【摘 要】
：
Human carboxylesterase 1 (hCE-1) are a representative B-esterase, involved in the hydrolysis of many endogenous and exogenous compounds and are thus responsible for the activation of many prodrugs.Dys
【机 构】
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Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Dalian 116023
【出 处】
：
2015年第一届药代动力学朝阳论坛
论文部分内容阅读
Human carboxylesterase 1 (hCE-1) are a representative B-esterase, involved in the hydrolysis of many endogenous and exogenous compounds and are thus responsible for the activation of many prodrugs.Dysfunction of hCE-1 in body has been proved to be related to many diseases, such as atherosclerosis, obesity, hepatic steatosis, hyperlipidemia, and hepatocellular carcinoma.In our previous work, we found N-(4-methyl butyrate)-4-hydroxy-l,8-naphthalimide (NMHN) could be rapidly deesterified by esterases to (3-carboxy propyl)-4-hydroxy-1, 8-naphthalimide (NCHN), which is a highly selective fluorescent probe for human UDP-glucuronosyltransferase 1A1.This elicits our interest in identifying which esterase is responsible for the hydrolysis of NMHN.In the present study, the hydrolysis pathway (s) of NMHN was investigated by using pooled human liver microsome (HLM) and various species of recombinant enzymes with hydrolytic activity.
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