结合释放一氧化碳的分子具有广泛的抗微生物活性
Sofia S Mendes1, Moritz Sorg1, Cláudia Malta Luís1
1Instituto de Tecnologia Química e Biológica António Xavier, Universidade Nova de Lisboa, Avenida da República (EAN), 2780-157, Oeiras, Portugal.
Future medicinal chemistry
|July 17, 2023
概括
与醇结合的一氧化碳释放分子 (CORM) 显示出广泛的抗菌潜力. 新型化合物ReBpyCtz有效地向低毒性的细菌,真菌和疟疾寄生虫.
科学领域:
- 药用化学 医学化学
- 微生物学 微生物学
- 寄生虫学的寄生虫学
背景情况:
- 抗菌素耐药性需要新的治疗策略.
- 一氧化碳释放分子 (CORM) 具有作为抗菌剂的潜力.
- 醇化合物是已确定的抗微生物药物.
研究的目的:
- 为了评估与醇结合的CORM的抗菌疗效.
- 为了研究一种特定的结合物的作用机制,ReBpyCtz.
- 评估ReBpyCtz. 的安全性.
主要方法:
- 汁微稀释和棋盘测试用于确定最小抑制度.
- 细胞毒性测试用于评估宿主细胞的安全性.
- 显微镜和光技术用于研究细胞效应和反应性氧物种的产生.
主要成果:
- ReBpyCtz对*黄金葡萄球菌*表现出强烈的活性,诱导膜损伤和增加活性氧物种.
- 该化合物对*Candida glabrata*表现出显著的杀菌活性,持续时间超过了克洛特里马.
- 在对脏上皮细胞的无毒度下,ReBpyCtz对血液阶段的疟疾寄生虫具有选择性活性.
结论:
- 将CORM与醇结合在一起,创造了一个有前途的广谱抗菌剂类.
- ReBpyCtz代表了对细菌,真菌和寄生虫感染的潜在治疗候选者.
- 这种方法为开发新抗微生物药物以打击耐药性提供了一种新的策略.
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