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
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.