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基双甲衍生物强烈抑制人类,老鼠和小鼠的淋巴腺3β-基固醇脱酶:结构-活性关系和在基分子对接分析

Yang Yu¹, Mengyun Wang², Ya Chen³

¹Key Laboratory of Anesthesiology of Zhejiang Province, Wenzhou Medical University, China; Department of Anesthesiology and Perioperative Medicine, The Second Affiliated Hospital and Yuying Children's Hospital；Key Laboratory of Pediatric Anesthesiology, Ministry of Education, Wenzhou Medical University, China; Key Laboratory of Environment and Male Reproductive Medicine of Wenzhou, and Key Laboratory of Structural Malformations in Children of Zhejiang Province, Wenzhou 325000 Zhejiang Province, China.

Toxicology letters

|September 8, 2023

概括

基双甲基 (BPA) 衍生物在人类,老鼠和小鼠中强烈抑制3β-基类固醇脱酶 (3β-HSD),影响类固醇生成. 这种结构依赖的抑制表明可能存在类固醇激素缺乏症.

科学领域:

环境化学环境化学
内分泌学在内分泌学.
毒理学毒理学毒理学

背景情况:

双A (BPA) 是一种无处不在的增塑剂;其基衍生物可以通过合成或环境过程形成.
基双对类固醇生成的影响,特别是对3β-基类固醇脱酶 (3β-HSDs) 等关键酶的抑制,尚不清楚.
了解这些影响对于评估潜在的内分泌干扰和与环境污染物相关的健康风险至关重要.

研究的目的:

为了比较六种双甲衍生物对三种物种:人类,老鼠和小鼠的淋巴体3β-HSDs的抑制作用.
阐明不同化BPA衍生物的抑制机制 (竞争性,非竞争性或混合).
为了研究化BPA衍生物之间的结构-活性关系,以及它们在抑制3β-HSD活性方面的功效.

主要方法:

进行了酶抑制试验,以确定各种双甲衍生物的IC50值,以对抗人类,老鼠和小鼠的3β-HSD.
动力分析被用来描述特定衍生品所施加的抑制类型.
用分子对接模拟来预测3β-HSD酶活性位点内的基BPA衍生物的结合相互作用.

主要成果:

与非替代BPA相比,化双甲衍生物对3β-HSDs具有显著更大的抑制作用.
甲BPA (TBBPA) 对人类3β-HSD2表现出强烈的非竞争性抑制,而其他衍生品则表现出竞争性或混合性抑制.
分子对接显示,强大的抑制剂如TBBPA,三BPA (TrCBPA) 和四BPA (TCBPA) 与酶活性位点中的关键残留物相互作用,与观察到的抑制常数 (Ki) 相对应.

结论:

基双甲衍生物比BPA更有效地抑制人类,老鼠和小鼠的3β-HSDs.
抑制依赖于化BPA衍生物的结构,表明有明确的结构-活性关系.
这些发现凸显了化双的潜力,包括在水化过程中形成的双,可以破坏类固醇激素的产生,导致缺乏.

关键词:

3β-基类固醇脱酶.作用方式作用方式孕产妇使用的孕.孕激素 (Progesterone) 是一种激素.类固醇激素类激素的使用

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