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Information × Registration Number 0222U001456, 0120U100128 , R & D reports Title The study of enzyme systems of enantioselective hydrolysis and tyrosinase inhibitors to create new biologically active compounds popup.stage_title Head Romanovska Iryna I., Доктор біологічних наук Registration Date 27-01-2022 Organization Physico-Chemical Institute O. Bogatsky National Academy of Sciences of Ukraine popup.description2 The object of the study - carboxylesterase of porcine liver and hepatopancreas Rapana venosa. The aim of this work is to study the substrate specificity of Rapana venosa and porcine liver enzyme preparations containing carboxylesterase. Development of conditions and implementation of enantioselective hydrolysis of 3-hydroxy-1,4-benzodiazepin-2-one esters - promising hypnotic and anxiolytic compounds - using enzyme systems of the digestive glands of Rapana venosa mollusc and pig liver, containing carboxylesterase (pH, temperature, ratio of reagents and etc.). A method for the isolation of carboxylesterase from the cytosolic fraction of pig liver was developed, a homogeneous enzyme with a molecular weight of ~ 175 kDa (molecular weight of a subunit - 62 kDa) with high esterase activity was obtained. The kinetics of hydrolysis of 1-naphthyl acetate catalyzed by cytosolic carboxylesterase of the pig liver (Km - 640.6 ±30.8 μmol/dm3 and Vmax - 2557.6 ±53.2 μmol/mg protein per minute). The regioselectivity of porcine liver and hepatopancreas Rapana venosa carboxylesterases towards 1- and 2-naphthyl acetate was studied. It was determined that the specific esterase activity of carboxylesterase in the microsomal fraction of pig liver in 1- and 2-naphthyl acetate is almost the same. Activity of carboxylesterase in the cytosolic fraction of porcine liver and the cytosolic fraction of hepatopancreas Rapana venosa to 2-naphthyl acetate were 2.1 and 3.6 times higher than the activity in 1-naphthyl acetate, respectively. Using the carboxylesterases, enantioselective hydrolysis of 3-acetoxy-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one with a 50 % degree of transformation was carried out. It has been shown that the S-enantiomer of the substrate, was formed using the carboxylesterase of the porcine liver microsomal fraction, while the R-enantiomer was formed with the use of porcine cytosolic carboxylesterase and Rapana venosa hepatopancreas cytosol carboxylesterase. Product Description popup.authors Dekina Svitlana S. Mikhaylova Tetiana V. Shesterenko Yevheniya A. Shesterenko Yuliya А. popup.nrat_date 2022-03-09 Close