activating the ERs.

摘要

大叶千斤拔传统上用于治疗与更年期相关的症状。这种植物在体外对人胚肾细胞以及在体内对去卵巢大鼠均显示出雌激素样作用。本研究旨在阐明大叶千斤拔产生雌激素样作用的潜在机制。为实现我们的目标,将瞬时转染雌激素α或β受体表达质粒的肾Hek293T细胞与纯抗雌激素ICI 182,780以及大叶千斤拔的二氯甲烷或甲醇可溶部分共同处理。接下来,在经典的子宫增重试验中,我们将去卵巢大鼠与这两种提取物和ICI 182,780共同处理3天。然后处死动物,评估子宫湿重、子宫中的总蛋白水平、子宫和阴道上皮高度以及乳腺。在体外,结果表明大叶千斤拔雌激素活性的诱导是由于其次级代谢产物与ERα和ERβ的结合。在体内,提取物与ICI 182,780的共同处理显著消除了单独提取物诱导的生物学反应。综上所述,这些结果表明大叶千斤拔的活性成分通过激活雌激素受体对更年期症状产生有益作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e6/4897398/9dfcc84f4a5b/ISRN2014-763781.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e6/4897398/7cb1a9cc0b2b/ISRN2014-763781.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e6/4897398/20714878b6b1/ISRN2014-763781.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e6/4897398/e9c5e9f045a0/ISRN2014-763781.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e6/4897398/9dfcc84f4a5b/ISRN2014-763781.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e6/4897398/7cb1a9cc0b2b/ISRN2014-763781.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e6/4897398/20714878b6b1/ISRN2014-763781.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e6/4897398/e9c5e9f045a0/ISRN2014-763781.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e6/4897398/9dfcc84f4a5b/ISRN2014-763781.004.jpg

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2
The methanol-soluble fraction of Millettia macrophylla (Fabaceae) stem bark endowed with estrogenic properties has adverse effects on the male reproductive system of Wistar rats.具有雌激素特性的大叶崖豆藤(豆科)茎皮的甲醇可溶部分对Wistar大鼠的雄性生殖系统有不良影响。
J Basic Clin Physiol Pharmacol. 2015 Jan;26(1):53-64. doi: 10.1515/jbcpp-2013-0136.
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BMC Complement Altern Med. 2016 Oct 26;16(1):421. doi: 10.1186/s12906-016-1385-5.
Effects of Millettia macrophylla (Fabaceae) extracts on estrogen target organs of female wistar rat.
鱼骨木(豆科)提取物对雌性 Wistar 大鼠雌激素靶器官的影响。
J Pharmacol Sci. 2013;123(2):120-31. doi: 10.1254/jphs.13094fp. Epub 2013 Sep 27.
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