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苯并呋喃喹啉鎓衍生物作为新型强效抗菌剂的研究及其靶向FtsZ的抑制模式

Study of Benzofuroquinolinium Derivatives as a New Class of Potent Antibacterial Agent and the Mode of Inhibition Targeting FtsZ.

作者信息

Zheng Yuan-Yuan, Du Ruo-Lan, Cai Sen-Yuan, Liu Zhi-Hua, Fang Zhi-Yuan, Liu Ting, So Lok-Yan, Lu Yu-Jing, Sun Ning, Wong Kwok-Yin

机构信息

Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guangdong University of Technology, Guangzhou, China.

Department of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong.

出版信息

Front Microbiol. 2018 Aug 17;9:1937. doi: 10.3389/fmicb.2018.01937. eCollection 2018.

DOI:10.3389/fmicb.2018.01937
PMID:30174667
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6107709/
Abstract

New generation of antibacterial agents are urgently needed in order to fight the emergence of multidrug-resistant bacteria. FtsZ is currently identified as a promising target for new types of antimicrobial compounds development because of its conservative characteristics and its essential role played in bacterial cell division. In the present study, the antibacterial activity of a series of benzofuroquinolinium derivatives was investigated. The results show that the compounds possess potent antibacterial activity against drug resistant pathogens including MRSA, VREF and NDM-1 . Biological studies reveal that the compound is an effective inhibitor that is able to suppress FtsZ polymerization and GTPase activity and thus stopping the cell division and causing cell death. More importantly, this series of compounds shows low cytotoxicity on mammalian cells and therefore they could be new chemotypes for the development of new antibacterial agents targeting the cell-division protein FtsZ.

摘要

为应对多重耐药菌的出现，迫切需要新一代抗菌剂。FtsZ因其保守特性及其在细菌细胞分裂中发挥的关键作用，目前被确定为新型抗菌化合物开发的一个有前景的靶点。在本研究中，对一系列苯并呋喃喹啉鎓衍生物的抗菌活性进行了研究。结果表明，这些化合物对包括耐甲氧西林金黄色葡萄球菌（MRSA）、耐万古霉素肠球菌（VREF）和NDM-1在内的耐药病原体具有强大的抗菌活性。生物学研究表明，该化合物是一种有效的抑制剂，能够抑制FtsZ聚合和GTP酶活性，从而阻止细胞分裂并导致细胞死亡。更重要的是，这一系列化合物对哺乳动物细胞显示出低细胞毒性，因此它们可能是针对细胞分裂蛋白FtsZ开发新型抗菌剂的新化学类型。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/375de6eb1e32/fmicb-09-01937-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/80436400c933/fmicb-09-01937-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/cfcd0e5aaa92/fmicb-09-01937-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/2084ac79741b/fmicb-09-01937-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/8d3a77f8e1ba/fmicb-09-01937-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/cfb814dd0ed0/fmicb-09-01937-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/361172b2a390/fmicb-09-01937-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/6cb59ecd8759/fmicb-09-01937-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/28ab51cce885/fmicb-09-01937-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/375de6eb1e32/fmicb-09-01937-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/80436400c933/fmicb-09-01937-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/cfcd0e5aaa92/fmicb-09-01937-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/2084ac79741b/fmicb-09-01937-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/8d3a77f8e1ba/fmicb-09-01937-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/cfb814dd0ed0/fmicb-09-01937-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/361172b2a390/fmicb-09-01937-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/6cb59ecd8759/fmicb-09-01937-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/28ab51cce885/fmicb-09-01937-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4a6/6107709/375de6eb1e32/fmicb-09-01937-g009.jpg

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