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设计,合成和14-aryloxy/amide替代的andrographolide衍生物的抗真菌活性

Zhuyun Liu¹, Shanshan Yang², Jierui Ma²

¹School of Intelligent Pharmaceutical Manufacturing & New Chemical Engineering Materials, Taizhou Polytechnic College, Taizhou, 225300, Jiangsu, PR China. llzzyy23@163.com.

Scientific reports

|November 25, 2025

概括

研究人员合成了来自andrographolide的新型抗真菌化合物. 化合物4d对六种真菌菌株和受损的P. piricola mycelia表现出显著的抗真菌活性,对牛豆种子具有高安全性.

科学领域:

自然产品化学自然产品化学
药用化学医学化学
菌类学菌类学是指菌类学.

背景情况:

迪特尔类乳,如安德罗格拉福利德,是具有潜在生物活性的天然产品.
探索天然产品的衍生品是发现新治疗剂的关键策略.
抗真菌耐药性需要开发具有强效活性的新型化合物.

研究的目的:

在andrographolide支架的基础上设计和合成新的化学实体.
评估这些新型化合物对各种真菌菌株的抗真菌潜力.
研究最有前途的化合物的作用机制和安全概况.

主要方法:

新型双酸乳衍生物的合成.
使用核磁共振 (H NMR,C NMR) 和高分辨率质谱 (HR-MS) 的结构阐明.
抗真菌生物测试以确定抑制率和EC₅₀值.
扫描电子显微镜 (SEM) 用于可视化对真菌骨髓的影响.
种子发芽试验,以评估化合物的安全性.

主要成果:

一系列新的化合物被成功合成和表征.
化合物4d表现出显著的抗真菌活性,抑制率超过60%对六种真菌菌株在100微克/毫升.
化合物4d的EC₅₀值较低,为9.09微克/毫升,对*P. piricola*.进行抗击.
SEM分析显示,4d化合物明显损害了P. piricola*的髓.
化合物4d对牛种子发芽没有任何不良影响,这表明它具有良好的安全性.

结论:

新型andrographolide衍生物具有有前途的抗真菌特性.
化合物4d是一种强大的抗真菌剂,其潜在机制涉及细胞损伤.
化合物4d的高安全性表明它有可能在农业或医药应用中进一步发展.

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