针对线粒体的中性和阴离子 (III) 抗癌复合物化简单的混合体 sp2 - N/sp3 - N 供体配体
Pengwei Li1, Lihua Guo1, 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, Institute of Anticancer Agents Development and Theranostic Application, School of Chemistry and Chemical Engineering, Qufu Normal University, Qufu 273165, P. R. China. guolihua@qfnu.edu.cn.
Dalton transactions (Cambridge, England : 2003)
|January 11, 2024
概括
新的 (III) 复合物通过向线粒体和诱导氧化应激,表现出抗癌活性. 虽然对癌细胞有效,但它们对正常细胞的选择性需要改善,以便进行治疗.
科学领域:
- 无机化学 无机化学 有机化学
- 药用化学 医学化学
- 癌症研究 癌症研究
背景情况:
- 环金属化 (III) 复合物具有发光和抗癌性质.
- 氨基 - 氨基联体被用于合成新型的 (III) 抗癌剂.
研究的目的:
- 合成和表征中性和阴阳性 (III) 复合物.
- 评估它们的抗癌活性,细胞机制和选择性.
主要方法:
- 使用希夫基联结体合成 (III) 复合物.
- 使用各种分析技术进行表征.
- 在体外细胞毒性测试对多个癌细胞系和正常细胞进行检测.
- 线粒体功能,ROS生产和细胞周期分析.
主要成果:
- 合成了具有中度光和BSA亲和力的稳定(III) 复合物.
- 对A549,A549/DDP,HeLa和HepG2细胞具有有前途的细胞毒性 (IC50:9.9819.63μM).
- 癌细胞和正常细胞之间的选择性较低 (选择性指数:1.621.98).
- 线粒体向,膜去极化,ROS生成,晚期亡和细胞周期扰乱 (G2/M或S阶段).
结论:
- 合成的 (III) 复合物表现出强大的抗癌活性.
- 涉及线粒体功能障碍和ROS产生的还氧化机制是它们有效性的关键.
- 需要进一步优化,以提高临床应用的选择性.
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