来自Streptomyces flaveolus的未描述的ansatrienin类似物,包括两个N-乙半氨酸合物
Xiaofan Zhu1, Xiaomei Wu2, Hongji Li1
1School of Pharmacy, Naval Medical University, 325 Guohe Road, Shanghai, 200433, China.
Phytochemistry
|June 23, 2025
概括
在Streptomyces flaveolus中发现了五种新的ansatrienin类似物. 三胺素N显示出强烈的细胞毒性活性,而C-25氧化和N-乙半氨酸附着等修改降低了有效性.
科学领域:
- 自然产品化学 自然产品化学
- 微生物学 微生物学
- 药用化学 医学化学
背景情况:
- 安萨特里宁是强大的细胞毒性C17-合素安萨米辛.
- 斯特雷普托米切斯 (Streptomyces) 种类是生物活性天然产品的丰富来源.
研究的目的:
- 为了识别和表征来自Streptomyces flaveolus的新型ansatrienin类似物.
- 评估这些新化合物的抗增殖活性.
主要方法:
- 使用HR-ESI-MS和NMR光谱学进行隔离和结构阐明.
- 通过生物合成分析和TD-DFT/ECD计算来确定绝对配置.
- 针对癌细胞系的抗增殖试验 (HeLa,HuCCT1,PANC-1).
主要成果:
- 确定了五种未经描述的安沙特里宁类型:三诺米辛M-O (1-3),N-AcCys-ansatrienin 3a (4) 和N-AcCys-ansatrienin B (5).
- 三胺氨酸M (3) 是第一个具有C-25基组的三胺氨酸.
- 针对测试的细胞系,诺米辛N (2) 显示出显著的细胞毒性 (IC50:0.81-1.84μM).
- 化合物1,4和5是不活跃的,这表明C-25氧化和N-乙半氨酸修饰对细胞毒性的负面影响.
结论:
- 发现了具有多种结构特征的新型安萨特里宁.
- 结构-活性关系的洞察表明,特定的修改可以减少细胞毒性潜力.
- 这项研究强调了Streptomyces flaveolus在生产复杂天然产品方面的生物合成能力.
关键词:
安萨米辛是一种安萨米辛.一个三角形在内.细胞毒性 细胞毒性N-乙半氨酸的结合物这种植物是Streptomyces flaveolus.链杆菌植物家族 (Streptomycetaceae) 的一个家族.更多相关视频
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