2011Biotechnologia ActaOpen access

Выделение и характеристика карбоксилэстеразы печени свиньи и ее использование в стереоселективном гидролизе производных 1,4-бенздиазепин-2-она

С. А. Андронати, Е. А. Шестеренко, О. В. Севастьянов, И. И. Романовская, В. И. Павловский, E.A. Semenishina, В. Е. Осетров

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Abstract

Since the commercial preparations of pig liver carboxylesterase are expensive, the development of convenient and available methods of carboxylesterase isolation for usage in stereoselective hydrolysis of new 1.4-benzodiazepine-2one esters is an essential task. An effective and convenient method for isolation of pig liver microsomal carboxylesterase with protein yield 2.24 mg/g tissue and esterase activity of 149 μmole·min –1·mg –1 protein is described in paper. With native electrophoresis usage, 19 protein fractions were found in carboxyl esterase preparation, 11 of which (73% of the total protein) possesses esterase activity. For the first time, using pig liver microsomal carboxyl esterase, the stereoselective 3-acetoxy-7-bromo1-methyl-5 phenyl-1,2-dihydro-3H-1,4-benzodiazepine-2-one hydrolysis was accomplished and thus S-enantiomer of substrate was obtained.

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Since the commercial preparations of pig liver carboxylesterase are expensive, the development of convenient and available methods of carboxylesterase isolation for usage in stereoselective hydrolysis of new 1.4-benzodiazepine-2one esters is an essential task. An effective and convenient method for isolation of pig liver microsomal carboxylesterase with protein yield 2.24 mg/g tissue and esterase activity of 149 μmole·min –1·mg –1 protein is described in paper. With native electrophoresis usage, 19 protein fractions were found in carboxyl esterase preparation, 11 of which (73% of the total protein) possesses esterase activity. For the first time, using pig liver microsomal carboxyl esterase, the stereoselective 3-acetoxy-7-bromo1-methyl-5 phenyl-1,2-dihydro-3H-1,4-benzodiazepine-2-one hydrolysis was accomplished and thus S-enantiomer of substrate was obtained.

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Available abstract

Since the commercial preparations of pig liver carboxylesterase are expensive, the development of convenient and available methods of carboxylesterase isolation for usage in stereoselective hydrolysis of new 1.4-benzodiazepine-2one esters is an essential task. An effective and convenient method for isolation of pig liver microsomal carboxylesterase with protein yield 2.24 mg/g tissue and esterase activity of 149 μmole·min –1·mg –1 protein is described in paper. With native electrophoresis usage, 19 protein fractions were found in carboxyl esterase preparation, 11 of which (73% of the total protein) possesses esterase activity. For the first time, using pig liver microsomal carboxyl esterase, the stereoselective 3-acetoxy-7-bromo1-methyl-5 phenyl-1,2-dihydro-3H-1,4-benzodiazepine-2-one hydrolysis was accomplished and thus S-enantiomer of substrate was obtained.

Key concepts: Carboxylesterase, Esterase, Pig liver, Microsome, Hydrolysis, Chemistry, Stereoselectivity, Chromatography

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Выделение и характеристика карбоксилэстеразы печени свиньи и ее использование в стереоселективном гидролизе производных 1,4-бенздиазепин-2-она — Research Paper | ScholarLens