Title : Inhibitory effects of deoxypodophyllotoxin from Anthriscus sylvestris on human CYP2C9 and CYP3A4.

Pub. Date : 2010 May

PMID : 19960413






4 Functional Relationships(s)
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1 Inhibitory effects of deoxypodophyllotoxin from Anthriscus sylvestris on human CYP2C9 and CYP3A4. deoxypodophyllotoxin cytochrome P450 family 2 subfamily C member 9 Homo sapiens
2 When a mixture of specific CYP substrates was incubated with DPT in HLM, CYP2C9-catalyzed diclofenac 4-hydroxylation and CYP3A4-catalyzed midazolam 1-hydroxylation were strongly inhibited by DPT, with IC (50) values of 6.3 and 9.2 microM, respectively. deoxypodophyllotoxin cytochrome P450 family 2 subfamily C member 9 Homo sapiens
3 When a mixture of specific CYP substrates was incubated with DPT in HLM, CYP2C9-catalyzed diclofenac 4-hydroxylation and CYP3A4-catalyzed midazolam 1-hydroxylation were strongly inhibited by DPT, with IC (50) values of 6.3 and 9.2 microM, respectively. deoxypodophyllotoxin cytochrome P450 family 2 subfamily C member 9 Homo sapiens
4 From these results, DPT was characterized to be a competitive inhibitor of CYP2C9 and CYP3A4, with K(i) values of 3.5 and 10.8 microM in HLM and 24.9 and 3.5 microM in baculovirus-insect cell-expressed human CYPs, respectively. deoxypodophyllotoxin cytochrome P450 family 2 subfamily C member 9 Homo sapiens