生物生产的epicoccamide-aglycone及其细胞毒性
Hyung-Jin Kwon1, Eun Ha Choi1, Umji Choi1
1Department of Biological Sciences and Bioinformatics, Myongji University, Yongin-si, Gyeonggi-do 17058, Republic of Korea.
Bioorganic & medicinal chemistry letters
|October 15, 2023
概括
这项研究分离了一种新型的真菌化合物,Epicoccamide-aglycone,它显示出强大的抗菌活性对金黄色葡萄球菌和增强的抗癌性质相比其前身,Epicoccamide. 提取文化在发现这种强大的天然产品方面被证明是有效的.
科学领域:
- 微生物学 微生物学
- 自然产品化学 自然产品化学
- 菌类生物化学 菌类生物化学
背景情况:
- 埃皮科卡米德 (Epicoccamide,简称EPC) 是一种具有有限生物活性的真菌多基基胺.
- 确定了EPC生物合成基因集群,但在淘汰突变者中没有发现EPC-aglycone.
- 糖化在EPC生物活性中的作用尚不清楚.
研究的目的:
- 从Epicoccum nigrum中分离和鉴定EPC-aglycone的特征.
- 评估EPC-aglycone的生物活性,并将其与EPC进行比较.
- 调查EPC生物合成的最后步骤和糖化酶的影响.
主要方法:
- 使用疏水性树脂Diaion HP-20的提取培养.
- 染色分离和化学分析用于结构阐明.
- 在体外测试以确定抗菌和细胞毒性活动.
主要成果:
- 成功隔离和结构识别了EPC-aglycone.
- 与EPC (64μg/mL) 相比,EPC-aglycone对金黄色葡萄球菌 (MIC 1μg/mL) 的抗菌活性显著更强.
- 与EPC相比,EPC-aglycone显示出对HeLa和WI-38细胞系的增长抑制,具有明显的剂量反应曲线.
结论:
- 附加d-曼诺斯是EPC生物合成的最后一步,调节生物活性.
- 糖基化显著影响了乙烯基四胺酸的抗菌和细胞毒性.
- 提取性培养对于发现具有增强生物活性的神秘微生物天然产品非常有价值.
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