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

Acta Pharmaceutica Sinica B

Shanshan Huang¹  Sa Deng²  Fei Yan²  Tian Xie³  Xiangge Tian⁴  Jingnan Cui⁵  Lei Feng⁵  Zhenhao Tian⁵  Baojing Zhang⁵  Xiaochi Ma⁶ 

[1] Corresponding authors. Tel./Fax: [phone].;Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou 221004, China;School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang 453007, China;School of Life Sciences, Northwestern Polytechnical University, Xi'an 710072, China;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;State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, China;

关键词: Vanin-1;    NIR fluorescent probe;    Kidney injury diagnosis;    Fluorescence imaging;    Oleuropein;   

DOI  :  

来源: DOAJ

【 摘 要 】

Vanin-1 is an amidohydrolase that catalyses the conversion of pantetheine into the amino-thiol 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 from herbal medicines library using a high-throughput screening method using DDAV, which held great promise for clinical therapy of inflammatory bowel disease.

【 授权许可】

Unknown