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目的对1株分离自广西红树林植物黄槿(Hibiscus tiliaceus)的内生真菌Penicilliumsp·LD-68的抗肿瘤活性成分进行研究。方法采用溶剂萃取、柱色谱层析及制备HPLC等方法对菌株发酵产物进行活性追踪分离,通过理化性质及波谱学手段进行化学结构鉴定,以SRB和MTT法评价化合物的抗肿瘤活性。结果从中分离得到5个弯孢霉菌素类化合物,其结构分别鉴定为curvularin(1)、dehydrocurvularin(2)、11-β-Hy-droxy-12-Oxocurvularin(3)、11-β-Hydroxycurvularin(4)、11-α-Hydroxycurvularin(5)。化合物1～5对A549、hela、BEL-7402、K562 4种人肿瘤细胞株具有不同程度的抑制作用,其中化合物2、3、4、5对hela细胞具有较好的抗肿瘤细胞活性,IC50分别为3.99、7.75、10.00、5.10μmol·L-1。结论首次测定了化合物3～5对A549、hela、BEL-7402、K562 4种肿瘤细胞系的细胞毒活性,其中对hela细胞显示出较高的抑制率。
Objective To study the antitumor activity of an endophytic fungus Penicillium sp. LD-68 isolated from Guangxi mangrove plant Hibiscus tiliaceus. Methods The fermentation products of the strains were isolated by the methods of solvent extraction, column chromatography and preparative HPLC. The chemical structures were identified by physico-chemical properties and spectroscopic methods. The antitumor activity of the compounds was evaluated by SRB and MTT methods. Results Five curcuminoids were isolated and identified as curvularin (1), dehydrocurvularin (2), 11-β-Hy-droxy-12-Oxocurvularin (3) and 11-β-Hydroxycurvularin ), 11-α-Hydroxycurvularin (5). Compounds 1 to 5 inhibited A549, hela, BEL-7402 and K562 cells to varying degrees, and compounds 2,3,4,5 showed good anti-tumor activity against hela cells with IC50 3.99,7.75,10.00,5.10μmol·L-1. Conclusions The cytotoxic activity of compounds 3 ~ 5 against four tumor cell lines A549, hela, BEL-7402 and K562 was determined for the first time, and the hela cells showed higher inhibitory rates.