H. Doostdar et al., THE EFFECTS OF INDUCING AGENTS ON CYTOCHROME-P450 AND UDP-GLUCURONOSYLTRANSFERASE ACTIVITIES IN HUMAN HEPG2 HEPATOMA-CELLS, Biochemical pharmacology, 46(4), 1993, pp. 629-635
Selective induction in vitro of cytochrome P450-dependent mixed-functi
on oxidase (MFO) and UDP-glucuronyltransferase (GT) activities was obs
erved in the human HepG2 hepatoma cell line. 1,2-Benzanthracene (BA) i
nduced MFO O-dealkylation activities for ethoxyresorufin, methoxyresor
ufin and benzyloxyresorufin, whereas phenobarbitone (PB) selectively i
nduced pentoxyresorufin O-dealkylation and rifampicin (RIF) selectivel
y induced benzyloxyresorufin O-dealkylation. Antibody inhibition exper
iments indicated that ethoxyresorufin and methoxyreSorufin O-dealkylat
ions were catalysed mainly by the P450 1A subfamily in untreated and B
A-induced HepG2 cells, that additional unidentified P450 forms were co
nsiderably involved in methoxyresorufin and benzyloxyresorufin O-dealk
ylations and that the P450 2B subfamily was partially responsible for
pentoxyresorufin O-dealkylation in PB-induced cells. Bilirubin GT acti
vity was induced by PB, BA, RIF and dexamethasone, but 1-naphthol, mor
phine and testosterone GT activities were not induced by any of these
treatments.