标题:Discovery of novel PC-PLC activity inhibitors
作者:Zhao Y.; Su L.; Li K.; Zhao B.
作者机构:[Zhao, Y] Jinan Hangchen Biotechnology Co., Ltd., Jinan, China;[ Su, L] State Key Laboratory of Biobased Material and Green Papermaking, School of Bio 更多
通讯作者:Su, L(sule@sdu.edu.cn)
通讯作者地址:[Su, L] State Key Laboratory of Biobased Material and Green Papermaking, School of Bioengineering, Shandong Academy of Sciences, Qilu University of Te 更多
来源:Chemical Biology and Drug Design
出版年:2019
DOI:10.1111/cbdd.13606
关键词:Bacillus cereus; PC-PLC inhibitor; R-7ABO; S-7ABO; vascular endothelial cells
摘要:Phosphatidylcholine-specific phospholipase C (PC-PLC) is one of the important members of phospholipase family which is capable of specifically hydrolyzing the third phosphate linker of glycerophospholipid molecules, releasing phosphocholine and diacylglycerols (DAG). It is a crucial virulence factor of bacteria contributed to cell-to-cell spread and leading multiple diseases in mammals. Moreover, PC-PLC has a wide range of biological functions and involves in various cell signaling pathway, including apoptosis, proliferation, differentiation, and metastasis. In this study, we have synthesized 2 chiral compounds ((R)-7-amino-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-ol, called R-7ABO, and (S)-7-amino-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-ol, called S-7ABO) and discovered their inhibitory effect on PC-PLC activity which derived from Bacillus cereus (B. cereus) and human umbilical vein endothelial cells (HUVEC). Therefore, as two novel efficient PC-PLC inhibitors, R-7ABO and S-7ABO might become favorable tools of antibacterial therapy in B. cereus infection diseases and researching the function of PC-PLC in HUVECs. © 2019 John Wiley & Sons A/S.
收录类别:SCOPUS
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85076791055&doi=10.1111%2fcbdd.13606&partnerID=40&md5=c476fa67ae8e474b26596ae2dee2a416
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