| Autor: |
Wang K; College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325035, P. R. China., Wang R; College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325035, P. R. China., Yan Z; School of Pharmacy, Changzhou University, Changzhou 213164, P. R. China., Li Y; School of Pharmacy, Changzhou University, Changzhou 213164, P. R. China., Shi Y; College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325035, P. R. China., Ge JY; College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325035, P. R. China., Bai Y; School of Pharmacy, Changzhou University, Changzhou 213164, P. R. China., Chen Z; College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325035, P. R. China.; Key Lab of Biohealth Materials and Chemistry of Wenzhou, Wenzhou University, Wenzhou 325035, P. R. China., Zhang L; Department of Infectious Diseases, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou 325035, P. R. China. |
| Abstrakt: |
Tracking carboxylesterases (CESs) through noninvasive and dynamic imaging is of great significance for diagnosing and treating CES-related metabolic diseases. Herein, three BODIPY-based fluorescent probes with a pyridine unit quaternarized via an acetoxybenzyl group were designed and synthesized to detect CESs based on the photoinduced electron transfer process. Notably, among these probes, BDPN2-CES exhibited a remarkable 182-fold fluorescence enhancement for CESs within 10 min. Moreover, BDPN2-CES successfully enabled real-time imaging of endogenous CES variations in living cells. Using BDPN2-CES, a visual high-throughput screening method for CES inhibitors was established, culminating in the discovery of an efficient inhibitor, WZU-13, sourced from a chemical library. These findings suggest that BDPN2-CES could provide a new avenue for diagnosing CES-related diseases, and WZU-13 emerges as a promising therapeutic candidate for CES-overexpression pathological processes. |
