新的神经保护性衍生物的 cinnamic 酸通过生物转化
Hadeer Elkharsawy1, Ramadan A Eldomany2, Amira Mira3,4
1Department of Pharmacognosy, Faculty of Pharmacy, Kafr El-Sheikh University, Kafr El-Sheikh 33516, Egypt.
Food & function
|March 26, 2024
概括
肉酸的微生物转化产生了具有显著药理潜力的新衍生物. 这些化合物有望通过向炎症,神经毒性和胆固醇缺乏症来治疗神经退行性疾病.
科学领域:
- 生物技术和微生物化学
- 药理学和药物发现
- 神经科学和神经保护 神经科学和神经保护
背景情况:
- 锡南酸具有已知的药理特性.
- 微生物转化是产生新生物活性化合物的关键策略.
- 开发神经退行性疾病的新疗法是一个关键的研究领域.
研究的目的:
- 通过微生物转化生产新的肉酸衍生物.
- 评估这些衍生物的循环氧化酶 (COX),乙胆化酶 (AChE) 抑制和神经保护作用.
- 探索这些代谢物的潜力,作为神经退行性疾病的治疗剂.
主要方法:
- 为了生物转化肉酸,采用了两阶段发酵协议.
- 五种代谢物被分离和鉴定出来,其中包括两种新衍生物:N-propyl cinnamamide和2-methyl heptyl benzoate.
- 实验室试验用于评估SH-SY5Y细胞中COX和ACHE抑制,以及对H2O2和Aβ1-42诱导毒性的神经保护. 此外,还进行了in silico研究.
主要成果:
- 代谢物4 (p-基酸) 显示出强大的COX-2抑制 (IC50 = 1.85 ± 0.07μM).
- 代谢物2 (N-propyl cinnamamide) 呈现出乙胆酶 (AChE) 抑制活性 (IC50 = 8.27 μM).
- 代谢物3 (2-甲基乙基酸盐) 与阳性对照组相比,对抗氧化和粉胺诱导的神经毒性产生更好的神经保护作用.
结论:
- 该研究成功地产生了具有显著生物活性的新型肉酸衍生物.
- 代谢物2,3和4显示出治疗神经退行性疾病的潜力.
- 这些发现强调了微生物转化在神经系统疾病的药物发现中的有用性.
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