【摘 要】
：
Catechol-O-methyltransferase (COMT) plays a central role in the metabolic inactivation of endogenous catechols including catecholic neurotransmitters and es
【机 构】
：
Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics,Chinese Academ
【出 处】
：
2015年第一届药代动力学朝阳论坛
论文部分内容阅读
Catechol-O-methyltransferase (COMT) plays a central role in the metabolic inactivation of endogenous catechols including catecholic neurotransmitters and estrogens as well as catecholic medicines, such as levodopa.Either the meta or para hydroxyl functions of catechol substrates can be methylation and the ratio of meta/para O-methylation ranged from 4 to 15, varying with the nature of the catechol substituent and the experimental conditions.In the present study, we performed the methylation of 7,8-dihydroxyeoumarins (7,8-DHCs) by using human liver cytosol and recombinant S-COMT in vitro and a computing model of COMT was constructed to verify the results by docking of 7,8-DHCs to COMT.A single mono-methyl conjugate was detected by liquid chromatography/mass spectrometry (LC-MS), when each of 7,8-DHC, 4-methyl-7,8-DHC, 4-phenyl-7,8-DHC and 4-acetic acid-7,8-DHC was incubated with human liver cytosol (HLC) in the presence of S-adenosyl-methionine (SAM).
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