A novel near-infrared chemodosimeter to monitor the change of carboxylesterase in treatment of diabetes

Sun, Wanlu; Zhao, Chunjiang; Huang, Xiaoyan; Tan, Baojin; Shangguan, Lina; Liu, Yi; Wang, Haiyan

doi:10.1016/j.snb.2023.133416

Cited by 9 publications

(1 citation statement)

References 36 publications

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“…As shown in Figure a, noticeable fluorescence was observed in 4T1 cells, suggesting a certain level of CES expression in these cells, along with BDPN2-CES exhibiting favorable cell membrane permeability. To validate that the fluorescence enhancement stemmed from CESs, two well-known inhibitors, 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride (AEBSF, serine protease inhibitor) and bis- p -nitrophenyl phosphate (BNPP, carboxylesterases inhibitor) were utilized to reduce intracellular CES activity. As expected, the fluorescence signals were significantly blocked upon pretreatment of 4T1 cells with AEBSF and BNPP, respectively, which may be ascribed to the reduction of CES activity.…”

Section: Resultsmentioning

confidence: 99%

Rational Design of a Highly Sensitive Carboxylesterase Probe and Its Application in High-Throughput Screening for Uncovering Carboxylesterase Inhibitors

Wang,

Yan

et al. 2024

J. Org. Chem.

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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.

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Section: Resultsmentioning

confidence: 99%