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学科主题: 物理化学
题名: Estrogenic and anti-estrogenic activities of hispolon from Phellinus lonicerinus (Bond.) Bond. et sing
作者: Wang, Junzhi1, 2;  Hu, Fang1;  Luo, Youcheng1;  Luo, Huajun1;  Huang, Nianyu1;  Cheng, Fan1;  Deng, Zhangshuang1;  Deng, Weiqiao3;  Zou, Kun1
通讯作者: NianyuHuang
关键词: Hispolon ;  Phellinus lonicerinus (Bond.) Bond. et sing ;  Estrogenic and anti-estrogenic activity ;  Breast cancer cells (MCF-7MDA-MB-231) ;  Yeast two-hybrid assay
刊名: FITOTERAPIA
发表日期: 2014-06-01
DOI: 10.1016/j.fitote.2014.03.007
卷: 95, 期:1, 页:93-101
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Chemistry, Medicinal ;  Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: Hispolon was the main antitumor active ingredient in Phellinus sensu lato species. In order to confirm the dual regulating estrogenic ingredient and obtain more effective natural estrogen replacement drugs, hispolon was separated from Phellinus lonicerinus (Bond.) Bond. et sing. Hispolon exhibited significant anti-proliferative effect against estrogen-sensitive ER (+) MCF-7 cells in the absence of estrogen, and exhibits antagonistic effects on 17 ss-estradiol (E-2)-induced MCF-7 cell proliferation when E-2 and the different concentrations of hispolon were treated simultaneously. Hispolon also inhibited the proliferation of estrogen-negative ER (-) MDA-MB-231 cells at the concentration of 5.00 x 10(-5) M. The yeast two-hybrid experiments showed that hispolon had strong and non-selective effects on the estrogen receptor (ER) alpha and ER ss at a concentration of 1.00 x 10(-6) M. The ER ss-binding ability of hispolon was larger than ER alpha in the concentration range of 1.00 x 10(-9) M and 1.00 x 10(-7) M. Hispolon could increase the body weight coefficient, serum E-2 and progesterone contents in immature female mice at dose of 9.10 x 10(-6) mol/kg, and increase coefficient of thymus and spleen in mice. The Gscores of hispolon-ER alpha and hispolon-ER ss docked complexes were -7.93 kcal/mol and -7.79 kcal/mol in docking simulations. Hispolon presented dual regulating estrogenic activities, which showed estrogenic agonist activity at low concentration or lack of endogenous estrogen, and the estrogenic antagonistic effect was stimulated at high concentrations or too much endogenous estrogen. Hispolon could be used for treating the estrogen deficiency-related disease with the benefit of non-toxic to normal cells, good antitumor effects and estrogenic activity. (C) 2014 Elsevier B.V. All rights reserved.
关键词[WOS]: BREAST-CANCER ;  MEDICINAL MUSHROOMS ;  THERAPY ;  PHYTOESTROGENS ;  CHEMICALS ;  RECEPTOR ;  LINTEUS ;  FUNGI ;  DRUGS ;  CELLS
语种: 英语
WOS记录号: WOS:000336819400012
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/143985
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.China Three Gorges Univ, Hubei Key Lab Nat Prod Res & Dev, Yichang 443002, Peoples R China
2.China Three Gorges Univ, Hubei Tujia Inst Med, Yichang 443002, Peoples R China
3.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China

Recommended Citation:
Wang, Junzhi,Hu, Fang,Luo, Youcheng,et al. Estrogenic and anti-estrogenic activities of hispolon from Phellinus lonicerinus (Bond.) Bond. et sing[J]. FITOTERAPIA,2014,95(1):93-101.
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