有效的半三明治16-18电子 (III) 和 (II) 抗癌复合物与随时可用的氨基-氨基联体
Lihua Guo1, Pengwei Li1, Jiaxing Li1
1Key Laboratory of Life-Organic Analysis of Shandong Province, Key Laboratory of Green Natural Products and Pharmaceutical Intermediates in Colleges and Universities of Shandong Province, School of Chemistry and Chemical Engineering, Qufu Normal University, Qufu 273165, P. R. China.
Inorganic chemistry
|December 14, 2023
概括
新的和半三明治复合物显示出强大的抗癌活性. 这些金属复合体向线粒体,诱导细胞死亡,并对癌细胞表现出选择性,提供了一个有前途的氧化还原驱动治疗策略.
科学领域:
- 有机金属化学 有机金属化学
- 药用无机化学 药用无机化学
- 癌症生物学 癌症生物学
背景情况:
- 稳定的16电子半三明治复合体是罕见的,并且在治疗应用中未得到充分探索.
- 氨基-氨基联体为金属复合体提供了多功能协调模式.
- (III) 和 (II) 复合物由于其潜在的生物活性而引起人们的兴趣.
研究的目的:
- 合成和表征新的16电子和18电子半三明治复合体.
- 评估这些复合物的体内细胞毒性和选择性,针对各种癌症细胞系.
- 阐明其抗癌作用背后的作用机制.
主要方法:
- 使用氨基-氨基联体合成和表征 (III) 和 (II) 复合物.
- 在体外细胞毒性测定对A549,A549/DPP,HeLa和HepG2癌细胞以及BEAS-2B正常细胞.
- 线粒体功能测试 (膜潜力,ROS生成),亡诱导和细胞周期分析.
主要成果:
- 成功合成了具有16电子的Ir (III) 和18电子的Ru (II) 复合体,具有多种不同的对抗离子.
- 显示出有前途的细胞毒性 (IC50:5.416.3μM) 和对测试癌细胞的选择性 (SI:2.13.7).
- 证明了线粒体向,ROS生成,亡诱导和G0/G1细胞周期停止.
结论:
- 合成的半三明治和复合物具有显著的抗癌潜力.
- 它们的有效性主要是由涉及线粒体功能障碍和亡的氧化还原机制驱动的.
- 金属中心,协调模式和带变异对观察到的细胞毒性和选择性影响最小.
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