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合成,细胞毒性,亡性活动,氧化应激诱导能力,以及来自甲状腺的胺素的分子相互作用

Dicle Sahin¹, Yalcin Erzurumlu², Muhammed Tilahun Muhammed³

¹Department of Pharmaceutical Research and Development, Institute of Health Sciences, Suleyman Demirel University, Isparta, Türkiye.

Journal of biochemical and molecular toxicology

|November 6, 2025

概括

基于甲基的希夫基通过诱导癌细胞死亡和氧化应激,显示出强烈的抗癌作用. 这些化合物,特别是4f和4k,向BCL-xL通路,为新的癌症治疗提供了潜力.

科学领域:

药用化学医学化学
分子生物学分子生物学
药理学药理学是指药理学的学科.

背景情况:

希夫基 (胺基) 已因其显著的抗癌潜力而得到认可.
提摩尔衍生物正在研究它们对癌细胞的细胞毒性和亡效应.

研究的目的:

合成和评估用于体外抗癌活性的基于蒂摩尔的新型希夫基.
阐明它们的细胞毒性作用背后的分子机制,包括亡诱导和氧化应激.
通过分子建模,研究与关键的亡蛋白的结合相互作用.

主要方法:

基于蒂摩尔的胺基的合成.
在体外细胞毒性测定对各种癌症细胞系.
定量实时PCR (qRT-PCR) 用于细胞亡和抗细胞亡的基因表达.
用于核形态评估的DAPI染色.
氧化应激分析.
分子对接和动力学模拟.

主要成果:

几种合成的希夫基在体外表现出强烈的细胞毒性活性,表现优于西斯和帕克利塔塞尔.
化合物4f显示了最高的细胞毒性 (IC50:4.089.94μM),其次是4k,4l和4m.
化合物上调的亲细胞亡基因 (BAX,caspase-3,BiD) 和下调的抗细胞亡基因 (BCL2,BCL-xL).
DAPI染色证实了亡形成的诱导,氧化应激水平显著增加.
分子建模表明它与BCL-xL和caspase3结合,对BCL-xL观察到稳定的相互作用和高亲和力.

结论:

以硫醇为基础的希夫基,以化合物4f和4k为例,具有显著的抗癌特性.
它们的机制包括刺激亡和增强细胞氧化应激.
这些化合物显示出作为新型抗癌剂的前景,可能准BCL-xL通路.

关键词:

模拟MD的模拟方法灭症 (apoptosis) 是一种死亡的过程.细胞毒性细胞毒性它们是无限的,无限的.分子对接的分子对接.蒂莫尔 (thymol) 是一种蛋白质.

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