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A Lipoaminopeptaibol Secreted by Alkalophilic Fungus Emericellopsis alkalina Demonstrates a Strong Cytotoxic Effect against Tumor Cell Lines

机译:由碱性真菌emericellopsis碱性碱分泌的脂肪氨酸氨基酚显示出对肿瘤细胞系的强烈细胞毒性作用

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Soil fungi are known to produce and secrete antibiotics with a strong antimicrobial effect towards eukaryotic organisms. In many occasions, these compounds belong to peptides that are products of non-ribosomal biosynthesis and are called peptaibols. Many peptaibols are cytotoxic and some of them suppress tumor cell lines much better than normal cells by inducing calcium-mediated apoptosis. The main antimicrobial lipoaminopeptaibol—emericellipsin A—isolated from the fungus Emericellopsis alkalina strain VKPM F-1428, which demonstrates promising antifungal activity against different fungal taxons,has been found to exhibit selective cytotoxic activity against HepG2 and Hela cell lines (EC50 2.8 and 0.5 μM, respectively) in MTT assays in vitro. This result corresponds to the standard antitumor antibiotic doxorubicin, which has an EC50 value of 440 nM. In a fibroblast toxicity test, emericellipsin A exhibited less cytotoxic activity than doxorubicin (EC50 14 and 0.34 μM, respectively). Therefore, it is less toxic to normal cells than doxirubicin (~40 times), but it yields a more potent cytotoxic effect on tumor cell lines. That is why emericellipsin A can be considered for future more detailed investigations to be an effective antitumor substance.
机译:已知土壤真菌产生和分泌抗生素,对真核生物有了强烈的抗菌效果。在许多情况下,这些化合物属于肽,其是非核糖体生物合成的产品,并且称为肽。许多肽是细胞毒性,其中一些通过诱导钙介导的细胞凋亡抑制肿瘤细胞系比正常细胞要好得多。来自真菌emericellopsis碱菌株VKPM F-1428的主要抗微生物脂素碱磷酸纤维素蛋白酶菌株VKPM F-1428,其证明了对不同真菌株的抗真菌活性有前途的抗真菌活性,其针对HepG2和HeLa细胞系(EC50 2.8和0.5μm)表现出选择性细胞毒性活性分别在体外MTT测定中。该结果对应于标准抗肿瘤抗生素多柔比星,其EC50值为440nm。在成纤维细胞毒性测试中,emeterlipsina分别表现出比多柔比星(EC 50 14和0.34μm)的细胞毒性活性较少。因此,对正常细胞的毒性较小,而不是多发性细胞(〜40次),但它对肿瘤细胞系产生更有效的细胞毒性作用。这就是为什么可以考虑未来更详细的研究成为有效抗肿瘤物质的原因。

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