合成一个循环octapeptide,Cyclopurpuracin,并评估其抗菌活性
Rani Maharani1,2,3, Hasna Noer Agus Yayat1, Ace Tatang Hidayat1,2,3
1Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Padjadjaran, Jatinangor 45363, West Java, Indonesia.
Molecules (Basel, Switzerland)
|June 28, 2023
概括
来自Annona purpurea的环环,Cyclopurpuracin,通过结合固体和溶液相方法成功合成. 合成的环紫色素没有显示任何符合混合物和微弱的抗菌活性.
科学领域:
- 自然产品化学 自然产品化学
- 合成有机化学 合成有机化学
- 药用化学 医学化学
背景情况:
- 环保素是一种从Annona purpurea种子中分离出来的环保.
- 以前试图循环连接线性环保素的尝试存在问题,反向版本产生了混合的适配物.
研究的目的:
- 报告使用固体和溶液阶段合成方法的结合,成功合成了环保素.
- 为了描述合成的环紫色素,并评估其抗菌活性.
主要方法:
- 制备两个线性前体:线性前体A和线性前体B.
- 使用PyBOP/NaCl方法循环生成前体.
- 使用HR-ToF-MS,1H-NMR和13C-NMR进行合成产品的表征.
主要成果:
- 顺利合成环保普拉,A和B前体的总产量分别为3.2%和3.6%.
- 合成环素表现出与天然产品相似的NMR配置文件,并且缺乏符合性混合物.
- 抗微生物评估显示,抗黄金菌,大肠杆菌和白菌的活性较弱 (MIC = 1000μg/mL).
结论:
- 这项研究成功地确定了循环紫色素的合成途径.
- 合成的环保素在形状上是均的,与之前合成的反向模拟不同.
- 环保普拉具有较弱的抗微生物特性,反向模拟物显示出稍微更好的疗效.
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