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锯叶棕对猪前列腺微粒体5α-还原酶活性动力学的抑制作用。

Inhibitory effects of Serenoa repens on the kinetic of pig prostatic microsomal 5alpha-reductase activity.

作者信息

Palin M F, Faguy M, LeHoux J G, Pelletier G

机构信息

Agriculture and Agri-Food Canada, Dairy and Swine Research and Development Centre, Lennoxville, Quebec.

出版信息

Endocrine. 1998 Aug;9(1):65-9. doi: 10.1385/ENDO:9:1:65.

DOI:10.1385/ENDO:9:1:65
PMID:9798732
Abstract

The pathogenesis of benign prostatic hyperplasia is linked to the accumulation of dihydrotestosterone (DHT), the active form of testosterone (T), in prostatic tissue. We have defined characteristics of 5alpha-reductase enzyme which catalyzes the conversion of T into DHT in prostatic microsomes of growing pigs. Peaks for the 5alpha-reductase activity were found at pH 5.5 and 8.0, which indicates the presence of both type 1 and type 2 isozymes. Kinetic parameters of porcine 5alpha-reductase in the presence of Serenoa repens extracts revealed uncompetitive, noncompetitive, and mixed types of inhibitions. Our results show the inhibitory action of S. repens on prostate porcine microsomal 5alpha-reductase activity.

摘要

良性前列腺增生的发病机制与双氢睾酮(DHT,睾酮(T)的活性形式)在前列腺组织中的蓄积有关。我们已明确了在生长猪前列腺微粒体中催化T转化为DHT的5α-还原酶的特性。在pH 5.5和8.0时发现了5α-还原酶活性的峰值,这表明同时存在1型和2型同工酶。在锯叶棕提取物存在的情况下,猪5α-还原酶的动力学参数显示出非竞争性、非竞争性和混合型抑制作用。我们的结果表明锯叶棕对猪前列腺微粒体5α-还原酶活性具有抑制作用。

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本文引用的文献

1
The Lipidosterolic Extract fromSerenoa repens Interferes with Prolactin Receptor Signal Transduction.锯叶棕的脂质固醇提取物干扰催乳素受体信号转导。
J Biomed Sci. 1995 Oct;2(4):357-365. doi: 10.1007/BF02255223.
2
Stimulation of prostate cancer growth by androgens and estrogens through the intermediacy of sex hormone-binding globulin.雄激素和雌激素通过性激素结合球蛋白介导刺激前列腺癌生长。
Endocrinology. 1996 Oct;137(10):4126-9. doi: 10.1210/endo.137.10.8828467.
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Characterization of Chinese hamster ovary cell lines expressing human steroid 5 alpha-reductase isozymes.
Acta Pharmacol Sin. 2009 Mar;30(3):227-81. doi: 10.1038/aps.2009.1.
表达人甾体5α-还原酶同工酶的中国仓鼠卵巢细胞系的特性分析。
J Biol Chem. 1993 Aug 15;268(23):17404-12.
4
Finasteride: a slow-binding 5 alpha-reductase inhibitor.非那雄胺:一种慢结合型5α-还原酶抑制剂。
Biochemistry. 1993 Jun 1;32(21):5705-10. doi: 10.1021/bi00072a028.
5
Inhibition of the activity of 'basic' 5 alpha-reductase (type 1) detected in DU 145 cells and expressed in insect cells.对在DU 145细胞中检测到并在昆虫细胞中表达的“基础”5α-还原酶(1型)活性的抑制作用。
J Steroid Biochem Mol Biol. 1994 Mar;48(4):347-52. doi: 10.1016/0960-0760(94)90074-4.
6
Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2.依立雄胺是一种对人甾体5α-还原酶同工酶2具有选择性和特异性的非竞争性抑制剂。
J Steroid Biochem Mol Biol. 1994 Feb;48(2-3):197-206. doi: 10.1016/0960-0760(94)90145-7.
7
Study of estramustine binding protein: its relationship to androgen dependency and histological differentiation in human prostatic carcinoma tissue.雌莫司汀结合蛋白的研究:其与人类前列腺癌组织中雄激素依赖性及组织学分化的关系
Urol Int. 1994;52(4):213-6. doi: 10.1159/000282611.
8
Steroid 5 alpha-reductase: two genes/two enzymes.类固醇5α-还原酶:两个基因/两种酶。
Annu Rev Biochem. 1994;63:25-61. doi: 10.1146/annurev.bi.63.070194.000325.
9
Androgen metabolism in the human prostatic cancer cell line LNCaP.人前列腺癌细胞系LNCaP中的雄激素代谢
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Tissue distribution and ontogeny of steroid 5 alpha-reductase isozyme expression.类固醇5α-还原酶同工酶表达的组织分布及个体发生
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