新型Ga(III) 聚二基甲基酸盐复合物的合成,表征和抗菌活性
Lewis More O'Ferrall1,2, Magdalena Piatek2,3, Brendan Twamley4
1School of Food Science & Environmental Health, Technological University Dublin, Dublin 7, Ireland.
Dalton transactions (Cambridge, England : 2003)
|August 14, 2023
概括
新的 ((III) 聚二甲基甲基酸盐复合物显示出强大的抗菌活性,对抗像大肠杆菌这样的格拉姆阴性病原体. 这些化合物是无毒的,并且在体内保护P. aeruginosa感染.
科学领域:
- 协调化学 协调化学
- 药用化学 医学化学
- 材料科学 材料科学 材料科学
背景情况:
- (III) 复合物正在探索治疗应用.
- 聚烯基和甲基酸盐连接体提供了多样化的协调可能性.
- 开发新型抗菌剂是全球卫生优先事项.
研究的目的:
- 合成和描述新型 (((III) 聚二甲基酸盐复合物.
- 为了评估这些复合物对病原细菌的体外抗菌疗效.
- 评估复合体对 Pseudomonas aeruginosa 感染的体内毒性和保护作用.
主要方法:
- 使用Ga(NO3) 3的Ga(III) 复合物的合成,使用catecholate连接物 (2,3-DHBA,3,4-DHBA,2,3,4-THBA,CafA) 和二平 (bipy) 或 (phen) 的合成.
- 使用X射线晶体学进行表征,以确认协调几何.
- 在体外抗菌测定对格拉姆阴性 (大肠杆菌,肺炎,P. aeruginosa) 和格拉姆阳性 (金黄色,MRSA) 细菌.
- 在感染P. aeruginosa的Galleria mellonella幼虫中进行了体内毒性和疗效研究.
主要成果:
- 成功合成和表征了Ga(III) 聚二甲基酸盐复合物.
- X射线晶体学证实了甲基酸盐连接体对Ga (III) 中心的双度协调.
- 所有复合物都表现出显著的体外抗菌活性,对抗阴性细菌.
- 复合物对包括MRSA在内的格兰美阳性细菌无活性.
- [Ga(bipy) 2(2,3-DHBA-2H) ](NO3) ·1.5H2O在高达2000μg mL-1.5的Galleria mellonella幼虫中没有显示出体内毒性.
- 这种复合物在体内提供了100和250μg mL-1的剂量对P. aeruginosa感染的保护.
结论:
- 新型Ga(III) 聚二甲基酸盐复合物具有强大的抗菌活性,可对抗关键的格拉姆阴性病原体.
- 复合体在体内表现出良好的安全性概况和对P. aeruginosa感染的治疗潜力.
- 这些发现凸显了定制的Ga(III) 复合物的潜力,作为一种新型抗菌剂.
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