使用果模型从草药中发现用于治疗石病的活性化合物的简化策略
Yunuo Ren1, Wen Zhang1, Youxin Li1
1School of Pharmaceutical Science and Technology, Faculty of Medicine, Tianjin University, Tianjin, China.
Journal of ethnopharmacology
|April 25, 2025
概括
这项研究开发了一种果模型,以快速识别用于治疗结石的传统中医药 (TCM) 的活性化合物. 在小鼠中发现并验证了三种化合物,显示出新疗法的潜力.
科学领域:
- 药理学 药理学是指药理学的学科.
- 自然产品 化学 化学
- 药物发现 药物发现 药物发现
背景情况:
- 传统中医药 (TCM) 具有治疗结石 (结石) 的潜力,副作用较少.
- 复杂的TCM成分挑战了活性化合物和治疗机制的识别.
- 动物模型对于调查结石治疗中TCM机制至关重要.
研究的目的:
- 通过Drosophila melanogaster (果) 模型建立一种快速策略,用于识别TCM中的新型活性成分.
- 在果模型中选候选TCM对结石的疗效.
- 从有效的TCM中分离,识别和验证活性化合物.
主要方法:
- 开发了一种果结石模型,通过诱导马尔皮吉亚管道 (MTs) 中用氧酸盐 (NaOx) 结晶.
- 使用LC-MS和NMR选TCM水提取物,分化有效的水提取物,并确定核心化合物.
- 通过DHE染色,RT-qPCR和体外测试来探索治疗机制,在小鼠模型中验证发现.
主要成果:
- 在果模型中确定了三种TCM (洪华,丹申,黄) 对结石有效.
- 发现并分离了三个核心活性化合物:氧糖花黄色A (HYA),沙尔维安酸A (SAA) 和Calycosin-7-O-β-D-glucoside (CG).
- HYA,SAA和CG抑制了结晶和减少了氧化应激;CG也增加了尿液,在小鼠中证实有效性.
结论:
- 开发了一种有效的策略,将果模型与化学隔离相结合,用于TCM结石成分发现.
- 确定了三种新的潜在化合物 (HYA,SAA,CG) 用于结石管理.
- 验证了果模型在发现生物活性TCM物质方面的实用性,为新疗法铺平了道路.
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