Title : Metabolic activation of the indoloquinazoline alkaloids evodiamine and rutaecarpine by human liver microsomes: dehydrogenation and inactivation of cytochrome P450 3A4.

Pub. Date : 2014 Jun

PMID : 24696463






5 Functional Relationships(s)
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1 Metabolic activation of the indoloquinazoline alkaloids evodiamine and rutaecarpine by human liver microsomes: dehydrogenation and inactivation of cytochrome P450 3A4. rutecarpine cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Formation of the evodiamine and rutaecarpine GSH conjugates was primarily catalyzed by heterologously expressed recombinant CYP3A4 and, to a lesser extent, CYP1A2 and CYP2D6, respectively. rutecarpine cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 Formation of the evodiamine and rutaecarpine GSH conjugates was primarily catalyzed by heterologously expressed recombinant CYP3A4 and, to a lesser extent, CYP1A2 and CYP2D6, respectively. rutecarpine cytochrome P450 family 1 subfamily A member 2 Homo sapiens
4 Formation of the evodiamine and rutaecarpine GSH conjugates was primarily catalyzed by heterologously expressed recombinant CYP3A4 and, to a lesser extent, CYP1A2 and CYP2D6, respectively. rutecarpine cytochrome P450 family 2 subfamily D member 6 Homo sapiens
5 In summary, these findings are of significance in understanding the bioactivation mechanisms of indoloquinazoline alkaloids, and dehydrogenation of evodiamine and rutaecarpine may cause toxicities through formation of electrophilic intermediates and lead to drug-drug interactions mainly via CYP3A4 inactivation. rutecarpine cytochrome P450 family 3 subfamily A member 4 Homo sapiens