2 research outputs found
Lipase B from Candida antarctica — the wide applicable biocatalyst in obtaining pharmaceutical compounds
Lipases are commonly applied in the pharmaceutical and chemical industry, especially in immobilizedform. The use of immobilized lipases facilitates the design of reactors and control of reactions, for example,fast stopping the reaction. The immobilization procedure should increase the stability of the lipaseand its activity, as well as be simple and efficient. Lipase B from Candida antarctica (CAL-B) is an enzymefrom the lipase group, isolated from the Candida antarctica species. CAL-B has the highest activity innon-polar organic solvents, such as hexane and toluene, and the lowest in polar solvents, e.g. acetonitrile.Due to its hydrolytic properties, this enzyme degrades triglycerides of fatty acids to free fatty acids (FFA)and glycerol. Described lipase is often immobilized, in the aim to increase enantioselective and lipolyticactivity. The kinetic and dynamic resolution with the application of lipase is one of the ways in obtainingan enantiopure form of the drugs, which usually are more effective and safer for the patient. The CAL-Bcould be also applied in the kinetic resolution of compounds being building blocks, derivates of drugs orconjugated forms. Furthermore, the CAL-B is used in the reactions in receiving of organic compounds,which are the natural origin, especially vegetable. Based on the presented data, it can be concluded, thatCAL-B is an enzyme with a wide application in the biosynthesis of compounds with therapeutic activity
Metabolic chiral inversion of 2-arylpropionic acid derivatives (profens)
2-arylpropionic acid derivatives (profens) are one of the most popular anti-inflammatory, analgesic, and antipyretic drugs. They belong to a group of nonsteroidal anti-inflammatory drugs (NSAID) and exhibit metabolic chiral inversion. Enantiomers of these chiral drugs are often characterised by different pharmacological activity. It is estimated that the values of metabolic chiral inversion of (R)-ibuprofen in humans are between 35 and 70%, depending on the condition of the liver and the intake of other medicines, while (R)-flurbiprofen undergoes chiral metabolic inversion to its opposed (S) form only in small range. The described phenomenon in the case of (R)-ketoprofen is limited to a maximum of around 10%. The metabolic chiral inversion is associated with potentially important pharmacotherapeutic and toxicological consequences, and so an attempt was made to analyse this phenomenon for the most commonly used drugs from the profens group