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Role of cytochrome P-450 isozyme 3a in microsomal metabolism of three nasal carcinogens

Conference · · Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States)
OSTI ID:7145085

Cytochrome P-450 isozyme 3a, first isolated from rabbit liver microsomes, also occurs in nasal mucosal microsomes. The role of the cytochrome in the metabolism of three nasal carcinogens, hexamethylphosphoramide (HMPA), N-nitrosodiethylamine (NDEA), and phenacetin (PA) was examined in the present study. Microsomal preparations from rabbit nasal ethmoturbinates catalyze the O- or N-deakylation of the above compounds at much greater rates than do liver microsomes. The participation of isozyme 3a was shown by immunochemical experiments involving inhibition by anti-isozyme 3a antibodies. With 1.0 mM substrate present, anti-3a IgG inhibited the activities in nasal membrane microsomes as follows: HMPA N-demethylation, 61%; NDEA N-deethylation, 67%; and PA O-deethylation, 75%. Similar results were obtained in experiments with liver microsomes except for PA O-deethylation, which was only slightly inhibited (18%) by the antibody. The involvement of isozyme 3a in the dealkylation activities was further indicated by a correlation between the increase in anti-3a-inhibited rates and the induction of isozyme 3a in liver microsomes from animals chronically administered ethanol. They conclude that isozyme 3a plays a significant role in the metabolism and, presumably, the known carcinogenicity of HMPA, NDEA, and PA in nasal mucosa.

Research Organization:
Univ. of Michigan, Ann Arbor
OSTI ID:
7145085
Report Number(s):
CONF-8606151-
Journal Information:
Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States), Journal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) Vol. 45:6; ISSN FEPRA
Country of Publication:
United States
Language:
English