Detection of carboxylesterase 1 and carbamates with a novel fluorescent protein chromophore based probe.

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]