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目的:研究二乙酰单肟(diacetylm onoxim e,DAM)对敌敌畏体内外抑制小鼠小肠羧酸酯酶重活化的作用。方法:用微量对硝基酚戊酸酯法测定DAM 对敌敌畏体内外抑制的小鼠小肠羧酸酯酶的重活化作用。结果与结论:1,0.5,0.1 m m ol/L的DAM 在体外对敌敌畏抑制的小鼠小肠羧酸酯酶有较强的重活化作用(重活化率分别为84.8% ,59.3% 和32.4% ),而对正常小肠羧酸酯酶没有抑制作用,但DAM 经口、肌肉和腹腔给药(均为100 m g/kg 体重)在整体对小鼠敌敌畏经口中毒(100 m g/kg 体重)没有显著的抗毒作用,对小鼠敌敌畏50 m g/kg 体重经口中毒后小肠羧酸酯酶的抑制也没有显著的重活化作用(P> 0.05);而且DAM 经口与腹腔给药后小鼠小肠羧酸酯酶活力显著下降(P< 0.05),但DAM 经肌肉给药后小鼠小肠羧酸酯酶活力没有显著变化,从而提示DAM 经口、肌肉与腹腔给药都不能有效地对抗敌敌畏对小鼠的毒性,其本身经口与腹腔给药后对小肠羧酸酯酶的抑制作用可能与肝肠首过效应有关。
Objective: To investigate the effect of diacetylm onoxim e (DAM) on the inhibition of carboxylesterase reactivation in mice small intestine in vitro and in vivo. Methods: The reactivation of carboxylesterase in mouse small intestine by DAM against Dichlorvos in vivo and in vitro was determined by micro p-nitrophenolacetate method. RESULTS AND CONCLUSION: DAM at 1, 0.5 and 0.1 m mol / L had a strong reactivation activity on small intestine carboxylesterase inhibited by dichlorvos in vitro (the rates of reactivation were 84.8% , 59.3% and 32.4%, respectively), whereas normal intestinal carboxylesterase had no inhibitory effect, but DAM was administered orally, intramuscularly and intraperitoneally (both at 100 m g / kg body weight) Oral toxicity (100 m g / kg body weight) had no significant antitoxic effect, and no significant reactivation of small intestine carboxylesterase was observed after oral administration of 50 μg / kg body weight of dichlorvos (P> 0 .05). Moreover, the activity of carboxylesterase in the small intestine of mice was significantly decreased (P <0.05) after oral and intraperitoneal administration of DAM, but there was no significant change in the intestinal carboxylesterase activity of DAM after intramuscular administration, It is suggested that oral administration of DAM, intramuscular and intraperitoneal injection of DAM can not effectively combat the toxicity of dichlorvos in mice, itself after oral and intraperitoneal administration of small intestinal carboxylesterase Production may be related to the first effect of the intestine.