Aim. To assess the antioxidants effectiveness (ascorbic acid, methylethylpiridinol, N-acetylcysteine) in reducing the gentamicin-induced nephrotoxicity in experimental infection caused by Escherichia coli or Klebsiella pneumoniae.Methods. The experiment was divided into two parts. In the first part, the effect of antioxidants on the sensitivity of bacteria to gentamicin in vitro according to changing the optical density of the bacterial suspension, in the second part - nephroprotective activity of antioxidants and their effects on antibiotic activity in experimental bacterial peritonitis were evaluated.Results. All antioxidants significantly reduce the sensitivity of E. coli to gentamicin in vitro, and the level of effect is directly proportional to the antioxidant concentration. Methylethylpiridinol has the most pronounced antagonistic action against gentamicin. It is found that methylethylpiridinol at a concentration of 4 mmol/l enhances development of Escherichia coli strain by 7 times by the 6th hour of incubation. Ascorbic acid and N-acetylcysteine have a similar probacterial activity profile. In the incubation mixtures containing a strain of Klebsiella pneumoniae, a similar pattern of increase in bacterial biomass optical density was observed with maximum values in the presence of the highest concentrations of antioxidants. In experimental infection, antioxidants reduce the activity of gentamicin against Escherichia coli and Klebsiella pneumoniae, without reducing the antibiotic nephrotoxicity.Conclusion. Ascorbic acid, methylethylpiridinol and N-acetylcysteine reduce the antibacterial activity of gentamicin against Escherichia coli and Klebsiella pneumoniae in vitro and in vivo, in a dose of 80 mg/kg they do not reduce gentamicin nephrotoxicity in bacterial peritonitis in rats; their use in the course of treatment with gentamicin is not only irrational, but also contraindicated.
The article discusses university information system (IS) development as a digital transformation process. It is noted that automating the development and implementation of educational programs (EP) provides a basis for educational environment digitization. Moreover, it is the main criterion of the extent of the university’s digital transformation.The article analyzes the current state of educational environment digitization at universities and highlights the necessity of using automation tools to form the structure and content of EPs. It is necessary to develop an automated technology for designing EPs at the state level. The technology will enable teachers to automatically comply with the requirements for EP structure and content, to develop EPs to a high methodological standard, and promptly bring them to all educational institutions.The article reveals the specifics of the project to automate the development of higher education EPs drawing on the example of Siberian State Medical University (SibMed). The possibility of solving this problem is based on employing the software product Intellect Info: Educational programs (1С:University PROF extension). The research proposes technological solutions for creating the content of higher education EPs. These solutions take into account professional (occupational) standards, the requirements of the Federal State Educational Standard 3++. The article also outlines methods of the automated formation of competencies achievement indicators, EP description, and the preparation of working programs for disciplines.The research discusses the possibility of developing the IS of any Russian university to solve the problems of forming the content of higher education EP on the basis of 1C:University PROF.
The aim of the work is to conduct an analytical review of the results of preclinical studies of levosalbutamol. The review discusses the pharmacodynamic features of the R-stereoisomer of salbutamol in vitro. The chemical bases of interaction of levosalbutamol with β 2 -adrenoreceptors, intracellular signaling cascades associated with β 2 -adrenoreceptors, and structural features of clinically significant ligands of β 2 -adrenoreceptors are presented. Broncholytic activity, influence on the contractility of the diaphragmatic muscles, mucociliary clearance of R-salbutamol in comparison with racemic salbutamol are described. The data presented indicate that all known β 2 -adrenergic receptor-dependent effects of racemic salbutamol, including bronchodilation, are realized by its R-enantiomer. There is evidence that the regular inhalation administration of racemic salbutamol is accompanied by a partial decrease in the bronchoprotective effect and an increase in airway hyperreactivity in response to the action of provocative factors. It was found that the development of hyperreactivity of the respiratory tract is excluded in the case of regular inhalation of levosalbutamol. Possible mechanisms of the paradoxical bronchoconstrictor effect of the salbutamol dystomer are described. This article shows the beneficial effect of levosalbutamol on mucociliary clearance, its anti-inflammatory activity and antiallergic effect. The image data are compared between the enantiomers and the racemate of salbutamol. Special attention is paid to the pharmacokinetics of enantiomers of salbutamol. The data presented from the preclinical studies provide evidence of chiral inversion of stereoisomers of salbutamol.Левосальбутамол как альтернатива лекарственным препаратам на основе рацемического сальбутамола: обзор результатов доклинических исследований А. Г. Мирошниченко, Я. С. Булгакова, В. Ю. Перфильев, Н. Г. Базарнова Алтайский государственный университет, Барнаул, РоссияПроанализированы результаты доклинических исследований лекарственного средства левосальбутамол. Обсуждаются фармакодинамические особенности R-стереоизомера сальбутамола in vitro. Представлены химические основы взаимодействия левосальбутамола с β 2 -адренорецепторами, внутриклеточные сигнальные каскады, ассоциированные с β 2 -адренорецепторами, а также структурные особенности клинически значимых лигандов β 2 -адренорецепторов. Описана бронхолитическая активность, влияние на контрактильность диафрагмальных мышц, мукоцилиарный клиренс R-сальбутамола по сравнению с рацемическим сальбутамолом. Приведены данные, которые указывают на то, что все известные β 2 -адренорецепторзависимые эффекты рацемического сальбутамола, включая бронходилатацию, реализуются за счет его R-энантиомера. Имеются свидетельства того, что регулярное ингаляционное введение рацемического сальбутамола сопровождается парциальным снижением бронхопротективного эффекта и увеличением гиперреактивности дыхательных путей в ответ на действие провокационных факторов. При этом развитие гиперреактивности дыхательных п...
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