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Liqing Tang¹, Yixing Xu¹, Jianglong He¹

¹School of Biotechnology, Jiangsu University of Science and Technology, Zhenjiang, Jiangsu 212100, China.

ACS medicinal chemistry letters

|November 20, 2024

概括

新型化合物C6,一种1-deoxynojirimycin衍生物,通过诱导HCT-116癌细胞中的亡,DNA损伤和线粒体功能障碍,显示出显著的抗瘤作用. 这项研究强调了C6作为癌症治疗的有希望的药物.

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:

1-deoxynojirimycin (DNJ) 衍生物正在探索其治疗潜力.
泰加 (Tegafur,TGF) 是一种抗癌前药物.
对抗增殖活性的新化合物的研究至关重要.

研究的目的:

设计和合成新的DNJ衍生物 (C4-C6).
评估C4-C6.6的抗增殖和抗瘤作用.
阐明C6对HCT-116细胞的潜在作用机制.

主要方法:

DNJ衍生物的化学合成.
在体外评估抗增殖活性.
细胞循环和细胞亡分析的流细胞计.
线粒体功能测试 (膜潜力,ROS).
对于蛋白质表达的西方涂抹 (Bax, Bcl-2, Nrf2).
酶活性测试 (SOD,GSH). 酶活性测试 (SOD,GSH). 酶活性测试 (SOD,GSH). 酶活性测试 (SOD,GSH). 酶活性测试 (SOD,GSH). 酶活性测试 (SOD,GSH). 酶活性测试 (SOD,GSH).
对DNA损伤的评估.

主要成果:

C4-C6衍生物,特别是C6,表现出良好的脂性,α-葡萄糖酶抑制和抗瘤作用.
C6诱导了显著的亡,S相停止,并抑制了HCT-116细胞的迁移.
C6引起了线粒体损伤,增加了活性氧物种 (ROS) 积累,并调节了与亡相关的蛋白质 (Bax/Bcl-2).
C6引发了氧化应激,由MDA,NO,GSH和SOD的水平变化以及Nrf2过度表达所证明.
C6诱导的DNA损伤通过降低调控甲基酸合成酶的表达.

结论:

C6是一种强大的抗瘤剂,对HCT-116细胞具有显著的抗增殖活性.
C6通过多种机制发挥其细胞毒性作用,包括DNA损伤,线粒体功能障碍和氧化应激诱导.
像C6这样的DNJ衍生物代表了癌症治疗开发的有前途的化合物类.

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