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首页> 外文期刊>Life sciences >GENDER-SPECIFIC DIFFERENCES IN ACTIVITY AND PROTEIN LEVELS OF COCAINE CARBOXYLESTERASE IN RAT TISSUES
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GENDER-SPECIFIC DIFFERENCES IN ACTIVITY AND PROTEIN LEVELS OF COCAINE CARBOXYLESTERASE IN RAT TISSUES

机译：大鼠组织中可卡因羧酸酯酶活性和蛋白水平的性别差异

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The gender-specific differences in the content of cocaine methyl esterase and ethyl transferase activities are examined in rat tissues and related to differences in hydrolase A protein in rat liver, lung, and kidney reported previously. The rat hydrolase A catalyzes the conversion of cocaine to benzoylecgonine and the ethyl transesterification of cocaine to form cocaethylene. An HPLC assay was used to quantitate and compare cocaine esterase activities in male and female rat tissues. The cocaine methyl esterase and ethyl transferase activities are 1.4 to 2.5 fold greater in male than in female liver and slightly greater in female than in male lung. No gender-specific differences were detected in the kidney. Gel electrophoresis was used to separate three non-specific carboxylesterases (hydrolases A, B, and C) in rat tissues and the isoenzymes were visualized with a hydrolase activity stain using 4-methylumbelliferyl acetate as substrate. The activity of cocaine methyl esterase and content of hydrolase A protein are not consistently different in the lung or the kidney of male versus female rats. Activity of hydrolase A in gels of male liver is greater than in female liver. Similarly, the content of the corresponding hydrolase A immunoreactive protein in male liver is 1.6 fold greater than in female liver. In contrast to hydrolase A, hydrolase C activity is greater in gels of female than male liver extracts. The greater content of cocaine methyl esterase and ethyl transferase activity in male versus female rat livers suggests that there may be gender-specific differences in pharmacokinetics of cocaine metabolism and extent of cocaine-induced hepatotoxicity in rats. [References: 25]
机译：在大鼠组织中检查了可卡因甲基酯酶含量和乙基转移酶活性的性别特异性差异，并且与先前报道的大鼠肝，肺和肾中水解酶A蛋白的差异有关。大鼠水解酶A催化可卡因向苯甲酰芽子碱的转化以及可卡因的乙基酯交换反应形成可卡乙烯。 HPLC测定法用于定量和比较雄性和雌性大鼠组织中的可卡因酯酶活性。男性可卡因甲基酯酶和乙基转移酶的活性比女性肝脏高1.4到2.5倍，女性比男性肺稍高。在肾脏中未检测到性别特异性差异。凝胶电泳用于分离大鼠组织中的三种非特异性羧酸酯酶（水解酶A，B和C），并使用水解酶活性染色剂（以乙酸4-甲基伞形酯为底物）观察同工酶。可卡因甲基酯酶的活性和水解酶A蛋白的含量在雄性和雌性大鼠的肺或肾中没有一致的差异。雄性肝凝胶中水解酶A的活性高于雌性肝。同样，男性肝脏中相应水解酶A免疫反应蛋白的含量是女性肝脏的1.6倍。与水解酶A相反，雌性凝胶中的水解酶C活性高于雄性肝提取物。雌性和雌性大鼠肝脏中可卡因甲基酯酶和乙基转移酶活性的含量较高，表明可卡因代谢的药代动力学和大鼠可卡因诱导的肝毒性程度可能存在性别特异性差异。 [参考：25]

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