展开蛋白质反应的克桑抑制剂 从Calophyllum caledonicum中分离出来
Marine Chambaud1, Anne-Marie Le Ray1, Racha Hamzi1
1SONAS | Substances d'Origine Naturelle et Analogues Structuraux Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France.
Journal of natural products
|June 13, 2024
概括
来自Calophyllum caledonicum的新桑衍生物抑制了真菌未折叠蛋白质反应 (UPR),这是一个关键的毒性因素. 化合物3和8显示强烈的抗UPR活性,为新的抗真菌策略提供了潜力.
科学领域:
- 自然产品 化学 化学
- 菌类学 菌类学是指菌类学.
- 生物化学 生物化学
背景情况:
- 展开的蛋白质反应 (UPR) 对真菌毒性至关重要.
- 预化桑,如来自Garcinia mangostana的γ-mangostin,可以抑制UPR.
- 卡洛菲勒 (Calophyllum caledonicum) 是一种富含前化桑的丰富来源.
研究的目的:
- 从 Calophyllum caledonicum 干皮中分离和鉴定了先化桑的特征.
- 为了评估这些孤立化合物的抗UPR活性.
主要方法:
- 在生物试验指导下分化 Calophyllum caledonicum 茎树皮提取物.
- 基于细胞的抗UPR试验用于活动查.
- 分离化合物的化学结构阐明.
主要成果:
- 分离了四种新的桑衍生物,卡莱多尼桑N-Q (化合物3,4,8,12).
- 化合物3和8显示出显著的抗UPR活性.
- 化合物3和8的IC50值分别为11.7 ± 0.9 μM和7.9 ± 0.3 μM.
结论:
- 卡洛菲勒 (Calophyllum caledonicum) 是一种具有抗UPR活性的新型前化桑的来源.
- 卡莱多尼克桑3和8是开发针对UPR途径的新抗真菌剂的有希望的线索.
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