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氨酸衍生替代双A,具有潜在的不可检测的雌激素活性和最小的发育毒性

Xinwen Zhang¹, Jignesh S Mahajan², Jinglin Zhang¹

¹Department of Animal and Food Sciences, University of Delaware, Newark, DE, 19716, USA.

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

|June 5, 2024

概括

与双甲相比,像比西林戈尔A这样的 Lignin衍生双醇显示了最小的雌激素活性和发育毒性.这些化合物的甲基替代物减少了雌激素反应,提供了更安全的替代品.

科学领域:

绿色化学绿色化学
毒理学毒理学毒理学
内分泌学在内分泌学.

背景情况:

商业双,包括双A (BPA) 和双F (BPF),是内分泌干扰剂.
素衍生 bisguaiacols/bissyringols 是潜在的替代品,但与 BPA/BPF 的结构相似性引起了人们的关注.
一些素衍生双中未被替代的桥梁碳增加了与BPA/BPF的结构相似性.

研究的目的:

调查二甲基替代桥梁碳基红素衍生双醇 (bisguaiacol A [BGA]和bissyringol A [BSA]) 的雌激素活性 (EA) 和发育毒性.
为了比较BGA和BSA与BPA和BPF的安全概况.
评估甲基替代剂对由素衍生的双醇EA的影响.

主要方法:

在体外MCF-7细胞增殖试验以评估EA.
在基分子对接中预测与雌激素受体的结合亲和力.
在体内胚胎测定以评估发育性毒性.
在胎肝中的基因表达分析 (阿波利波蛋白II).

主要成果:

比西林戈A (BSA) 在七种度 (10-12M) 中表现出不可检测的EA,与BPA不同 (可检测的EA在10-10M).
在分析显示,BSA对雌激素受体的结合亲和力最低.
与BPA相比,在环境相关度下,宁衍生单体显示出最小的发育毒性.
雌激素反应基因 (apolipoprotein II) 表达在胎肝中显着较低,用于素衍生化合物 (折叠变化~1.814.41) 与BPA (折叠变化~11.51).

结论:

用二甲基替代的素衍生双,特别是BSA,是商业双的更安全替代品,因为EA和发育毒性显著降低.
甲基替代物在素衍生双上对于减轻雌激素活性至关重要.
这些发现支持开发以素为基础的化学品,作为对内分泌干扰双醇的可持续和更安全的替代品.

关键词:

基于生物的生物制品.双甲替代品的替代品的胚胎是一个胚胎.发展性毒性发展性毒性雌激素活性雌激素活性素衍生性的可用性.

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