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发现一种八面体硅配合物作为一种强效抗真菌剂。

Discovery of an Octahedral Silicon Complex as a Potent Antifungal Agent.

作者信息

Fu Chen, Fu Bin, Peng Xixi, Liao Guojian

机构信息

College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China.

出版信息

Molecules. 2017 Apr 15;22(4):637. doi: 10.3390/molecules22040637.

Abstract

Octahedral transition metal complexes have been shown to have tremendous applications in chemical biology and medicinal chemistry. Meanwhile, structural transition metals can be replaced by inert octahedral silicon in a proof-of-principle study. We here introduce the first example of octahedral silicon complexes, which can very well serve as an efficient antimicrobial agent. The typical silicon arenediolate complex {(phen)₂Si(OO)₂, with phen = 1,10-phenanthroline, OO = 9,10-phenanthrenediolate} exhibited significant inhibition towards the growth of with MIC and MFC values of 4.5 and 11.3 μM, respectively. Moreover, it was fungicidal against both proliferative and quiescent Cryptococcus cells. This work may set the stage for the development of novel antifungal drugs based upon hexacoodinate silicon scaffolds.

摘要

八面体过渡金属配合物已被证明在化学生物学和药物化学中具有巨大的应用。同时,在一项原理验证研究中,结构过渡金属可以被惰性八面体硅取代。我们在此介绍八面体硅配合物的首个实例,其可很好地用作高效抗菌剂。典型的硅芳二醇盐配合物{(phen)₂Si(OO)₂,其中phen = 1,10 - 菲咯啉,OO = 9,10 - 菲二酚盐}对[具体微生物名称未给出]的生长表现出显著抑制作用,其MIC(最低抑菌浓度)和MFC(最低杀菌浓度)值分别为4.5 μM和11.3 μM。此外,它对增殖型和静止型隐球菌细胞均具有杀菌作用。这项工作可能为基于六配位硅支架开发新型抗真菌药物奠定基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c23/6154614/b4007a426aa0/molecules-22-00637-g001.jpg

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