甲氧杀虫酯的药效、毒性及生物降解的研究——Ⅰ.甲氧杀虫酯的药效、降解和对酯酶的影响

The Effectiveness, Toxicity and Biodegradation of Methoxyphenyl Acetate (8701).——Ⅰ. The effectiveness, biodegradation of methoxyphenyl Acetate and its effect on the activity of esterase.

甲氧杀虫酯是在研究三氯杀虫酯类似物的化学结构与生物活性关系中所发现的一种对蚊(淡色库蚊KT_(50)=3.22分,埃及伊蚊KT_(50)=1.77分)、家蝇(LD_(50)=0.31ug/只)药效较好的新品种。经试验,它对连续染毒20天的小白鼠血清的乙酰胆碱酯酶和羧酸酯酶活性无抑制作用。凝胶电泳法证明,其对小白鼠血清和肝组织(包括离体组织)酯酶活性亦无影响。离体鼠肝细胞降解试验表明,45分钟降解72.5%,90分钟可降解93%,这表明该化合物极易生物降解。

Methoxy phenyl Acetate which was screened from study on the relationship between the chemical structure of 1-(3, 4-dichlorophenyl)-2, 2, 2-triehloroethyl acetate analogues and insecticidal activities is a new type of insecticide to mosquito and housefly. The LD_(50) to houseflies (Musea domestica vicina L,) is 0.3 lug/hody. The KT_(50) to mosquitoes (Aedes aegypti L.) is 1.77 min. and 3.22 min. ( Culex pipiens var. pallens) respectively. No effect of this compound on the activities of acetylcholinesterase and carboxylesterase releasing from serum has been determinted, the serum used come from mice which was treated with methoxyphenyl acetate ench day stccessively for 20 days. The activity of esterase from serum(enzyme source is same as AchE) and liver tissue were analyzed by SDS-gel electrophoresis, the result showed that there is no inhibition of this compound to esterase activity.Rate of Biodegradation of Methoxyphenyl Acetate was carried out in special apparatus, 5ml of Waymouth's medium or the medium containing the desired chemical (1×10^(-4) mol/L) was introduced into each incubation flask. The same volume of Waymouth's medium containing hepatocytes was then transferred from the maintance flask to the incubation at 37℃, 0.4ml aliquot were removed at intervals and centrifuged (2000 rpm/min.) for 5 sec. A 0.2ml aliquot of supernatant fluid was carefully removed into a tube containing 0.1ml of TCA(10%) and added 2ml of hexane for extraction. The extract was stored at-20℃ until GC analysis. It has been shown that the rate of biodegradation of Methoxyphenyl Acetate was 72.5% and 93% within 45 min. and 90 min. respectively. It seems to be biogradated with ease.