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Identification and characterization of reactive metabolites in myristicin-mediated mechanism-based inhibition of CYP1A2

Aihong Yang,Xin He,Junxiu Chen,Lina He,Chunhuan Jin,Lili Wang,Fangliang Zhang,Lijun An

Chemico-Biological Interactions（2015）

Cited 29|Views2
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Abstract
It is identified that myristicin is a mechanism-based inhibitor of CYP1A2 through CYP cocktail screening, IC50 shift calculation and GSH capturing assays in HLMs. And the reactive metabolites were identified as a quinone and its tautomer through detailed analysis the cleavage processes of metabolites and GSH-myristicin adduct in phase I metabolism assays using UPLC-MS2.
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Key words
MBI,RMs,CYPs,GSH,HLMs,NADPH,MI complex
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