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目的阐明无活性真菌野生株产紫青霉G59的超声诱变活性突变株N3001d1-1新产抗肿瘤活性产物。方法采用活性跟踪与高效硅胶薄层检测分析相结合的实验方法,组合利用各种色谱技术,通过将突变株样品与原始菌直接比对分离纯化突变株新产活性产物。根据理化性质和波谱数据鉴定化合物结构。用MTT法测试抗肿瘤活性。结果从突变株N3001d1-1发酵物中分离鉴定了2个突变株新产抗肿瘤活性产物,即橘霉素(citrinin)(1)和fructigenine A(2)。化合物1和2对K562细胞均呈抗肿瘤活性,抑制K562细胞的IC50分别为50.6μg/ml和69.1μg/ml。结论化合物1和2均为原始真菌产紫青霉G59所不生产的突变株N3001d1-1新产抗肿瘤活性次级代谢产物。研究结果表明,超声诱变技术可用于改造真菌无活性野生株的次级代谢功能并从中筛选获取活性突变株,从而拓展真菌药源活性新菌株资源。
Objective To elucidate the antitumor activity of N3001d1-1, an ultrasonic mutagenized mutant of Penicillium sp. G59 against wild-type fungus. Methods The active tracing method combined with high performance silica gel thin layer detection and analysis was used in combination with various chromatographic techniques to directly isolate and purify the new active product of the mutants by comparing the samples of the mutants directly with the original bacteria. Compound structure was identified based on physico-chemical properties and spectral data. Antitumor activity was tested by MTT assay. Results Two new mutants were identified as citrinin (1) and fructigenine A (2) from the mutant N3001d1-1. Compounds 1 and 2 showed antitumor activity against K562 cells, with IC50 of 50.6μg / ml and 69.1μg / ml, respectively. Conclusion Both compounds 1 and 2 are secondary metabolites of the new antitumor activity of mutant N3001d1-1 which is not produced by the original fungus Penicillium sp. G59. The results showed that the ultrasonic mutagenesis can be used to transform the secondary metabolites of inactive wild strains of fungi and obtain the active mutant strains from them, so as to expand the resources of new fungal active strains.