A NIR fluorescent probe for Vanin-1 and its applications in imaging, kidney injury diagnosis,and the development of inhibitor  

作　　者：Zhenhao Tian Fei Yan Xiangge Tian Lei Feng Jingnan Cui Sa Deng Baojing Zhang Tian Xie Shanshan Huang Xiaochi Ma 

机构地区：[1]Dalian Key Laboratory of Metabolic Target Characterization and Traditional Chinese Medicine Intervention,The Second Affiliated Hospital,College of Integrative Medicine,College of Pharmacy,Dalian Medical University,Dalian 116044,China [2]Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy,Xuzhou Medical University,Xuzhou 221004,China [3]School of Life Sciences,Northwestern Polytechnical University,Xi'an 710072,China [4]School of Chemistry and Chemical Engineering,Henan Normal University,Xinxiang 453007,China [5]State Key Laboratory of Fine Chemicals,Dalian University of Technology,Dalian 116024,China [6]College of Pharmacy,Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines,Hangzhou Normal University,Hangzhou 311121,China

出　　处：《Acta Pharmaceutica Sinica B》2022年第1期316-325,共10页药学学报（英文版）

基　　金：financially supported by National Natural Science Foundation of China(Nos.81930112 and 82004211);State Key Laboratory of Fine Chemicals KF1912,Distinguished professor of Liaoning Province,Dalian Science and Technology Leading Talents Project(2019RD15,China);the Open Research Fund of the School of Chemistry and Chemical Engineering,Henan Normal University(2021YB07)。

摘　　要：Vanin-1 is an amidohydrolase that catalyses the conversion of pantetheine into the aminothiol cysteamine and pantothenic acid(coenzyme A precursor), which plays a vital role in multiple physiological and pathological processes. In this study, an enzyme-activated near-infrared(NIR) fluorescent probe(DDAV) has been constructed for sensitively detecting Vanin-1 activity in complicated biosamples on the basis of its catalytic characteristics. DDAV exhibited a high selectivity and sensitivity toward Vanin-1 and was successfully applied to the early diagnosis of kidney injury in cisplatin-induced kidney injury model. In addition, DDAV could serve as a visual tool for in situ imaging endogenous Vanin-1 in vivo. More importantly, Enterococcus faecalis 20247 which possessed high expression of Vanin-1 was screened out from intestinal bacteria using DDAV, provided useful guidance for the rational use of NSAIDs in clinic. Finally, oleuropein as a potent natural inhibitor for Vanin-1 was discovered fromherbal medicines library using a high-throughput screening method using DDAV, which held great promise for clinical therapy of inflammatory bowel disease.

关 键 词：Vanin-1 NIR fluorescent probe Kidney injury diagnosis Fluorescence imaging OLEUROPEIN 

分 类 号：R914[医药卫生—药物化学]