Ketterman A J, Pond S M, Becker C E
Toxicol Appl Pharmacol. 1987 Mar 15;87(3):389-92. doi: 10.1016/0041-008x(87)90243-2.
The organophosphorous pesticide malathion is metabolized by three hepatic enzyme systems: the microsomal cytochrome P-450-dependent monooxygenase system, the microsomal carboxylesterases, and the cytosolic glutathione S-transferases. We produced differential induction of these three enzyme systems in mice with phenobarbital and 2(3)-tert-butyl-4-hydroxyanisole (BHA) and examined the effects of the induction on the inhibition of acetylcholinesterases by malathion. Phenobarbital not only significantly induced hepatic microsomal cytochrome P-450 (p less than 0.05) but also increased microsomal carboxylesterase activity (p less than 0.05). BHA not only increased the activity of microsomal carboxylesterases (p less than 0.05) but also substantially increased cytosolic glutathione S-transferase activity (p less than 0.05). Despite the differential effects of phenobarbital and BHA on the three enzyme systems, neither agent protected the mice against malathion toxicity.
微粒体细胞色素P-450依赖性单加氧酶系统、微粒体羧酸酯酶和胞质谷胱甘肽S-转移酶。我们用苯巴比妥和2(3)-叔丁基-4-羟基茴香醚（BHA）在小鼠中对这三种酶系统进行了差异诱导，并研究了诱导对马拉硫磷抑制乙酰胆碱酯酶的影响。苯巴比妥不仅显著诱导肝脏微粒体细胞色素P-450（p<0.05），还增加了微粒体羧酸酯酶活性（p<0.05）。BHA不仅增加了微粒体羧酸酯酶的活性（p<0.05），还大幅增加了胞质谷胱甘肽S-转移酶的活性（p<0.05）。尽管苯巴比妥和BHA对这三种酶系统有不同的影响，但这两种药物均不能保护小鼠免受马拉硫磷的毒性作用。
