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Structure and total synthesis of aspernigerin: A novel cytotoxic endophyte metabolite

机译:曲霉菌素的结构和全合成:一种新型的细胞毒性内生代谢物

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摘要

Aspernigerin (1), a novel cytotoxic alkaloid consisting of an unprecedented structural framework has been isolated from the extract of a culture of Aspergillus niger IFB-E003, an endophyte in Cyndon dactylon. Its structure was elucidated on the basis of comprehensive NMR spectral analysis and confirmed by single-crystal X-ray analysis. Aspernigerin (1) has been shown to be cytotoxic to the tumor cell lines nasopharynyeal epidermoid KB, cervical carcinoma Hela, and colorectal carcinoma SW1116 with corresponding IC50 values of 22, 46, and 35 mu m, respectively. A feasible total synthetic route for aspernigerin (1) has been established for further pharmacological research.
机译:从黑曲霉IFD-E003的培养物提取物中分离出了曲霉菌素(1),它是一种由前所未见的结构框架组成的新型细胞毒性生物碱。在全面的NMR光谱分析的基础上阐明了其结构,并通过单晶X射线分析对其进行了确认。已显示曲霉菌素(1)对鼻咽上皮表皮样KB,宫颈癌Hela和结直肠癌SW1116等肿瘤细胞系具有细胞毒性,其IC50值分别为22、46和35μm。已经建立了可行的曲霉菌素(1)的总合成途径,以用于进一步的药理研究。

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