来自尼泊尔原产的Zanthoxylum armatumDC的强有力的ROS抑制剂
Janaki Baral1,2, Dipesh Shrestha2, Hari Prasad Devkota3
1Central Department of Chemistry, Tribhuvan University, Kathmandu, Nepal.
Natural product research
|October 3, 2023
概括
桑托西 (Zanthoxylum armatum) 产生的坦布林和普鲁多梅斯是活性氧物种 (ROS) 的强有力的抑制剂和抗氧化剂. 这些化合物表现出有希望的抗炎性质和有利的类似药物的特征.
科学领域:
- 自然产品化学 自然产品化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- 反应性氧物种 (ROS) 与各种炎症状况有关.
- 药用植物的植物化学研究是新型治疗剂的重要来源.
- 桑托西 (Zanthoxylum armatum) 传统上是因为其药用特性而被使用的.
研究的目的:
- 从Zanthoxylum armatum中分离和描述生物活性化合物.
- 评估分离化合物的ROS抑制和抗氧化潜力.
- 通过分子对接和药物相似性预测来研究抗炎机制.
主要方法:
- 在生物试验指导下分化Zanthoxylum armatum乙烯酸提取物.
- 使用质谱法和核磁共振 (NMR) 谱法阐明结构.
- 在体外抗氧化剂和ROS抑制测定,对抗COX-2的分子对接,以及ADMET预测.
主要成果:
- 坦布林 (1) 和普鲁多梅斯 (2) 被分离并鉴定出来.
- 这两种化合物都显示出显著的ROS抑制 (IC50值:7.5±0.3和1.5±0.3μg/mL) 和抗氧化活性 (IC50值:32.65±0.31和26.96±0.19μg/mL).
- 分子对接显示出强烈的结合亲和力与COX-2 (-8.4到-8.6千卡/mol),优于易布洛芬 (-7.7千卡/mol),具有有利的ADMET配置文件.
结论:
- 坦布林和普鲁多梅斯是强大的ROS抑制剂和抗氧化剂,具有潜在的抗炎活性.
- 这些化合物表现出有利的类似药物的特性和良好的胃肠道吸收.
- 桑托西 (Zanthoxylum armatum) 是一种新型抗炎药物的宝贵来源.
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