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亚类杀菌剂抑制人类和老鼠的淋巴腺3β-基固醇脱酶:结构-活性关系和in silico对接分析

Jianmin Sang¹, Hong Wang¹, Yang Yu¹

¹Department of Anaesthesiology, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325027, China.

Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association

|September 13, 2023

概括

在农业中使用的醇杀菌剂可以通过抑制3β-基固醇脱酶 (3β-HSDs) 等关键酶来破坏生殖健康. 迪芬可纳是一种强大的抑制剂,影响孕激素分泌.

科学领域:

内分泌学在内分泌学.
毒理学毒理学毒理学
农业科学农业科学

背景情况:

醇杀菌剂对于作物防治真菌病至关重要.
新出现的证据表明,酸杀菌剂的潜在内分泌干扰作用.
具体来说,已经观察到淋巴体3β-基固醇脱酶 (3β-HSDs) 的抑制.

研究的目的:

研究各种醇杀菌剂对3β-HSD酶的抑制作用.
确定杀菌剂特性与它们的抑制作用之间的关系.
评估醇杀菌剂对生殖细胞中类固醇激素产生的影响.

主要方法:

选16种醇杀菌剂,以抑制人类3β-HSD2和大鼠3β-HSD1.
在人类KGN细胞中测量孕激素分泌.
药分析和分子对接,以了解抑制机制.
抑制强度与物理化学特性如脂性 (LogP) 的相关性分析.

主要成果:

八种醇杀菌剂抑制了人类的3β-HSD2 (IC50 < 100μM),其中二可纳是最强的 (IC50 = 1.88μM).
三种醇杀菌剂对大鼠3β-HSD1.1的抑制作用较弱.
醇杀菌剂在度≥5μM时显著降低了KGN细胞中的孕激素分泌.
抑制功效与脂友性,分子量,pKa和结合能相关,其中一个关键的药特征是键受体-脂质组.

结论:

亚类杀菌剂对淋巴腺3β-HSDs,特别是3β-HSD2.的强烈抑制.
这些对类固醇生成的影响表明,可能对生殖健康产生不良影响.
杀菌剂的脂性和分子结构是3β-HSD抑制活性的关键决定因素.

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