@entity13439 (GA) has been used clinically in the treatment of @entity1 with @entity3619 . This study evaluated the effect of GA on the activity of five P450(CYP450) cytochrome enzymes: @entity5944 , @entity5060 , @entity4433 , @entity5320 , and @entity5322 , in @entity1 liver microsomes (HLMs) and recombinant cDNA-expressed enzyme systems using a HPLC-MS/MS CYP-specific probe substrate assay. With @entity1363 as the probe substrate, GA greatly decreased @entity5322 activity with IC50 values of 8.195  M in HLMs and 7.498  M in the recombinant cDNA-expressed @entity5322 enzyme system, respectively. It significantly decreased @entity5322 activity in a dose- but not time-dependent manner. Results from Lineweaver-Burk plots showed that GA could inhibit @entity5322 activity competitively, with a Ki value of 1.57  M in HLMs. Moreover, @entity5060 and @entity4433 could also be inhibited significantly by GA with IC50 of 42.89 and 40.26  M in HLMs, respectively. Other CYP450 isoforms were not markedly affected by GA. The inhibition was also confirmed by an in vivo study of @entity19 . In addition, it was observed that mRNA expressions of the Cyps2c and 3a family decreased significantly in the livers of @entity19 treated with GA. In conclusion, this study indicates that GA may exert herb-drug interactions by competitively inhibiting @entity5322 .

In Vitro and in Vivo Inhibitory Effects of XXXX in @entity19 and @entity1 Cytochrome P450 3A4.

@entity1 :: ('9606', 'Species') :: ['human', 'patients'] @entity5944 :: ('1548', 'Gene') :: ['CYP2A6'] @entity5320 :: ('1565', 'Gene') :: ['CYP2D6'] @entity4433 :: ('1557', 'Gene') :: ['CYP2C19'] @entity5322 :: ('1576', 'Gene') :: ['CYP3A4'] @entity19 :: ('10090', 'Species') :: ['mice'] @entity13439 :: ('MESH:D006034', 'Chemical') :: ['Glycyrrhetinic acid'] @entity5060 :: ('1559', 'Gene') :: ['CYP2C9'] @entity3619 :: ('MESH:D006521', 'Disease') :: ['chronic hepatitis'] @entity1363 :: ('MESH:D008874', 'Chemical') :: ['midazolam']
@entity13439 :: (MESH:D006034,Chemical) :: ['Glycyrrhetinic Acid']
