New biocatalysts for the creation of potential drugs
According to the materials of scientific report at the meeting of the Presidium of NAS of Ukraine, December 13, 2017
DOI:
https://doi.org/10.15407/visn2018.03.073Keywords:
immobilization, pig liver microsomal fraction, polymeric supports, enantioselective hydrolysis, 3-hydroxy- 1,4-benzodiazepin-2-one estersAbstract
Methods of carboxylesterase immobilization as a component of pig liver microsomal fraction immobilization in polyvinyl alcohol, phyllophorine from Phyllophora nervosa and sodium alginate were developed. The highly active biocatalysts (65—80 % retaining of initial esterase activity), stable at storage and to elevated temperatures action, were
obtained. Biotechnologies of 3-hydroxy-1,4-benzodiazepin-2-one esters enantioselective hydrolysis with a help of free
and immobilized microsomal fraction preparation were created. As a result of enzymatic hydrolysis the S-enantiomers
of substrates, with increased affinity to central benzodiazepine receptors and anticonvulsant activity, were obtained
for the first time. The immobilized pig liver microsomal fraction preparations, as it was shown, catalyzed enantioselective hydrolysis of 3-hydroxy-1,4-benzodiazepin-2-one esters with 50 % degree of transformation during 5-12 cycles of
usage in batch mode.
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