Carboxylesterase and Cholinesterase Inhibition in Rats

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Abstract
Hydrolysis of diethyl succinate, methyl butyrate, and triacetin by rat liver carboxylesterases was inhibited in vivo and in vitro by the insecticide, Abate. Liver carboxylesterases were severalfold more sensitive to such inhibition than blood, brain, or submaxillary gland cholinesterases. Administration for eight weeks of 1 ppm Abate, the recommended concentration for mosquito larvicidal use in drinking-water containers, produced a small (20%), but consistent, inhibition of liver triacetin esterase. Abate at 5 ppm in drinking water for seven days inhibited liver carboxylesterases by 40% and increased rat susceptibility to the anticholinesterase action of a single 400-mg/kg dose of malathion, which is detoxified by carboxylesterases. Technical-grade Abate was about 100 times more potent as a carboxylesterase inhibitor in vitro than was a purified sample; however, in vivo differences in carboxylesterase-inhibiting potency were small.

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