目的 研究人参Panax ginseng内生真菌强壮土赤壳菌Ilyonectria robusta RSA2004次生代谢产物的化学成分，以期发现具有抗乳腺癌活性的化合物。方法 该菌大米固体发酵的95%乙醇水提取物经硅胶、Sephadex LH-20凝胶及HPLC等多种柱色谱技术进行分离纯化，并根据核磁共振、质谱、圆二色谱（electronic circular dichroism，ECD）、计算ECD等手段鉴定化合物的结构，采用MTT法评价化合物对乳腺癌细胞MDA-MB-231的细胞毒性。结果 从人参内生真菌强壮土赤壳菌RSA2004发酵产物中分离得到4个化合物，分别鉴定为强壮土赤壳菌内酰胺A（1）、根赤壳菌素（2）、单青霉素I（3）和单青霉素IV（4）。活性测试结果表明化合物1和3对乳腺癌细胞MDA-MB-231的增殖有显著的抑制活性，半数抑制浓度为（9.37±3.1）、（5.13±2.5）μmol/L。结论 化合物1为新的生物碱类化合物，命名为强壮土赤壳菌内酰胺A；化合物1和3对MDA-MB-231细胞增殖有较强的细胞毒性。

Objective To study the secondary metabolites of the endophytic fungus Ilyonectria robusta RSA2004 from Panax ginseng in order to obtain compounds with anti-breast cancer activity. Methods The 95% ethanol extracts from the solid fermentation of rice were separated and purified by silica gel, Sephadex LH-20 gel and HPLC. The structures of the compounds were determined by NMR, mass spectrometry, circular dichroism, computational circular dichroism, etc. MTT experiment was used to evaluate the cytotoxicity of the compounds to breast cancer cell line MDA-MB-231.Results Four compounds were isolated and identified from the fermentation products of the endophytic fungus Ilyonia robusta RSA2004, which were identified as robusta A (1), radicicol (2), monocillin I (3), and monocillin IV (4). The activity test results showed that compounds 1 and 3 had significant inhibitory activity on breast cancer cell line MDA-MB-231 with the IC₅₀ values of (9.37±3.1) μmol/L and (5.13±2.5) μmol/L. Conclusion Compound 1 is a new alkaloid compound named robusta A. Compounds 1 and 3 have strong cytotoxicity on the proliferation of MDA-MB-231 cells.

R284.1

浙江省医药卫生科技计划项目（2023KY880）