Protein Information

Name liver carboxylesterase
Synonyms ACAT; Cholesteryl ester hydrolase; CES1; SES 1; SES1; ANAE; Acid esterase; Acyl coenzyme A cholesterol acyltransferase…

Compound Information

Name malathion
CAS diethyl 2-[(dimethoxyphosphinothioyl)thio]butanedioate

Reference List

PubMed Abstract RScore(About this table)
3434778 Ashour MB, Gee SJ, Hammock BD: Use of a 96-well microplate reader for measuring routine enzyme activities. Anal Biochem. 1987 Nov 1;166(2):353-60.

Examples include monitorings of the rate of hydrolysis of acetylthiocholine iodide by eel acetylcholinesterase and the rate of hydrolysis of malathion and nonconventional esters such as O-methyl, O-ethyl, and O-isobutyl carbonates of p-nitrophenol by commercial porcine liver carboxylesterase.
6(0,0,1,1) Details
8321828 Huang TL, Szekacs A, Uematsu T, Kuwano E, Parkinson A, Hammock BD: Hydrolysis of carbonates, thiocarbonates, carbamates, and carboxylic esters of alpha-naphthol, beta-naphthol, and p-nitrophenol by human, rat, and mouse liver carboxylesterases. Pharm Res. 1993 May;10(5):639-48.

Malathion was a 15-fold better substrate for hydrolase B than for hydrolase A.
2(0,0,0,2) Details
6639686 Imamura T, Gandy J, Fukuto TR: Selective inhibition of rat pulmonary monooxygenase by O,O,S-trimethyl phosphorothioate treatment. Biochem Pharmacol. 1983 Nov 1;32(21):3191-5.

In contrast, a dose-dependent decrease was observed in the liver carboxylesterase.
Pulmonary malathion carboxylesterase activity was not affected by OOS treatment.
1(0,0,0,1) Details
3593399 Ashour MB, Hammock BD: Substituted trifluoroketones as potent, selective inhibitors of mammalian carboxylesterases. Biochem Pharmacol. 1987 Jun 15;36(12):1869-79.

A series of substituted trifluoroketones were tested as inhibitors of mammalian liver microsomal carboxylesterase (s) hydrolyzing a variety of substrates including malathion, diethylsuccinate (DES) and p-nitrophenyl acetate (p-NpAc).
The trifluoroketones used were very potent "transition state" inhibitors of crude mouse and human liver microsomal carboxylesterases as well as commercial porcine liver carboxylesterase (Sigma EC 3.1.1.1 Type I).
1(0,0,0,1) Details
7420466 Mallipudi NM, Talcott RE, Ketterman A, Fukuto TR: Properties and inhibition of rat malathion carboxylesterases. J Toxicol Environ Health. 1980 May;6(3):585-96.

Isomalathion appeared to be equipotent in inhibiting the rat liver carboxylesterase-catalyzed reactions leading to either alpha or beta-monoacid.
1(0,0,0,1) Details
6642106 Costa LG, Murphy SD: Unidirectional cross-tolerance between the carbamate insecticide propoxur and the organophosphate disulfoton in mice. Fundam Appl Toxicol. 1983 Sep-Oct;3(5):483-8.

While hepatic microsomal enzymes appeared to be unchanged in disulfoton-tolerant mice, brain and liver carboxylesterase activities were significantly inhibited.
The acute toxicity of the organophosphate malathion was also increased in disulfoton-tolerant mice.
1(0,0,0,1) Details