来自日本虫的异乙烯糖精和它们的细胞毒性活动
Yimeng Wang1, Zhibin Wang1, Yanping Sun1
1Key Laboratory of Basic and Application Research of Beiyao, Ministry of Education, Heilongjiang University of Chinese Medicine, Harbin 150040, China.
Molecules (Basel, Switzerland)
|July 13, 2024
概括
来自Atractylodes japonica的异乙烯糖精子对结肠和肺癌细胞具有适度的抗癌活性. 分子对接表明与FGFR3和BRAF的潜在相互作用,为开发新的植物衍生抗癌药物提供了基础.
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.
- 分子生物学分子生物学
背景情况:
- 癌症仍然是全球主要的健康挑战.
- 植物衍生化合物,包括异黄糖,是抗癌药物的重要来源.
- 异二烯糖的抗癌机制尚未得到充分理解.
研究的目的:
- 为了隔离和识别来自Atractylodes japonica根的异乙烯糖精.
- 评估这些化合物对人类结肠癌 (HCT-116) 和肺腺癌 (A549) 细胞的细胞毒性作用.
- 通过使用计算方法,研究潜在的分子机制,这些机制是它们抗癌活性的基础.
主要方法:
- 隔离了12个异乙烯糖精子成分 (5个新,7个已知) 来自Atractylodes japonica.
- 使用1D/2D-NMR光谱和HR-ESI-MS进行结构阐明.
- 通过CCK8测定进行细胞毒性评估;用于机制探索的分子对接和动力学模拟.
主要成果:
- 化合物2,4和6显示对HCT-116细胞的中度抑制 (IC50值7.49-13.49μM).
- 化合物1和6对A549细胞表现出中度抑制 (IC50值7.10-8.36μM).
- 分子对接表明FGFR3和BRAF具有强烈的结合亲和力,其中化合物2显示FGFR3的最低能量 (-10.63 kcal/mol).
结论:
- 来自Atractylodes japonica的isovaleryl糖精对人类结肠和肺癌细胞系具有中度的细胞毒性作用.
- 计算分析表明FGFR3和BRAF是潜在的分子标.
- 这项研究为开发基于异乙烯糖精子的新型抗癌疗法提供了基础.
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