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

Evaluation of Designed Immobilized Catalytic Systems: Activity Enhancement of Lipase B from Candida antarctica

Publisher's version (útgefin grein)Immobilized enzymatic catalysts are widely used in the chemical and pharmaceutical industries. As Candida antarctica lipase B (CALB) is one of the more commonly used biocatalysts, we attempted to design an optimal lipase-catalytic system. In order to do that, we investigated the enantioselectivity and lipolytic activity of CALB immobilized on 12 different supports. Immobilization of lipase on IB-D152 allowed us to achieve hyperactivation (178%) in lipolytic activity tests. Moreover, the conversion in enantioselective esterification increased 43-fold, when proceeding with lipase-immobilized on IB-S861. The immobilized form exhibited a constant high catalytic activity in the temperature range of 25 to 55°C. Additionally, the lipase immobilized on IBD152 exhibited a higher lipolytic activity in the pH range of 6 to 9 compared with the native form. Interestingly, our investigations showed that IB-S500 and IB-S60S offered a possibility of application in catalysis in both organic and aqueous solvents. A significant link between the reaction media, the substrates, the supports and the lipase was confirmed. In our enzymatic investigations, highperformance liquid chromatography (HPLC) and the titrimetric method, as well as the Bradford method were employed.This work was supported by the National Science Centre Poland grant DEC-2013/09/N/NZ7/03557.Peer Reviewe

The Awareness of Risks Associated with OTC Drugs Available in Non-Pharmacy Outlets among Polish Patients—A Cross-Sectional Study

Background: Many OTC drugs are available in non-pharmacy outlets, and as such the risk of overuse and/or improper use of this class of drugs is more likely. In light of this observation, our study was conducted with the aim of exploring opinions on non-pharmaceutical distribution among Polish patients. This study was a part of an informative project to educate patients about the possible risks associated with the use of OTC medicines. Methods: We conducted a cross-sectional study among Polish patients in which we used an authorial questionnaire, previously tested via content, face validity, and a pilot study. The questionnaire was distributed both electronically and in a traditional form. Results: ‘Time saving’ had a statistically significant role in the patient’s decision about purchasing drugs in a non-pharmacy outlet (p = 0.0052; R = 0.276994). The lack of a pharmacist’s consultation/advice (p = 0.0072; R = −0.3290490), improper storage (p = 0.0044; R = −0.238246), risk of overdose (p = 0.0125; R = −0.189564), and the risk of purchasing out-of-date drugs (p = 0.0125; R = −0.145411), as well as the risk of purchasing falsified drugs (p = 0.0265; R = −0.159428), were all associated with the patient’s non-willingness to purchase drugs in non-pharmacy outlets. Patients supported the idea of the elimination of non-pharmacy outlet distribution (p = 0.0074; R = −0.195932); they also emphasized that they are advocates of purchasing drugs only in community pharmacies (p = 0.0006; R = −0.238625). Conclusion: Patients are aware of the risks associated with buying drugs outside of community pharmacies. They perceived pharmacists as professional health care advisors and supported the fact that OTC drugs should be available only via pharmaceutical distribution

Searching for Celts in Upper Silesia. Verification by excavation of a geophysical survey in Samborowice

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Farming and stock-breeding in the La Tène culture communities in Poland

In this article, the basic information on the research on the economy of the La Tène culture communities living in the southern part of Poland in the early and middle La Tène period is presented. The analysis of natural data shows that the local economy of the Celtic settlers from Silesia and Lesser Poland did not differ in quality from that of their countrymen from the area south of the Carpathians and the Sudetes. Agriculture was based on the cultivation of cereals, among which different varieties of wheat dominated with a relatively small share of barley and common millet. Contrary to earlier opinions, rye and oat cultivation was not widespread. In typical rural settlements, cattle farming was by far the dominant activity. Breeding swine and small ruminants were in the second position, but the proportion between these species varied from region to region. The very small proportion of wild animal bones known from the surveyed settlements indicates an advanced process of deforestation of the inhabited area and well-developed domestic animal husbandry

The High ‘Lipolytic Jump’ of Immobilized Amano A Lipase from Aspergillus niger in Developed ‘ESS Catalytic Triangles’ Containing Natural Origin Substrates

