醇的神经保护作用:在体外和在体内进行研究
Yhiya Amen1, Ahmed Othman2, Ahmed M Sayed3,4
1Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.
Natural product research
|April 26, 2025
概括
一种天然化合物Coixol通过抑制乙胆化酶 (AChE) 和降低氧化应激,表现出神经保护作用. 它还破坏了粉样β (Aβ) 原纤维,为新的神经保护药物开发提供了潜力.
科学领域:
- 自然产品化学 自然产品化学
- 神经药理学神经药理学
- 计算化学计算化学
背景情况:
- 神经退行性疾病的特点是氧化应激和粉样β (Aβ) 聚合.
- 乙胆酶 (AChE) 抑制剂是治疗认知衰退的治疗策略.
- 自然化合物为新药发现提供了丰富的来源.
研究的目的:
- 研究来自Coix lacryma-jobi的化合物coixol的神经保护潜力.
- 阐明coixol对ACHE活性,氧化应激和Aβ聚合的影响的分子机制.
主要方法:
- 在体外酶定量测试以测量ACHE抑制.
- 使用SH-SY5Y细胞进行基于细胞的测定,以评估对神经毒性的保护.
- 分子对接和高斯加速分子动力学 (GaMD) 模拟以研究coixol-Aβ相互作用.
主要成果:
- 科伊克索尔显著抑制了AChE (IC50 = 3.63μM),相当于塔克林.
- 科伊索尔以剂量依赖的方式保护SH-SY5Y细胞免受H2O2和Aβ诱导的神经毒性.
- GaMD模拟显示了coixol破坏Aβ原纤维结构的能力.
结论:
- 科伊索尔表现出多目标神经保护性质.
- 科伊克索尔的机制涉及ACHE抑制,抗氧化作用和Aβ聚合破坏.
- 科伊克索尔是开发新型神经保护剂的有希望的化合物.
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