G Arajyan, Q Navoyan, N Pahutyan, H Hunanyan, A Pogosyan, H Gasparyan
{"title":"草酸二酰胺衍生物抗氧化活性及其对白鼠脑和肝组织中丙二醛浓度影响的综合研究。","authors":"G Arajyan, Q Navoyan, N Pahutyan, H Hunanyan, A Pogosyan, H Gasparyan","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>The wide range of chemical structures of antioxidants provides opportunities for individual selection of the most suitable compounds, taking into account the unique needs and characteristics of the body. Synthetic antioxidants can be specially designed with certain characteristics, which helps to create more effective and stable compounds. The aim of this work was to conduct a series of studies to identify the antioxidant activity of newly synthesized compounds of a number of oxalic acid diamides based on 3,4-dimethoxyphenylcyclopentylamine N1 ((1-3,4-dimethoxyphenyl)methyl)-N2-(2-methoxyphenyl)oxalamide on the content of malondialdehyde (MDA) in the brain and liver tissues of white rats (in vivo, in vitro), as well as to determine their potential pharmacological properties that correspond to Lipinsky's \"Rule of Five\" (in silico).</p><p><strong>Material and methods: </strong>The studies were conducted on white male rats weighing 180-200 g, kept on a normal diet. The brain and liver were washed with physiological solution, purified from vessels and homogenized in Tris-HCl buffer. The level of lipid peroxides was determined in a non-enzymatic peroxidation system by the yield of the final product - (MDA), which forms a complex compound with thiobarbituric acid in the form of a chromogen (trimethine complex).</p><p><strong>Results and discussion: </strong>As a result of the conducted studies, it was established that the synthesized compounds exhibit antioxidant properties with varying degrees of effectiveness. The most pronounced activity was demonstrated by compound 1.24.50 both in liver tissue and in brain tissue. The least activity, both in liver tissue and in brain tissue, was demonstrated by compound 1.24.43. In addition, all physicochemical descriptors of the studied compounds correspond to Lipinsky's \"Rule of Five\". These data confirm the prospects of further studies of these compounds as potential sources for the development of new molecules for the treatment of oxidative stress.</p><p><strong>Conclusion: </strong>Analysis of the obtained data allows us to conclude that the studied compounds demonstrate antioxidant properties, helping to protect cells from oxidative stress. These results are of significant importance for the prevention and treatment of diseases associated with increased levels of free radicals.</p>","PeriodicalId":12610,"journal":{"name":"Georgian medical news","volume":" 352-353","pages":"18-23"},"PeriodicalIF":0.0000,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"COMPREHENSIVE STUDY OF ANTIOXIDANT ACTIVITY OF OXALIC ACID DIAMIDE DERIVATIVES AND THEIR EFFECT ON THE CONCENTRATION OF MALONIC DIALDEHYDE IN THE BRAIN AND LIVER TISSUES OF WHITE RATS.\",\"authors\":\"G Arajyan, Q Navoyan, N Pahutyan, H Hunanyan, A Pogosyan, H Gasparyan\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The wide range of chemical structures of antioxidants provides opportunities for individual selection of the most suitable compounds, taking into account the unique needs and characteristics of the body. Synthetic antioxidants can be specially designed with certain characteristics, which helps to create more effective and stable compounds. The aim of this work was to conduct a series of studies to identify the antioxidant activity of newly synthesized compounds of a number of oxalic acid diamides based on 3,4-dimethoxyphenylcyclopentylamine N1 ((1-3,4-dimethoxyphenyl)methyl)-N2-(2-methoxyphenyl)oxalamide on the content of malondialdehyde (MDA) in the brain and liver tissues of white rats (in vivo, in vitro), as well as to determine their potential pharmacological properties that correspond to Lipinsky's \\\"Rule of Five\\\" (in silico).</p><p><strong>Material and methods: </strong>The studies were conducted on white male rats weighing 180-200 g, kept on a normal diet. The brain and liver were washed with physiological solution, purified from vessels and homogenized in Tris-HCl buffer. The level of lipid peroxides was determined in a non-enzymatic peroxidation system by the yield of the final product - (MDA), which forms a complex compound with thiobarbituric acid in the form of a chromogen (trimethine complex).</p><p><strong>Results and discussion: </strong>As a result of the conducted studies, it was established that the synthesized compounds exhibit antioxidant properties with varying degrees of effectiveness. The most pronounced activity was demonstrated by compound 1.24.50 both in liver tissue and in brain tissue. The least activity, both in liver tissue and in brain tissue, was demonstrated by compound 1.24.43. In addition, all physicochemical descriptors of the studied compounds correspond to Lipinsky's \\\"Rule of Five\\\". These data confirm the prospects of further studies of these compounds as potential sources for the development of new molecules for the treatment of oxidative stress.</p><p><strong>Conclusion: </strong>Analysis of the obtained data allows us to conclude that the studied compounds demonstrate antioxidant properties, helping to protect cells from oxidative stress. These results are of significant importance for the prevention and treatment of diseases associated with increased levels of free radicals.</p>\",\"PeriodicalId\":12610,\"journal\":{\"name\":\"Georgian medical news\",\"volume\":\" 352-353\",\"pages\":\"18-23\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Georgian medical news\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Georgian medical news","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"Medicine","Score":null,"Total":0}
COMPREHENSIVE STUDY OF ANTIOXIDANT ACTIVITY OF OXALIC ACID DIAMIDE DERIVATIVES AND THEIR EFFECT ON THE CONCENTRATION OF MALONIC DIALDEHYDE IN THE BRAIN AND LIVER TISSUES OF WHITE RATS.
The wide range of chemical structures of antioxidants provides opportunities for individual selection of the most suitable compounds, taking into account the unique needs and characteristics of the body. Synthetic antioxidants can be specially designed with certain characteristics, which helps to create more effective and stable compounds. The aim of this work was to conduct a series of studies to identify the antioxidant activity of newly synthesized compounds of a number of oxalic acid diamides based on 3,4-dimethoxyphenylcyclopentylamine N1 ((1-3,4-dimethoxyphenyl)methyl)-N2-(2-methoxyphenyl)oxalamide on the content of malondialdehyde (MDA) in the brain and liver tissues of white rats (in vivo, in vitro), as well as to determine their potential pharmacological properties that correspond to Lipinsky's "Rule of Five" (in silico).
Material and methods: The studies were conducted on white male rats weighing 180-200 g, kept on a normal diet. The brain and liver were washed with physiological solution, purified from vessels and homogenized in Tris-HCl buffer. The level of lipid peroxides was determined in a non-enzymatic peroxidation system by the yield of the final product - (MDA), which forms a complex compound with thiobarbituric acid in the form of a chromogen (trimethine complex).
Results and discussion: As a result of the conducted studies, it was established that the synthesized compounds exhibit antioxidant properties with varying degrees of effectiveness. The most pronounced activity was demonstrated by compound 1.24.50 both in liver tissue and in brain tissue. The least activity, both in liver tissue and in brain tissue, was demonstrated by compound 1.24.43. In addition, all physicochemical descriptors of the studied compounds correspond to Lipinsky's "Rule of Five". These data confirm the prospects of further studies of these compounds as potential sources for the development of new molecules for the treatment of oxidative stress.
Conclusion: Analysis of the obtained data allows us to conclude that the studied compounds demonstrate antioxidant properties, helping to protect cells from oxidative stress. These results are of significant importance for the prevention and treatment of diseases associated with increased levels of free radicals.