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An aggregation-induced emission (AIE) fluorescent protein chromophore-based probe (CBZ-FP) for detection of human carboxylesterases (CESs) was designed and synthesized. CBZ-FP exhibited good cell permeability with a large stokes shift (116 nm) and can be applied to reveal the actual activities of CES1 in living cells associated with pesticides detoxification process. CBZ-FP can also serve as a fluorescence indicator of pesticide exposure in the way of hydrolyzing the carboxylic acid ester group in CBZ-FP. Therefore, CBZ-FP has high selectivity for CESs and can detect real-time activity of CES1 in biological samples. Molecular docking study was used to explore the binding of CESs and CBZ-FP. Finding that only one specific activity site of CESs can bind with probe. In view of the fact that, the biotransformation of drugs and poisons containing ester groups can carry out normally depending on CESs, Carboxylesterase probes are expected to contribute to the characterization of relevant disease. [Display omitted] • An aggregation-induced emission (AIE) fluorescent protein chromophore-based probe (CBZ-FP) for detection of human carboxylesterase 1 (CES1) as well as pesticide residue carbaryl was designed and synthesized. • CES1 and carbaryl can be quantitatively determined by CBZ-FP, which is believed due to hydrolyzing the carboxylic acid ester group in CBZ-FP by CES1. • CBZ-FP further exhibits good cell permeability as well as good tolerance towards wide pH variations, and can be applied to monitor the real activities of CES1 in living cells. • Molecular docking study shows that only one specific activity site of CES1 can bind with probe before and after hydrolysis. [ABSTRACT FROM AUTHOR]

Herein, a lysosomal targeting LysFP@ZIF-8 metal-organic framework (MOF) was fabricated using fluorescent protein chromophore-based probe (LysFP) for selectively detection of carboxylesterase 1 (CES1) in living cells. Unlike the regular small molecule fluorescent probes, LysFP@ZIF-8 showed wide range pH tolerabiligy, high selectivity and sensitivity to CES1 in bio-samples, and was successfully applied to achieve the visual monitoring of CES1 activity in living cells. Low detection limit and high fluorescence quantum yield was calculated as 79 ng/mL and 0.76 for LysFP@ZIF-8, respectively. Furthermore, LysFP@ZIF-8 can also serve as a fluorescence indicator of organophosphates pesticide exposure in the way of hydrolyzing the carboxylic acid ester group in LysFP. This type of probe can inspire the development of fluorescent tools for further explore many pathological processes. ga1 • A LysFP@ZIF-8 metal-organic framework (MOF) was fabricated for selectively detection of carboxylesterase 1 (CES1). • LysFP@ZIF-8 with lysosome labeling ability and can be used for monitoring CES1 activities in living cells. • LysFP@ZIF-8 was successfully applied to the quantitative detection of endogenous and exogenous carboxylesterase 1. • LysFP@ZIF-8 has been successfully used as an effective tool in pesticide residue detection. [ABSTRACT FROM AUTHOR]

Designing fluorescent probe for detecting carboxylesterase 1 is remains challenging. Herein, a red emission human carboxylesterase 1 (CES1) probe (CAE-FP) was synthesized based on fluorescent protein chromophore. Probe CAE-FP can specific detect human CES1 with high selectively. The fluorescence quantum yield was calucated as 0.19. The carboxylic acid ester in CAE-FP could be easily hydrolyzed by CES1 under physiological conditions, and this process could induce the obvious fluorescence signal in red emission region. The detection limit of CES1 was calculated as 84.5 ng/mL. Due to the biological detoxification mechanism of carboxylesterase and the obvious inhibitory effect of pesticides on its activity, CAE-FP was applied to detect carbamate pesticide and have achieved good application results. Since fluorescent protein chromophore has excellent biocompatibility, probe CAE-FP with good cell membrane permeable and was successfully applied to monitor the real activities of CES1 in living cells. In summary, this is one of the few reported fluorescent probes that can specific detect the real-time activity of CES1 in biological samples. Besides, we first applied the fluorescent protein chromophore to construct the specific target enzyme probe. This work would contribute to further investigate CES1-associated physiological and pathological processe. Image 1 • A red emission carboxylesterase 1 (CES1) probe (CAE-FP) was developed based on fluorescent protein chromophore. • CAE-FP could selectively detect CES1 from other hydrolytic esterases with fluorescence enhancement phenomenon. • CAE-FP exhibits a good linear relationship with the concentrations of CES1 and carbaryl, from which CAE-FP could quantitatively detect CES1 and carbaryl. • CAE-FP could monitor the real-time activities of CES1 in biological samples. [ABSTRACT FROM AUTHOR]