BACKGROUND: Descurainia sophia seeds have a variety of pharmacological functions and been widely used in traditional folk medicine. However, their effects on @entity1 drug metabolizing enzyme (DME) activities have not been elucidated. The present study investigated the inhibitory effects of an @entity1068 extract of D. sophia seeds (EEDS) on @entity1 Phase I/II (DMEs) and @entity1262 ( @entity1262 ) in vitro. METHODS: The enzyme activities of @entity1 Phase I (cytochrome P450s, CYPs), Phase II ( @entity858 glucuronosyltransferases, UGTs) DMEs, and the drug transporter @entity7895 were determined in the presence of various concentrations of EEDS using commercially available luminogenic assay systems. The mode of enzyme inhibition and the inhibitory constant (Ki) value of EEDS were graphically determined with Lineweaver-Burk double reciprocal plots and secondary plots, respectively. RESULTS: The enzyme activity assays showed that EEDS moderately inhibited the @entity4914 , @entity5060 , and @entity4433 isoforms with half maximal inhibitory concentrations (IC50) of 47.3, 25.8, and 38.7   g/mL, respectively. Graphical analyses with Lineweaver-Burk double reciprocal plots and secondary plots indicated that EEDS competitively inhibited @entity5060 with a Ki value of 19.8   g/mL; however, it inhibited @entity5060 and @entity4433 in a mixed mode with Ki values of 5.2, and 11.9   g/mL, respectively. Other Phase I ( @entity12327 , @entity5320 , and @entity5322 ) and Phase II ( @entity6912 and @entity22642 ) enzymes as well as @entity7895 were weakly or negligibly affected by EEDS with concentrations up to 500   g/mL. CONCLUSIONS: EEDS is a selective inhibitor of @entity4914 , @entity5060 , and @entity4433 with moderate enzymatic inhibition. Clinically, full consideration should be given to a potential toxic adverse effect from a herb-drug interaction when drugs that are particularly susceptible to @entity4914 , @entity5060 , or @entity4433 -mediated metabolism are taken together with EEDS. Characterization of metabolic profiles of specific herbal drugs could help consumers and medical specialists to use them safely as a complementary and alternative medicine.

Effect of an @entity1068 extract of Descurainia sophia seeds on Phase I and II drug metabolizing enzymes and XXXX activity in vitro.

@entity1 :: ('9606', 'Species') :: ['human'] @entity6912 :: ('54658', 'Gene') :: ['UGT1A1'] @entity1262 :: ('5243', 'Gene') :: ['P-glycoprotein', 'p-gp'] @entity5320 :: ('1565', 'Gene') :: ['CYP2D6'] @entity4433 :: ('1557', 'Gene') :: ['CYP2C19'] @entity5322 :: ('1576', 'Gene') :: ['CYP3A4'] @entity858 :: ('MESH:D014530', 'Chemical') :: ['uridine diphosphate'] @entity5060 :: ('1559', 'Gene') :: ['CYP2C9'] @entity7895 :: ('283871', 'Gene') :: ['P-gp'] @entity12327 :: ('1558', 'Gene') :: ['CYP2C8'] @entity4914 :: ('1544', 'Gene') :: ['CYP1A2'] @entity22642 :: ('7364', 'Gene') :: ['UGT2B7'] @entity1068 :: ('MESH:D000431', 'Chemical') :: ['ethanol']
@entity1262 :: (5243,Gene) :: ['P-glycoprotein']
