{"title":"New Amino-Anthracene-9, 10-Dione Derivatives: Synthesis and Pharmacological Evaluation as Powerful Neuroprotective and Antidepressant Agents","authors":"Chandrakant Suryawanshi, Rajendra Wagh","doi":"10.25258/ijpqa.14.3.50","DOIUrl":null,"url":null,"abstract":"The monoamine oxidase (MAO) enzyme resides in the outer mitochondrial membranes of all body cells, including the ones found in the brain, liver, and intestinal mucosa. Dopamine, serotonin, norepinephrine, tyramine, and tryptamine are extrinsic and indigenous amines that MAO oxidatively deaminates. MAO-A has been correlated with depression and other mental health issues, while MAO-B has been associated with the conditions Alzheimer’s and Parkinson’s disease. In a targeted assessment of naturally occurring anthraquinones, two isoforms of recombinant human MAOs were utilized. The inhibitory effects of purpurin and alizarin on MAO-A were observed, with calculated IC50 values of 2.50 and 30.1 M, respectively. This research on anthraquinones, purpurin, and alizarin offers promising new information that might eventually be used as a lead molecule in the discovery of the unique synthetic anthraquinones, anthracene 9, 10-dione compounds 1 to 9. On 96-well black polystyrene microtiter plates, both MAOs inhibiting action of 9 distinct synthetic anthracene 9,10-dione compounds has been evaluated. Compared to clorgyline, compounds 1, 2, 5, 8, and 9 inhibit MAO-A significantly, while compounds 1, 3, 5, 8, and 9 considerably inhibit MAO-B. Significant findings indicate that these compounds may be beneficial When employed to treat depression owing to their intense selective MAO-B activity and antidepressant effects as a result of their selective MAO-inhibition.","PeriodicalId":14260,"journal":{"name":"International Journal of Pharmaceutical Quality Assurance","volume":"30 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2023-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Pharmaceutical Quality Assurance","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.25258/ijpqa.14.3.50","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 0
Abstract
The monoamine oxidase (MAO) enzyme resides in the outer mitochondrial membranes of all body cells, including the ones found in the brain, liver, and intestinal mucosa. Dopamine, serotonin, norepinephrine, tyramine, and tryptamine are extrinsic and indigenous amines that MAO oxidatively deaminates. MAO-A has been correlated with depression and other mental health issues, while MAO-B has been associated with the conditions Alzheimer’s and Parkinson’s disease. In a targeted assessment of naturally occurring anthraquinones, two isoforms of recombinant human MAOs were utilized. The inhibitory effects of purpurin and alizarin on MAO-A were observed, with calculated IC50 values of 2.50 and 30.1 M, respectively. This research on anthraquinones, purpurin, and alizarin offers promising new information that might eventually be used as a lead molecule in the discovery of the unique synthetic anthraquinones, anthracene 9, 10-dione compounds 1 to 9. On 96-well black polystyrene microtiter plates, both MAOs inhibiting action of 9 distinct synthetic anthracene 9,10-dione compounds has been evaluated. Compared to clorgyline, compounds 1, 2, 5, 8, and 9 inhibit MAO-A significantly, while compounds 1, 3, 5, 8, and 9 considerably inhibit MAO-B. Significant findings indicate that these compounds may be beneficial When employed to treat depression owing to their intense selective MAO-B activity and antidepressant effects as a result of their selective MAO-inhibition.
期刊介绍:
INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE is a quarterly international journal publishing the finest peer-reviewed research in the field of Pharmaceutical Quality Assurance and Pharmaceutical Analysis on the basis of its originality, importance, disciplinary interest, timeliness, accessibility, elegance, and surprising conclusions. IJPQA also provides rapid, authoritative, insightful and arresting news and interpretation of topical and coming trends affecting science, scientists and the wider public.