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山奈酚通过拮抗雌激素相关受体 α 和 γ 的活性来抑制癌细胞生长。

Kaempferol inhibits cancer cell growth by antagonizing estrogen-related receptor α and γ activities.

机构信息

First Affiliated Hospital, Guangzhou University of Chinese Medicine, Guangzhou, 510405, China.

出版信息

Cell Biol Int. 2013 Nov;37(11):1190-6. doi: 10.1002/cbin.10152. Epub 2013 Aug 5.

DOI:10.1002/cbin.10152
PMID:23852933
Abstract

Kaempferol is a dietary flavonoid that can function as a selective estrogen receptor modulator (SERM). Estrogen-related receptors alpha and gamma (ERRα and ERRγ) are orphan nuclear receptors that play important roles in mitochondrial biogenesis and cancer development. We have shown that kaempferol can functionally antagonize the activities of ERRs based on both response element reporter systems and target gene analysis. Kaempferol modulation of mitochondrial function and suppression cancer cell growth has been confirmed. These findings suggest that kaempferol may exert their anti-cancer activities through antagonizing ERRs activities.

摘要

山柰酚是一种膳食类黄酮,可作为选择性雌激素受体调节剂(SERM)。雌激素相关受体α和γ(ERRα和 ERRγ)是孤儿核受体,在线粒体生物发生和癌症发展中发挥重要作用。我们已经证明,山柰酚可以通过反应元件报告系统和靶基因分析来拮抗 ERR 的功能。山柰酚对线粒体功能的调节和抑制癌细胞生长已得到证实。这些发现表明,山柰酚可能通过拮抗 ERR 活性发挥其抗癌作用。

相似文献

1
Kaempferol inhibits cancer cell growth by antagonizing estrogen-related receptor α and γ activities.山奈酚通过拮抗雌激素相关受体 α 和 γ 的活性来抑制癌细胞生长。
Cell Biol Int. 2013 Nov;37(11):1190-6. doi: 10.1002/cbin.10152. Epub 2013 Aug 5.
2
Kaempferol is an estrogen-related receptor alpha and gamma inverse agonist.山奈酚是一种雌激素相关受体α和γ反向激动剂。
FEBS Lett. 2009 Feb 18;583(4):643-7. doi: 10.1016/j.febslet.2009.01.030. Epub 2009 Jan 24.
3
Inhibition of estrogen receptor alpha expression and function in MCF-7 cells by kaempferol.山奈酚对MCF-7细胞中雌激素受体α表达和功能的抑制作用。
J Cell Physiol. 2004 Feb;198(2):197-208. doi: 10.1002/jcp.10398.
4
Epidermal growth factor-induced signaling in breast cancer cells results in selective target gene activation by orphan nuclear receptor estrogen-related receptor alpha.表皮生长因子诱导的乳腺癌细胞信号传导导致孤儿核受体雌激素相关受体α选择性激活靶基因。
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ERRgamma suppresses cell proliferation and tumor growth of androgen-sensitive and androgen-insensitive prostate cancer cells and its implication as a therapeutic target for prostate cancer.ERRγ抑制雄激素敏感和雄激素不敏感前列腺癌细胞的细胞增殖和肿瘤生长及其作为前列腺癌治疗靶点的意义。
Cancer Res. 2007 May 15;67(10):4904-14. doi: 10.1158/0008-5472.CAN-06-3855.
6
Estrogen-related receptor alpha and estrogen-related receptor gamma associate with unfavorable and favorable biomarkers, respectively, in human breast cancer.在人类乳腺癌中,雌激素相关受体α和雌激素相关受体γ分别与不良和良好的生物标志物相关联。
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7
Estrogen-related receptor gamma modulates energy metabolism target genes in human trophoblast.雌激素相关受体γ调节人滋养层细胞能量代谢靶基因。
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ERRs and cancers: effects on metabolism and on proliferation and migration capacities.错配修复基因缺陷与癌症:对代谢以及增殖和迁移能力的影响。
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ERRα metabolic nuclear receptor controls growth of colon cancer cells.ERRα 代谢核受体控制结肠癌细胞的生长。
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Characterization of a selective inverse agonist for estrogen related receptor α as a potential agent for breast cancer.雌激素相关受体α选择性反向激动剂作为乳腺癌潜在药物的特性研究
Eur J Pharmacol. 2016 Oct 15;789:439-448. doi: 10.1016/j.ejphar.2016.08.008. Epub 2016 Aug 4.

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