Acta Med. 2002, 45: 7-12

New Potential Nonsteroidal Anti-Inflammatory Drugs with Antileukotrienic Effects: Influence on Model Proteins with Catalytic Activity

Miloslava Netopilováa,b, Jaroslav Dršataa,b, Martin Beránekc, Vladimír Paličkac

aCharles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Biochemical Sciences, Hradec Králové, Czech Republic
bCharles University in Prague, Faculty of Pharmacy in Hradec Králové, Research Centre LN00B125, Hradec Králové, Czech Republic
cUniversity Hospital in Hradec Králové, Department of Clinical Biochemistry, Hradec Králové, Czech Republic

Received December 1, 2001
Accepted April 1, 2002

Unspecific and side effects caused by interaction with proteins belong to common problems of many structures synthesized as potential medicaments. Possible in vitro interactions with proteins of a group of phenylsulfonyl benzoic acid derivatives (VÚFB 19363, 19369, 19370, 19371, and 19760) as new potential anti-inflammatory compounds with antileukotrienic activities were studied in the present work. Three purified enzymes were used as model proteins with catalytic activities: Pig heart aspartate aminotransferase (AST, EC, alanine aminotransferase (ALT, EC, and glutamate decarboxylase (GAD, EC from E. coli. Catalytic activities during incubation of individual compounds (6 x 10-5 M solution to 5 x 10-2 M suspension) at 37 °C with enzymes served as criteria of stability and function of the proteins. No immediate influence of any compound studied on enzyme activities was found. Aminotransferase activities were not affected even during incubation up to 20 d. In the case of GAD, the compounds VÚFB 19369, 19370, 19371, and 19760 had stabilizing influence on GAD activity during incubation at enzyme concentrations of 11.25 and 5.62 mg prot/l. The lack of an immediate effect of compounds and the stability of enzymes during incubation them are favorable and support the prospective of the compounds as potential drugs.


This work was supported by the Research project LN00B125 of Czech Ministry of Education.


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