EFFECTS OF 1-ETHYNYLPYRENE AND RELATED INHIBITORS OF P450 ISOZYMES UPON BENZO[A]PYRENE METABOLISM BY LIVER-MICROSOMES

被引:26
作者
HALL, M
PARKER, DK
GROVER, PL
LU, JYL
HOPKINS, NE
ALWORTH, WL
机构
[1] ROYAL CANC HOSP,CHESTER BEATTY RES INST,INST CANC RES,LONDON SW3 6JB,ENGLAND
[2] TULANE UNIV,DEPT CHEM,NEW ORLEANS,LA 70118
关键词
1-Ethynylpyrene; 2-Ethynylnaphthalene; 3-Ethynylperylene; Aryl acetylenes; Benzo[a]pyrene; Benzo[a]pyrene 7,8-dihydrodiol; Microsomal metabolism; Tetrols from benzo[a]pyrene;
D O I
10.1016/0009-2797(90)90087-4
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The effects of three aryl acetylenes, 1-ethynylpyrene (EP), 2-ethynylnaphthalene (EN) and 3-ethynylperylene (EPE), upon the metabolism of benzo[a]pyrene (BaP) by microsomes isolated from rat liver were investigated. These aryl acetylenes all inhibited the total metabolism of BaP. Formation of BaP 7,8-dihydrodiol and BaP tetrol products by microsomal preparations from rats that had been pretreated with 3-methylcholanthrene (3MC) were preferentially inhibited. The effects of EP upon the metabolism of BaP 7,8-dihydrodiol by microsomes from rat liver were also studied. This aryl acetylene strongly inhibited the formation of BaP tetrols from BaP 7,8-dihydrodiol by liver microsomes both from untreated rats and from rats pretreated with 3MC, but enhanced the conversion of the BaP dihydrodiol into other metabolites. © 1990.
引用
收藏
页码:181 / 192
页数:12
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