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Updated: Jun 27, 2025

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协调环境的依赖性抗癌活性在循环金属化石中(III) 复合物与C,O-化联体

Jian Lei¹, Yongping Liu², Mingming Yin³

¹School of Medicine, Hunan University of Chinese Medicine, Changsha 410208, PR China; Key Laboratory of Prevention and Treatment of Cardiovascular and Cerebrovascular Disease of the Ministry of Education, Key Laboratory for Tissue Engineering of Jiangxi Province, College of Pharmacy, Gannan Medical University, Ganzhou 341000, PR China; State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, PR China.

Journal of inorganic biochemistry

|April 26, 2024

概括

新 bismuth (III) 复合物显示出强大的抗癌活性,表现优于 cisplatin. 这些化合物诱导了亡并克服了西斯普拉丁耐药性,为基于斯木的新型癌症化疗提供了有希望的基础.

科学领域:

无机化学无机化学
药用化学医学化学
材料科学材料科学材料科学

背景情况:

循环金属 bismuth ((III) 复合物正在探索治疗应用.
了解结构-活性关系对于开发有效的抗癌药物至关重要.
比斯穆特化合物为基药物 (如思丁) 提供了潜在的替代品.

研究的目的:

合成和表征新型循环金属化石 (((III) 复合物与C,O-双酸联体.
为了评估这些复合物的体外细胞毒性,与各种人类癌症细胞系和正常细胞相比.
研究作用机制和结构-活性关系,以确定它们的抗癌疗效和克服药物耐药性的潜力.

主要方法:

使用UV-vis,NMR,HRMS和单晶X射线衍射合成和表征珠 (III) 复合物.
在体外细胞毒性测定对结肠,乳腺,肺癌和胃癌细胞系以及正常的细胞.
细胞灭绝试验 (附录V-FITC/PI染色) 和西部斑点分析,以阐明细胞死亡的机制.
对抗耐思的卵巢癌细胞的疗效评估.

主要成果:

大多数合成的木 (III) 复合物表现出明显更高的抗癌活性和选择性.
结构-活动关系研究表明,协调环境影响抗癌性能.
细胞毒性是通过亡中介的,由Bcl-2下调和caspase-3激活证明.
精选的复合物证明了对抗抗西斯普拉丁抗性癌细胞的有效性,这表明了绕过抗性的机制.

结论:

与C,O-bidentate连接体结合的环金属 bismuth (III) 复合物具有优异的抗癌特性.
木复合物的协调化学与它们的细胞毒性活性之间存在着强烈的相关性.
这些发现为设计先进的基于石的化疗药物提供了基础,特别是用于克服耐药性.

关键词:

细胞灭亡 (apoptosis) 是一种死亡的过程.比斯穆特是一种石.癌症化疗癌症化疗协调环境协调环境细胞毒性细胞毒性药物耐药性药物耐药性药物耐药性

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