Butorphanol inhibits androgen biosynthesis and metabolism in rat immature Leydig cells in vitro.

IF 1.7 4区医学 Q3 PHARMACOLOGY & PHARMACY

Canadian journal of physiology and pharmacology Pub Date : 2024-04-01 Epub Date: 2024-01-23 DOI:10.1139/cjpp-2023-0191

Changchang Li, Lei Shi, Ming Su, Xiaoheng Li, Qiqi Zhu, Ren-Shan Ge, Huitao Li

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引用次数: 0

Abstract

Butorphanol is a synthetic opioid analgesic medication that is primarily used for the management of pain. Butorphanol may have an inhibitory effect on androgen biosynthesis and metabolism in rat immature Leydig cells. The objective of this study was to investigate the influence of butorphanol on androgen secretion by rat Leydig cells isolated from the 35-day-old male rats. Rat Leydig cells were cultured with 0.5-50 μM butorphanol for 3 h in vitro. Butorphanol at 5 and 50 μM significantly inhibited androgen secretion in immature Leydig cells. At 50 μM, butorphanol also blocked the effects of luteinizing hormone (LH) and 8bromo-cAMP-stimulated androgen secretion and 22R-hydroxycholesterol- and pregnenolone-mediated androgen production. Further analysis of the results showed that butorphanol downregulated the expression of genes involved in androgen production, including Lhcgr (LH receptor), Cyp11a1 (cholesterol side-chain cleavage enzyme), Srd5a1 (5α-reductase 1), and Akr1c14 (3α-hydroxysteroid dehydrogenase). Additionally, butorphanol directly inhibited HSD3B1 (3β-hydroxysteroid dehydrogenase 1) and SRD5A1 activity. In conclusion, butorphanol may have side effects of inhibiting androgen biosynthesis and metabolism in Leydig cells.

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布托诺啡醇可抑制体外大鼠未成熟髓质细胞中雄性激素的生物合成和代谢。

布托啡诺是一种合成阿片类镇痛药，主要用于治疗疼痛。布托诺啡醇可能对大鼠未成熟莱德细胞中雄激素的生物合成和代谢有抑制作用。本研究的目的是调查丁吗啡醇对从 35 天大的雄性大鼠体内分离出的大鼠莱德细胞分泌雄激素的影响。在体外用 0.5-50 μM 的丁吗啡醇培养大鼠 Leydig 细胞 3 小时。5 μM和50 μM的丁吗啡醇能明显抑制未成熟的Leydig细胞分泌雄激素。在 50 μM 的浓度下，丁吗啡醇还能阻止黄体生成素（LH）和 8 溴-CAMP 刺激的雄激素分泌以及 22R- 羟基胆固醇和孕烯醇酮介导的雄激素生成。对结果的进一步分析表明，丁吗啡醇下调了参与雄激素分泌的基因的表达，包括Lhcgr（LH受体）、Cyp11a1（胆固醇侧链裂解酶）、Srd5a1（5α-还原酶1）和Akr1c14（3α-羟类固醇脱氢酶）。此外，丁吗啡醇还能直接抑制 HSD3B1（3β-羟基类固醇脱氢酶 1）和 SRD5A1 的活性。总之，丁吗啡醇可能具有抑制雄性激素在莱狄格细胞中的生物合成和代谢的副作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Canadian journal of physiology and pharmacology 医学-生理学

CiteScore

4.00

自引率

4.80%

发文量

审稿时长

3-8 weeks

期刊介绍： Published since 1929, the Canadian Journal of Physiology and Pharmacology is a monthly journal that reports current research in all aspects of physiology, nutrition, pharmacology, and toxicology, contributed by recognized experts and scientists. It publishes symposium reviews and award lectures and occasionally dedicates entire issues or portions of issues to subjects of special interest to its international readership. The journal periodically publishes a “Made In Canada” special section that features invited review articles from internationally recognized scientists who have received some of their training in Canada.