含有克洛特里马作为强大的可光激活的选择性抗真菌剂的ru-terpyridine复合物
Carlos Gonzalo-Navarro1, Antonio J Troyano1, Beatriz García-Béjar Bermejo2
1Departamento de Química Inorgánica, Orgánica y Bioquímica, Facultad de Ciencias y Tecnologías Químicas, Avda. C. J. Cela, 10, UCLM, Ciudad Real, Spain.
Journal of inorganic biochemistry
|August 16, 2024
概括
新型复合物与克洛特里马显示强大的光活性抗真菌活性对酵母. 这种由光触发的药物输送系统提供了一种有前途的策略来打击抗菌素耐药性.
科学领域:
- 协调化学 协调化学
- 摄影化学的使用.
- 抗微生物耐药性 抗微生物耐药性
背景情况:
- 抗菌素耐药性是一个重大的全球健康问题.
- 过渡金属复合物具有作为光激活药物递送系统的潜力.
- 具有可光激活性质的鲁复合物被探索以克服电阻.
研究的目的:
- 合成Ru复合物与特皮里丁配体和克洛特里马.
- 评估合成复合物的光活性抗真菌活性.
- 研究替代剂对特皮里丁配体的影响.
主要方法:
- -特皮里丁-克洛特里马复合物的合成.
- 在可见光辐射下进行光解离研究.
- 对三种酵母菌种进行抗真菌活性测试.
- 用TD-DFT计算来解释替代物效应.
主要成果:
- 复合物在可见光照射后成功地输送了克洛特里马.
- 一种含有碳基替代物的复合物表现出优异的抗真菌活性.
- 最低抑制度 (MIC) 为0.88μM,光毒性指数 (PTI) 为50的最佳复合体.
- 活性明显高于自由克洛特里马,特别是在光下 (141x).
结论:
- 复合物与克洛特里马是有效的光活性抗真菌剂.
- 替代剂对特皮里丁配体的修饰会影响光解离和活性.
- 这种方法是对抗耐药真菌感染的可行策略.
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