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Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
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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

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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.

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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.