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首页> 外文期刊>Journal of Cellular Physiology >Pregnane glycosides interfere with steroidogenic enzymes to down-regulate corticosteroid production in human adrenocortical H295R cells
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Pregnane glycosides interfere with steroidogenic enzymes to down-regulate corticosteroid production in human adrenocortical H295R cells

机译：孕烷苷steroidogenic干扰酶抑制皮质类固醇在人体肾上腺皮质H295R细胞生产

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摘要

A group of bioactive steroidal glycosides (pregnanes) with anorectic activity in animals was isolated from several genera of milkweeds including Hoodia and Asclepias. In this study, we investigated the effects, structure-activity relationships, and mechanism of action of pregnane glycosides on steroidogenesis in human adrenocortical H295R cells. Administration of pregnane glycosides for 24h suppressed the basal and forskolin-stimulated release of androstenedione, corticosterone, and cortisone from H295R cells. The conversion of progesterone to 11-deoxycorticosterone and 17-hydroxyprogesterone to either androstenedione or 11-deoxycortisol was most strongly affected, with 12-cinnamoyl-, benzoyl-, and tigloyl-containing pregnanes showing the highest activity. Incubation of pregnane glycosides for 24h had no effect on mRNA transcripts of CYP11A1, CYP21A1, CYP11B1 cytochrome enzymes and steroidogenic acute regulatory protein (StaR) protein, yet resulted in twofold decrease in HSD3B1 mRNA levels. At the same time, pregnane glycosides had no effect on the CYP1, 2, or 3 drug and steroid metabolism enzymes and showed weak Na+/K+ ATPase and glucocorticoid receptor binding. Taken together, these data suggest that pregnane glycosides specifically suppress steroidogenesis through strong inhibition of 11??-hydroxylase and steroid 17-alpha-monooxygenase, and weak inhibition of cytochrome P450 side chain cleavage enzyme and 21??-hydroxylase, but not 3??-hydroxysteroid dehydrogenase/isomerase. J. Cell. Physiol. ? 2013 Wiley Periodicals, Inc.
机译：一群生物活性的甾体苷在动物(孕烷)厌食的活动从几个孤立的乳草属包括蝴蝶和Asclepias。调查的影响,结构活性关系和机制的作用孕烷苷在人类类固醇生成肾上腺皮质H295R细胞。孕烷苷24 h抑制基底和forskolin-stimulated释放雄烯二酮、皮质甾酮和可的松从H295R细胞。11-deoxycorticosterone和17-hydroxyprogesterone要么雄烯二酮或11-deoxycortisol最强烈的影响,12-cinnamoyl -苯甲酰-,tigloyl-containing孕烷显示最高的活动。24小时没有影响CYP11A1 mRNA转录,CYP21A1 CYP11B1细胞色素酶和steroidogenic急性监管蛋白(明星)蛋白质,还导致了双重的减少HSD3B1 mRNA水平。苷没有影响CYP1 2或3药和类固醇代谢酶和显示弱Na + / K + atp酶和糖皮质激素受体绑定。孕烷苷特别压抑类固醇生成通过强烈的抑制11 ? ?17-alpha-monooxygenase,弱的抑制细胞色素P450侧链裂解酶21 ? ?脱氢酶/异构酶。威利期刊公司。

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