目的 研究大头兔儿风Ainsliaea macrocephala内生真菌温特曲霉Aspergillus wentti Y1次生代谢产物的化学结构及其生物活性。方法 运用硅胶、Sephadex LH-20凝胶、薄层色谱（TLC）和半制备高效液相色谱等方法对菌株发酵液的醋酸乙酯萃取物及菌丝甲醇提取物进行分离纯化，根据理化性质和波谱数据分析鉴定化学结构；采用CCK-8法测定化合物的细胞毒活性。结果 从发酵液的醋酸乙酯萃取物及菌丝甲醇提取物中分离到10个化合物，分别鉴定为2-羟基异硫赭曲菌素脱水合物（1）、yicathin A（2）、isosulochrin dehydrate（3）、1，6-二羟基-3-甲基-8-甲氧羰基呫吨酮（4）、yicathin C（5）、wentiquinone B（6）、大黄素甲醚（7）、曲霉内酯B（8）、8-羟基-1，3-二甲氧基-6-甲基蒽醌（9）、藤黄绿脓菌素（10）。化合物10对人食管癌细胞株OE19的增殖显示出较强的抑制作用，其半数抑制浓度（IC₅₀）值为5.8 μmol/L。结论 化合物1为新的呫吨酮类化合物，命名为2-羟基异硫赭曲菌素脱水合物；化合物10为首次从曲霉属真菌中分离得到。化合物10对人食管癌细胞株OE19具有明显的细胞毒性。

Objective To study the secondary metabolites of the endophytic fungus Aspergillus wentti Y1 isolated from Ainsliaea macrocephala. Methods The compounds were isolated and purified from the ethyl acetate extract of the fungal fermentation broth and the methanol extract of the mycelial by silica gel, reverse phase silica gel ODS, Sephadex-LH20 column chromatography, TLC, HPLC, and so on. Their structures were identified by extensive spectroscopic analysis. The compounds were evaluated for cytotoxic activity against human esophagus cancer cell lines OE19 and SK-GT-4 by CCK8 assay. Results Ten compounds were isolated from the fermentation broth and mycelial extracts of the strain Aspergillus wentti Y1, and identified as 2-hydroxyisosulochrin dehydrate (1), yicathin A (2), isosulochrin dehydrate (3), 1,6-dihydroxy- 3-methyl-8-carbomethoxyxanthone (4), yicathin C (5), wentiquinone B (6), physcion (7), aspergillactone B (8), 8-hydroxy-1,3-dimethoxy-6-methylanthraquinone (9) and pyoluteorin (10), respectively. Compound 10 exhibited potent cytotoxicity against human esophagus cancer cell lines OE19 with the IC₅₀ value of 5.8 μmol/L. Conclusion Compound 1 was identified as new compound, and named 2-hydroxyisosulochrin dehydrate. Compound 10 is isolated from Aspergillus species for the first time. Compound 10 exhibited potent cytotoxicity against human esophagus cancer cell lines OE19.

R284.1

国家自然科学基金资助项目（31870327）；国家自然科学基金资助项目（81520108030）；国家自然科学基金资助项目（81573318）