来自Aspergillus terreus的各种生物活性二次代谢物:抗菌,抗癌和抗SARS-CoV-2活性研究
Abdelaaty Hamed1, Ahmed S Abdel-Razek2,3, Ahmed B Abdelwahab4
1Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City-Cairo 11884, Egypt.
概括
海洋Aspergillus terreus LGO13发酵产生了23种生物活性化合物. 富米特雷摩根C显示出对SARS-CoV-2有前途的抗病毒活性,向类似帕帕因的蛋白酶.
科学领域:
- 海洋微生物学 海洋微生物学
- 自然产品化学 自然产品化学
- 药理学 药理学是指药理学的学科.
背景情况:
- 海洋衍生真菌是各种生物活性化合物的丰富来源.
- 之前的研究已经确定了来自Aspergillus terreus LGO13.13的生物活性代谢物.
- 扩大发酵的规模允许分离较小/更有前途的二次代谢产物.
研究的目的:
- 从海洋Aspergillus terreus LGO13.13中分离和识别较小/更有前途的生物活性二次代谢物.
- 评估这些代谢物的抗菌性,细胞毒性和抗病毒性质.
- 用分子对接模拟来调查潜在的抗SARS-CoV-2候选药物.
主要方法:
- 大规模的液体培养发酵阿斯伯吉勒斯土壤LGO13.13.
- 使用HR-ESI-MS和1D/2DNMR光谱学进行结构阐明.
- 对微生物,癌细胞系 (KB-3-1,A549) 和SARS-CoV-2进行生物活动查.
- 分子对接模拟以识别潜在的病毒目标.
主要成果:
- 已知23种生物活性代谢物被分离出来,其中包括N-二三甲 (1).
- 柴托明因 (2) 被确定为SARS-CoV-2帕帕因类蛋白酶 (PLpro) 的潜在抑制剂.
- 富米特雷摩根C (6) 对SARS-CoV-2具有很高的选择性指数 (19.77),而沙托米宁 (2) 和阿扎斯皮洛A (9) 则具有中等的选择性.
结论:
- 富米特雷摩根C显示出作为抗SARS-CoV-2的抗病毒剂的显著潜力.
- 这项研究强调了海洋衍生真菌在发现新型治疗化合物的价值.
- 针对像PLpro这样的病毒蛋白酶是开发新抗病毒药物的有希望的策略.
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