Department of Pharmacy University of Malakand, Dir (L) Pakistan.
Department of Pharmacology & Toxicology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
Future Med Chem. 2024 Aug 17;16(16):1649-1663. doi: 10.1080/17568919.2024.2363713. Epub 2024 Jun 28.
To synthesize aurone (Ar) derivatives and to demonstrate their effects against diabetes mellitus (DM) and neurodegeneration. Five Ar () 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. 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. Synthesized Ar () exhibits promising therapeutic potential against STZ-induced neurodegeneration and DM by modulating inflammatory and oxidative pathways, suggesting a novel avenue for disease management.
合成橙酮 (Ar) 衍生物并研究其对糖尿病 (DM) 和神经退行性变的作用。合成了 5 种 Ar () 衍生物,通过质子 NMR 进行了表征,并筛选了其抗氧化、抗糖尿病和抗胆碱酯酶活性。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。在橙酮衍生物中,ArE 显示出对认知障碍、氧化应激和神经炎症的显著逆转作用。生化分析显示出抗糖尿病和神经保护作用,可能是通过下调炎症标志物和上调抗氧化酶来实现的。合成的 Ar () 通过调节炎症和氧化途径,显示出对 STZ 诱导的神经退行性变和 DM 有潜在的治疗作用,为疾病管理提供了新途径。