阿斯塔利德是来自海洋衍生物的衍生物
Mohamed S Elnaggar1,2, Ahmed M Elissawy1,3, Fadia S Youssef1
1Department of Pharmacognosy, Faculty of Pharmacy, Ain Shams University Abbassia 11566 Cairo Egypt aelissawy@pharma.asu.edu.eg dean@pharma.asu.edu.eg.
RSC advances
|June 5, 2023
概括
研究人员发现了来自Aspergillus真菌的新化合物,包括austalide Z,具有预防癌症的潜力. 这些天然产品在药物开发中显示出有前途的特性.
科学领域:
- 自然产品化学 自然产品化学
- 海洋生物技术 海洋生物技术
- 药理学 药理学是指药理学的学科.
背景情况:
- 软珊瑚是生物活性天然产品的丰富来源.
- 包括Aspergillus物种在内的真菌可以产生复杂的二次代谢产物.
- 来自海洋相关真菌的美罗特类和类对药物发现有兴趣.
研究的目的:
- 为了隔离和描述来自Aspergillus sp.的化学成分. 与软珊瑚Sinularia物种相关.
- 评估与Caco-2癌细胞系对抗分离化合物的细胞毒性活性.
- 为了评估化合物的药物相似性,使用in silico ADME/TOPKAT预测.
主要方法:
- 使用Aspergillus sp.的乙烯酸乙烯提取物进行化学研究.
- 通过1D和2DNMR,UV和ESI-MS阐明结构.
- 在体外细胞毒性测定 (MTT) 和在中ADME/TOPKAT分析.
主要成果:
- 隔离了一种新的美洛特化物,austalide Z (1) 和十种已知的化合物.
- 奥斯塔利德Z (1) 对Caco-2细胞表现出较弱至中度的细胞毒性 (IC50 = 51.6μg mL-1).
- 在 silico 分析表明大多数化合物具有有利的药理动力学,药理动力学和毒性概况.
结论:
- 亚斯伯菌 sp. 的情况. 与软珊瑚相关的可以产生新的生物活性化合物.
- 奥斯塔利德Z和其他分离化合物代表了预防癌症的潜在药物.
- 这些已识别的化合物对药物应用具有有前途的特性.
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