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Siberian Scientific Medical Journal

2018 year, number 2

ANTIULCER AND ANTI-INFLAMMATORY ACTIVITY OF THE CAMPHOLENIC ALDEHYDE-DERIVED THIAZOLIDINONE

Marina Sergeevna BORISOVA, Dmitriy Nikolaevich SOKOLOV, Natalya Anatolevna ZHUKOVA, Tatyana Genrikhovna TOLSTIKOVA, Nariman Faridovich SALAKHUTDINOV
N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry of SB RAS
Keywords: тиазолидинон, противоязвенная активность, противовоспалительная активность, этаноловая язва, ацетатная язва, гистаминовый отек

Abstract

The research objective was the study of antiulcer and anti-inflammatory activity of the 3-[3-(morpholine-4-yl)propyl]-2-[(2,2,3-trimethylcyclopent-3-en-1-yl)methyl]-1,3-thiazolydin-4-one. Material and methods. The study was performed on 24 male outbred mice and 102 female Wistar rats. The investigation of antiulcer activity of the substance as a preventive medication in comparison with omeprazole and famotidine was carried out on 24 rats using the 96 % ethanol-induced gastric ulcer test. The ethanol-induced lesion area was measured to evaluate the antiulcerogenic activity. The curative effect of the compound was studied on 78 female rats using the chronic acetic acid-induced model on the 5th, 10th, 15th, and 25th day of administration, omeprazole being used as a reference drug. A diameter of the ulcers was measured and a histological investigation of the gastric tissue samples including leukocyte counting was performed to estimate the influence on the regeneration process. Anti-inflammatory activity of the substance in comparison with diclofenac was studied on mice using histamine-induced edema model. Results and discussion. The substance of interest was shown to possess antiulcerogenic action comparable to the activity of omeprazole on ethanol-induced ulcer whereas famotidine did not exhibit gastroprotective properties. The administration of the agent did not lead to a significant decrease of acetic acid-induced ulcer size, whereas omeprazole promoted the marked reduction of the lesion area on the 15th and 25th day of the experiment. There were no significant morphological differences observed between the experimental groups. Notably, the administration of the substance under investigation resulted in significant decreasing of leukocyte quantity in the ulcer margins. The marked anti-inflammatory action of the substance similar to the effect of diclofenac was demonstrated on the histamine-induced edema model.