New Amino-Anthracene-9, 10-Dione Derivatives: Synthesis and Pharmacological Evaluation as Powerful Neuroprotective and Antidepressant Agents

Q3 Pharmacology, Toxicology and Pharmaceutics International Journal of Pharmaceutical Quality Assurance Pub Date : 2023-09-25 DOI:10.25258/ijpqa.14.3.50
Chandrakant Suryawanshi, Rajendra Wagh
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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.
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新的氨基蒽- 9,10 -二酮衍生物:合成及其作为强效神经保护和抗抑郁药物的药理评价
在对天然存在的蒽醌的靶向评估中,利用了重组人MAOs的两种异构体。这项关于蒽醌、紫外光素和茜素的研究提供了有希望的新信息,可能最终被用作发现独特的合成蒽醌、蒽9,10 -二酮化合物1至9的先导分子。在96孔黑色聚苯乙烯微滴板上,对9种不同的合成蒽9,10-二酮化合物的MAOs抑制作用进行了评价。
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来源期刊
International Journal of Pharmaceutical Quality Assurance
International Journal of Pharmaceutical Quality Assurance Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
0.80
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0.00%
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0
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.
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