赤芝中脂溶性化合物的体外抗肿瘤活性

Liposoluble Compounds Isolated from Ganoderma lucidum and Their Cytotoxic Activity against Tumor Cells in vitro

从赤芝中分离获得3个化合物:灵芝萜烯酮醇(Ⅰ)、麦角甾-7,22-二烯-3β-醇(Ⅱ)、过氧化麦角甾醇(Ⅲ)。化疗药物顺氯氨铂(DDP)作为阳性对照,用MTT(microculture tetrazolium)法和形态学方法评定了它们对人肝癌细胞株BEL-7402、人胃癌细胞株MGC-803的增殖抑制作用。Ⅰ、Ⅱ、Ⅲ、DDP对BEL-7402的半数抑制浓度IC50值分别为:20.15、5.05、24.35、7.67μmol/L;对MGC-803的IC50值分别为:6.32、10.09、9.88、3.52μmol/L。Ⅰ和Ⅱ分别与DDP以质量比1∶1混合处理BEL-7402细胞有正协同作用,效果明显优于单独使用DDP。化合物Ⅰ、Ⅱ、Ⅲ对HMEC人微血管内皮细胞的毒性很小,质量浓度6.25 mg/L的Ⅰ甚至能促其增殖,增长率为0.93%,Ⅱ、Ⅲ的抑制率仅为21.14%和2.86%。Ⅰ、Ⅱ、Ⅲ是极具潜力的抗肿瘤药物。

Three compounds from Ganoderma lucidum were obtained and identified as ganodermenonol （ Ⅰ ）, （ 22E, 24R ） -ergosta-7,22-dien-3β-ol （ Ⅱ ） and ergosterol peroxide （ Ⅲ ）. MTT （ microcuhure tetrazolium） assay and morphological method were used to evaluate the inhibitive effect of compounds on the proliferation of human hepatocarcinoma cell line BEL - 7402 and human gastric cancer cell line MGC- 803, in contrast to the positive control of cis-diaminedichloroplatinum （DDP）. The IC50 values of Ⅰ , Ⅱ, Ⅲ and DDP towards BEL -7402 cell were 20. 15,5.05,24.35 and 7.67 μmol/L respectively, and those towards MGC -803 cell were 6.32, 10. 09, 9. 88 and 3.52 μmol/L respectively. When combined with DDP, Ⅰ and Ⅱ have synergistic interaction against BEL- 7402 cells. On the other hand, they have but very low toxicity impact on HMEC, no matter used alone or combined with DDP. Compound Ⅰ even increased the proliferation of HMEC cells by 0. 93% at 6.25 mg/L. The inhibitive ratios of Ⅱ and Ⅲ toward HMEC cells were only 21.14 % and 2. 86 %.