Synthesis, characterization and biological evaluation of aurones as potential neuroprotective agents.

IF 3.2 4区医学 Q3 CHEMISTRY, MEDICINAL Future medicinal chemistry Pub Date : 2024-08-17 Epub Date: 2024-06-28 DOI:10.1080/17568919.2024.2363713

Muhammad Ayaz, Syed Wadood Ali Shah, Mohammad Shoaib, Fawad Ali Shah, Fawad Ahmed

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Abstract

Aim: To synthesize aurone (Ar) derivatives and to demonstrate their effects against diabetes mellitus (DM) and neurodegeneration.Materials & methods: Five Ar (A-E) derivatives were synthesized, characterized by proton NMR and screened for antioxidant, anti-diabetic and anti-cholinesterase activities. They were further evaluated for neuroprotective effects in streptozotocin (STZ)-induced neurodegenerative model.Results: Among the aurone derivatives ArE demonstrated significant reversal of cognitive impairment, oxidative stress and neuroinflammation. Biochemical analysis revealed anti-diabetic and neuroprotective effects, possibly through downregulation of inflammatory markers and upregulation of antioxidant enzymes.Conclusion: Synthesized Ar (A-E) exhibits promising therapeutic potential against STZ-induced neurodegeneration and DM by modulating inflammatory and oxidative pathways, suggesting a novel avenue for disease management.

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作为潜在神经保护剂的醛酮的合成、表征和生物学评估。

目的：合成枳实（Ar）衍生物，并证明其对糖尿病（DM）和神经变性的作用。材料与方法：合成了五种 Ar（A-E）衍生物，对其进行了质子核磁共振表征，并对其抗氧化、抗糖尿病和抗胆碱酯酶活性进行了筛选。进一步评估了它们在链脲佐菌素（STZ）诱导的神经退行性模型中的神经保护作用。结果在醛酮衍生物中，ArE 能显著逆转认知障碍、氧化应激和神经炎症。生化分析显示了抗糖尿病和神经保护作用，这可能是通过下调炎症标志物和上调抗氧化酶实现的。结论合成的 Ar（A-E）通过调节炎症和氧化途径，对 STZ 诱导的神经变性和 DM 具有良好的治疗潜力，为疾病治疗提供了一条新途径。

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来源期刊

Future medicinal chemistry CHEMISTRY, MEDICINAL-

CiteScore

5.80

自引率

2.40%

发文量

118

审稿时长

4-8 weeks

期刊介绍： Future Medicinal Chemistry offers a forum for the rapid publication of original research and critical reviews of the latest milestones in the field. Strong emphasis is placed on ensuring that the journal stimulates awareness of issues that are anticipated to play an increasingly central role in influencing the future direction of pharmaceutical chemistry. Where relevant, contributions are also actively encouraged on areas as diverse as biotechnology, enzymology, green chemistry, genomics, immunology, materials science, neglected diseases and orphan drugs, pharmacogenomics, proteomics and toxicology.