Lipase Amano A from Aspergillus niger (AA-ANL) is among the most commonly applied enzymes in biocatalysis processes, making it a significant scientific subject in the pharmaceutical and medical disciplines. In this study, we investigated the lipolytic activity of AA-ANL immobilized onto polyacrylic support IB-150A in 23 oils of natural origin containing various amounts of polyunsaturated fatty acids (PUFAs) and monounsaturated fatty acids (MUFAs). The created systems were expressed as an ‘ESS catalytic triangle’. A distinct ‘jump’ (up to 2400%) of lipolytic activity of immobilized AA-ANL compared to free lipase and hyperactivation in mostly tested substrates was observed. There was a ‘cutoff limit’ in a quantitative mutual ratio of ω-PUFAs/MUFAs, for which there was an increase or decrease in the activity of the immobilized AA-ANL. In addition, we observed the beneficial effect of immobilization using three polyacrylic supports (IB-150A, IB-D152, and IB-EC1) characterized by different intramolecular interactions. The developed substrate systems demonstrated considerable hyperactivation of immobilized AA-ANL. Moreover, a ‘lipolytic jump’ in the full range of tested temperature and pH was also observed. The considerable activity of AA-ANL-IB-150A after four reuse cycles was demonstrated. On the other hand, we observed an essential decrease in stability of immobilized lipase after 168 h of storage in a climate chamber. The tested kinetic profile of immobilized AA-ANL confirmed the increased affinity to the substrate relative to lipase in the free form

The Application of Two-Phase Catalytic System in Enantioselective Separation of Racemic (<i>R</i>,<i>S</i>)-1-Phenylethanol

Kinetic resolution is one of the methods which allows obtaining enantiomerically pure compounds. In the study presented herein, enantioselective biotransformations of (R,S)-1-phenylethanol were performed with the use of various catalytic systems containing ionic liquids and n-heptane or toluene as a reaction medium, vinyl acetate or isopropenyl acetate as an acetylating agent, and lipases from Burkholderia cepacia or Candida rugosa. The conducted studies proved that the use of Burkholderia cepacia lipase, vinyl acetate, and n-heptane with [EMIM][BF4] allows obtaining enantiomerically pure 1-phenylethyl acetate, with the enantiomeric excess of products eep = 98.9%, conversion c = 40.1%, and high value of enantioselectivity E > 200. Additionally, the use of ionic liquids allowed us to reuse enzyme in 5 reaction cycles, ensuring the high operational stability of the protein

The Awareness of Risks Associated with OTC Drugs Available in Non-Pharmacy Outlets among Polish Patients—A Cross-Sectional Study

Background: Many OTC drugs are available in non-pharmacy outlets, and as such the risk of overuse and/or improper use of this class of drugs is more likely. In light of this observation, our study was conducted with the aim of exploring opinions on non-pharmaceutical distribution among Polish patients. This study was a part of an informative project to educate patients about the possible risks associated with the use of OTC medicines. Methods: We conducted a cross-sectional study among Polish patients in which we used an authorial questionnaire, previously tested via content, face validity, and a pilot study. The questionnaire was distributed both electronically and in a traditional form. Results: ‘Time saving’ had a statistically significant role in the patient’s decision about purchasing drugs in a non-pharmacy outlet (p = 0.0052; R = 0.276994). The lack of a pharmacist’s consultation/advice (p = 0.0072; R = −0.3290490), improper storage (p = 0.0044; R = −0.238246), risk of overdose (p = 0.0125; R = −0.189564), and the risk of purchasing out-of-date drugs (p = 0.0125; R = −0.145411), as well as the risk of purchasing falsified drugs (p = 0.0265; R = −0.159428), were all associated with the patient’s non-willingness to purchase drugs in non-pharmacy outlets. Patients supported the idea of the elimination of non-pharmacy outlet distribution (p = 0.0074; R = −0.195932); they also emphasized that they are advocates of purchasing drugs only in community pharmacies (p = 0.0006; R = −0.238625). Conclusion: Patients are aware of the risks associated with buying drugs outside of community pharmacies. They perceived pharmacists as professional health care advisors and supported the fact that OTC drugs should be available only via pharmaceutical distribution