Title : Oxidative metabolism of the alkaloid rutaecarpine by human cytochrome P450.

Pub. Date : 2006 May

PMID : 16501007






8 Functional Relationships(s)
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1 These results indicated that multiple hepatic P450s including CYP1A2, CYP2D6, and CYP3A4 participate in rutaecarpine hydroxylations. rutecarpine cytochrome P450 family 1 subfamily A member 2 Homo sapiens
2 These results indicated that multiple hepatic P450s including CYP1A2, CYP2D6, and CYP3A4 participate in rutaecarpine hydroxylations. rutecarpine cytochrome P450 family 2 subfamily D member 6 Homo sapiens
3 These results indicated that multiple hepatic P450s including CYP1A2, CYP2D6, and CYP3A4 participate in rutaecarpine hydroxylations. rutecarpine cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 Among recombinant P450s, CYP1A1 had the highest rutaecarpine hydroxylation activity. rutecarpine cytochrome P450 family 1 subfamily A member 1 Homo sapiens
5 CYP1A1-catalyzed rutaecarpine hydroxylations had V(max) values of 1,388 to approximately 1,893 pmol/min/nmol P450, K(m) values of 4.1 to approximately 9.5 microM, and K(i) values of 45 to approximately 103 microM. rutecarpine cytochrome P450 family 1 subfamily A member 1 Homo sapiens
6 The major metabolite 10-hydroxyrutaecarpine decreased CYP1A1, CYP1A2, and CYP1B1 activities with respective IC(50) values of 2.56 +/- 0.04, 2.57 +/- 0.11, and 0.09 +/- 0.01 microM, suggesting that product inhibition might occur during rutaecarpine hydroxylation. rutecarpine cytochrome P450 family 1 subfamily A member 1 Homo sapiens
7 The major metabolite 10-hydroxyrutaecarpine decreased CYP1A1, CYP1A2, and CYP1B1 activities with respective IC(50) values of 2.56 +/- 0.04, 2.57 +/- 0.11, and 0.09 +/- 0.01 microM, suggesting that product inhibition might occur during rutaecarpine hydroxylation. rutecarpine cytochrome P450 family 1 subfamily A member 2 Homo sapiens
8 The major metabolite 10-hydroxyrutaecarpine decreased CYP1A1, CYP1A2, and CYP1B1 activities with respective IC(50) values of 2.56 +/- 0.04, 2.57 +/- 0.11, and 0.09 +/- 0.01 microM, suggesting that product inhibition might occur during rutaecarpine hydroxylation. rutecarpine cytochrome P450 family 1 subfamily B member 1 Homo sapiens