Ashour M B, Moody D E, Hammock B D
Toxicol Appl Pharmacol. 1987 Jul;89(3):361-9. doi: 10.1016/0041-008x(87)90155-4.
Treatment with 0.5% (w/w) dietary clofibrate, a peroxisome proliferator, for 14 days induced microsomal carboxylesterase activities for five substrates including malathion, clofibrate, diethylsuccinate, diethylphthalate, and p-nitrophenylacetate in liver and kidney of male Swiss-Webster mice and Sprague-Dawley rats. The induction was substrate, tissue, and species dependent. The carboxylesterase activity was induced in mouse from 1.2- to 2.2-fold (liver) and from 1.1- to 1.7-fold (kidney) depending upon substrate used. Analogous values from rat ranged from 1.0- to 1.4-fold (liver) and from 1.1- to 1.8-fold (kidney). Enzyme activities were either decreased or not affected in testes of treated mice and rats. Substituted trifluoroketones ("transition-state" inhibitors of carboxylesterase) were found to be very potent inhibitors of clofibrate-metabolizing carboxylesterase(s) and to be potentially useful in distinguishing among isozymes. The inhibition data suggested that changes in carboxylesterase activity following clofibrate treatment were both qualitative and quantitative.
用0.5%（w/w）的膳食氯贝丁酯（一种过氧化物酶体增殖剂）对雄性瑞士韦伯斯特小鼠和斯普拉格-道利大鼠进行为期14天的处理，诱导了肝脏和肾脏中包括马拉硫磷、氯贝丁酯、琥珀酸二乙酯、邻苯二甲酸二乙酯和对硝基苯乙酸在内的五种底物的微粒体羧酸酯酶活性。这种诱导作用取决于底物、组织和物种。根据所使用的底物，小鼠肝脏中的羧酸酯酶活性诱导倍数为1.2至2.2倍，肾脏中的诱导倍数为1.1至1.7倍。大鼠的类似数值范围为肝脏1.0至1.4倍，肾脏1.1至1.8倍。处理过的小鼠和大鼠睾丸中的酶活性要么降低，要么不受影响。发现取代的三氟酮（羧酸酯酶的“过渡态”抑制剂）是氯贝丁酯代谢羧酸酯酶的非常有效的抑制剂，并且可能有助于区分同工酶。抑制数据表明，氯贝丁酯处理后羧酸酯酶活性的变化既有定性的也有定量的。
