抑菌型Fischer卡宾类一氧化碳缓释分子

发布时间：2018-01-02 13:13

本文关键词：抑菌型Fischer卡宾类一氧化碳缓释分子　出处：《有机化学》2016年11期 　论文类型：期刊论文

【摘要】：过渡金属羰基化合物类一氧化碳释放分子(CORMs)的设计是当下无机化学、生物医学、材料化学等多学科交叉的热点.针对现有先导结构传输效率低、水溶性差的关键问题,发展了一类离子型Fischer卡宾类CORM先导结构([(CO)_5ML]~-)的化合物Fc-CORMs,其中五羰基卡宾阴离子单元可水解缓释一氧化碳,季铵盐阳离子有效调节CORM水溶性.肌红蛋白测试表明,每分子Fc-CORM可以在体外生理环境下至少缓释两分子CO.动力学分析显示,Fc-CORM释放速度取决于中心金属的种类,Fc-CORM-Mo(2a~2e)释放速度大于Fc-CORM-Cr(1a~1e),且远大于Fc-CORM-W(3a~3e).抗菌实验发现,中速释放分子1b可有效抑制大肠杆菌,其MIC为30μmol/L.对于具有耐药性的细菌,Fc-CORM-Mo(2b)和Fc-CORM-W(3b)表现出一定抗菌活性.机理研究证明,Fc-CORMs的抗菌活性取决于其释放CO的速度.
[Abstract]:The design of transition metal carbonyl compounds like carbon monoxide (CONCO) is a hot spot in inorganic chemistry, biomedicine, material chemistry and so on. A class of ionic Fischer carbine-like CORM leading structures were developed for the key problem of poor water solubility. [The compound Fc-Corms, in which pentacarbonyl carbene anion unit can hydrolyze and slow release carbon monoxide. Quaternary ammonium cations can effectively regulate the water solubility of CORM. The results of myoglobin test showed that each Fc-CORM could release at least two molecules in physiological environment in vitro. Kinetic analysis showed that. The release rate of Fc-CORM depends on the release rate of Fc-CorM-Mo-2a ~ (2e) of the central metal is higher than that of Fc-Corm ~ (-Cr) 1a ~ (1) e). And it was much larger than that of Fc-CorM-WN 3a 3e. The antibacterial experiment showed that 1b could effectively inhibit Escherichia coli. Its MIC was 30 渭 mol / L. It showed certain antimicrobial activity against resistant bacteria (Fc-CorM-Mo2b) and Fc-CorM-Wn3b). The antibacterial activity of Fc-CORMs depends on the rate of CO release.
【作者单位】：陕西师范大学化学化工学院;西北大学材料与化学科学学院;解放军第二军医大学上海长征医院;
【基金】：国家自然科学基金(No.21371112) 教育部博士点新教师基金(No.20120202120005) 中央高校基金(No.GK201501005) 陕西省自然科学基金(No.2012JM2006)资助项目~~
【分类号】：O621.1
【正文快照】： 一氧化碳(Carbon monoxide,CO)是一类重要气体信使分子,它可强烈结合呼吸氧化酶和球蛋白,抑制微生物呼吸作用[1,2].近期研究发现,CO是金色葡萄球菌呼吸链的有效抑制剂[3];同时,CO可增强宿主防御对于大肠杆菌的吞噬作用.CO还能够促进细胞内氢氧根自由基产生,大量活性氧物种的富

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