Antiulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate in ethanol-prednisolone damage to gastric mucosa

Nowadays, the search for new effective and safe medicines for the treatment of acid-dependent gastrointestinal diseases remains an urgent problem of modern pharmacology.The aim of this study was an experimentally study of the anti-ulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimida...

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Main Authors: M. V. Chernikov, M. A. Oganova, S. A. Kalashnikova, L. V. Polyakova, N. A. Khromova
Format: Article
Language:Russian
Published: Volgograd State Medical University, Pyatigorsk Medical and Pharmaceutical Institute 2020-01-01
Series:Фармация и фармакология (Пятигорск)
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Online Access:https://www.pharmpharm.ru/jour/article/view/554
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author M. V. Chernikov
M. A. Oganova
S. A. Kalashnikova
L. V. Polyakova
N. A. Khromova
author_facet M. V. Chernikov
M. A. Oganova
S. A. Kalashnikova
L. V. Polyakova
N. A. Khromova
author_sort M. V. Chernikov
collection DOAJ
description Nowadays, the search for new effective and safe medicines for the treatment of acid-dependent gastrointestinal diseases remains an urgent problem of modern pharmacology.The aim of this study was an experimentally study of the anti-ulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate on the model of damage to the gastric mucosa caused by the administration of 80% ethanol and prednisolone combination (20 mg/kg).Materials and methods. To simulate the damage to the gastric mucosa, the experimental animals (white male Wistar rats) were administrated with prednisone at the rate of 20 mg/kg and 80% ethyl alcohol at the dose of 0.6 ml/100 g of the animal body weight. Prednisolone was dissolved in 80% alcohol. Antisecretory antiulcer agents actively used in clinical practice, were selected as reference drugs: ranitidine (30 mg/kg, 10 mg/kg and 3 mg/kg) and omeprazole (3 mg/kg, 1 mg/kg and 0.3 mg/kg). The studied compound was used at the doses of 30 mg/kg, 10 mg/kg and 3 mg/kg. All the substances under study were administered intragastrically with the use of an atraumatic probe. Results. It has been established that the benzimidazole derivative in the studied doses contributes to a dose-dependent reliable reduction in the area and depth of ulcerative lesions of the gastric mucosae relative to the control and reference drugs (ranitidine and omeprazole). In addition, in the maximum studied dose (30 mg/kg), the proportion of the animals with ulcerative lesions significantly decreases by more than 2 times. The calculated ED50 values for the benzimidazole derivative and ranitidine were 5.09 mg/kg and 38.23 mg/kg, respectively.Conclusion. The obtained experimental data indicate that the benzimidazole derivative has a pronounced dose-dependent antiulcer effect on the model of ethanol-prednisolone erosive-ulcerous defects of the rats’ gastric mucosae, which is superior to the effects of the reference preparations. It makes its further study promising.
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spelling doaj-art-0efb1ba475b8483d984aef8d6d8f7f332025-08-20T03:21:16ZrusVolgograd State Medical University, Pyatigorsk Medical and Pharmaceutical InstituteФармация и фармакология (Пятигорск)2307-92662413-22412020-01-017633934510.19163/2307-9266-2019-7-6-339-345328Antiulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate in ethanol-prednisolone damage to gastric mucosaM. V. Chernikov0M. A. Oganova1S. A. Kalashnikova2L. V. Polyakova3N. A. Khromova4Pyatigorsk Medical and Pharmaceutical Institute – branch of Volgograd State Medical UniversityPyatigorsk Medical and Pharmaceutical Institute – branch of Volgograd State Medical UniversityPyatigorsk Medical and Pharmaceutical Institute – branch of Volgograd State Medical UniversityPyatigorsk Medical and Pharmaceutical Institute – branch of Volgograd State Medical UniversityPyatigorsk Medical and Pharmaceutical Institute – branch of Volgograd State Medical UniversityNowadays, the search for new effective and safe medicines for the treatment of acid-dependent gastrointestinal diseases remains an urgent problem of modern pharmacology.The aim of this study was an experimentally study of the anti-ulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate on the model of damage to the gastric mucosa caused by the administration of 80% ethanol and prednisolone combination (20 mg/kg).Materials and methods. To simulate the damage to the gastric mucosa, the experimental animals (white male Wistar rats) were administrated with prednisone at the rate of 20 mg/kg and 80% ethyl alcohol at the dose of 0.6 ml/100 g of the animal body weight. Prednisolone was dissolved in 80% alcohol. Antisecretory antiulcer agents actively used in clinical practice, were selected as reference drugs: ranitidine (30 mg/kg, 10 mg/kg and 3 mg/kg) and omeprazole (3 mg/kg, 1 mg/kg and 0.3 mg/kg). The studied compound was used at the doses of 30 mg/kg, 10 mg/kg and 3 mg/kg. All the substances under study were administered intragastrically with the use of an atraumatic probe. Results. It has been established that the benzimidazole derivative in the studied doses contributes to a dose-dependent reliable reduction in the area and depth of ulcerative lesions of the gastric mucosae relative to the control and reference drugs (ranitidine and omeprazole). In addition, in the maximum studied dose (30 mg/kg), the proportion of the animals with ulcerative lesions significantly decreases by more than 2 times. The calculated ED50 values for the benzimidazole derivative and ranitidine were 5.09 mg/kg and 38.23 mg/kg, respectively.Conclusion. The obtained experimental data indicate that the benzimidazole derivative has a pronounced dose-dependent antiulcer effect on the model of ethanol-prednisolone erosive-ulcerous defects of the rats’ gastric mucosae, which is superior to the effects of the reference preparations. It makes its further study promising.https://www.pharmpharm.ru/jour/article/view/5542-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate, antiulcer action, ethanol-prednisolone damages / injuries, preclinical studies
spellingShingle M. V. Chernikov
M. A. Oganova
S. A. Kalashnikova
L. V. Polyakova
N. A. Khromova
Antiulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate in ethanol-prednisolone damage to gastric mucosa
Фармация и фармакология (Пятигорск)
2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate, antiulcer action, ethanol-prednisolone damages / injuries, preclinical studies
title Antiulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate in ethanol-prednisolone damage to gastric mucosa
title_full Antiulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate in ethanol-prednisolone damage to gastric mucosa
title_fullStr Antiulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate in ethanol-prednisolone damage to gastric mucosa
title_full_unstemmed Antiulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate in ethanol-prednisolone damage to gastric mucosa
title_short Antiulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate in ethanol-prednisolone damage to gastric mucosa
title_sort antiulcer activity of 2 phenyl 9 diethylaminoethylimidazo 1 2 a benzimidazole dinitrate in ethanol prednisolone damage to gastric mucosa
topic 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate, antiulcer action, ethanol-prednisolone damages / injuries, preclinical studies
url https://www.pharmpharm.ru/jour/article/view/554
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