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抗雄激素非那雄胺对米诺环素作用下人牙龈成纤维细胞中5α-还原酶活性的影响。

Effects of the anti-androgen finasteride on 5alpha-reductase activity in human gingival fibroblasts in response to minocycline.

作者信息

Soory M, Virdi H

机构信息

Department of Periodontology, King's College School of Medicine & Dentistry, London, United Kingdom.

出版信息

J Clin Periodontol. 1998 Jan;25(1):67-73. doi: 10.1111/j.1600-051x.1998.tb02365.x.

Abstract

In addition to their antimicrobial properties, tetracyclines have antiinflammatory and pro-anabolic effects on the reparatory potential of connective tissue and bone. The physiologically active androgen 5alpha-dihydrotestosterone (DHT) implicated in matrix synthesis is formed in gingivae from androgen substrates. The aim of this investigation is to study the androgen metabolic response of gingivae to minocycline, in the presence or absence of the anti-androgen finasteride. Chronically inflamed gingival tissue derived from 12 subjects aged 30-50 years and passaged fibroblasts derived from this source, were used for the experiments. Duplicate incubations were performed in Eagle's MEM with 14C-testosterone/14C-4-androstenedione in the presence or absence of minocycline (5-60 microg/ml) or finasteride for 24 h. The androgen substrate 14C-testosterone was metabolised mainly to DHT and 4-androstenedione, while 14C-4-androstenedione was converted mainly to DHT and testosterone. Minocycline at 20-30 microg/ml stimulated the formation of these metabolites from both substrates by 13-25%. In the tissue incubations there were 3- and 2-fold increases in DHT and 4-androstenedione formation (n=12; p<0.01). The anti-androgen finasteride caused significant inhibition of 5alpha-reductase activity on both substrates at 0.1 & 1.0 microg/ml with total inhibition at 10 & 50 microg/ml (n=3; p<0.01). Minocycline-induced stimulation of 5alpha-reductase activity was also inhibited by finasteride (n=4; p<0.02). Since finasteride inhibition of 5alpha-reductase activity is specific for the type 2 isoenzyme associated with anabolic functions of target tissue, this enzyme activity may contribute to some of the cited anabolic tissue responses to minocycline.

摘要

除了具有抗菌特性外,四环素对结缔组织和骨骼的修复潜能还具有抗炎和促合成代谢作用。参与基质合成的生理活性雄激素5α-二氢睾酮(DHT)由雄激素底物在牙龈中形成。本研究的目的是研究在有或没有抗雄激素非那雄胺的情况下,牙龈对米诺环素的雄激素代谢反应。实验使用了来自12名30 - 50岁受试者的慢性炎症牙龈组织以及由此来源传代的成纤维细胞。在含有14C - 睾酮/14C - 4 - 雄烯二酮的伊格尔氏MEM培养基中,在有或没有米诺环素(5 - 60微克/毫升)或非那雄胺的情况下进行重复孵育24小时。雄激素底物14C - 睾酮主要代谢为DHT和4 - 雄烯二酮,而14C - 4 - 雄烯二酮主要转化为DHT和睾酮。20 - 30微克/毫升的米诺环素刺激这两种底物形成这些代谢物的量增加了13% - 25%。在组织孵育中,DHT和4 - 雄烯二酮的形成分别增加了3倍和2倍(n = 12;p < 0.01)。抗雄激素非那雄胺在0.1和1.0微克/毫升时对两种底物的5α - 还原酶活性均有显著抑制作用,在10和50微克/毫升时完全抑制(n = 3;p < 0.01)。非那雄胺也抑制了米诺环素诱导的5α - 还原酶活性刺激(n = 4;p < 0.02)。由于非那雄胺对5α - 还原酶活性的抑制作用对与靶组织合成代谢功能相关的2型同工酶具有特异性,这种酶活性可能有助于解释上述一些关于米诺环素的组织合成代谢反应。

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