目的比较人工虫草菌HK-1与天然虫草提取物抗肿瘤活性及主要化学成分。方法人工虫草菌HK-1与天然虫草分别用石油醚、醋酸乙酯、乙醇和水提取。用MTT法测定各提取物对小鼠黑色素瘤细胞B16、人肝癌细胞HepG2、人乳腺癌细胞MCF-7和类前骨髓白血病细胞HL-60的细胞毒作用。对活性提取物进一步用动物模型检测其体内抗肿瘤作用。高效液相色谱法测定提取物中的化学成分。结果对于小鼠黑色素瘤细胞B16,所有虫草菌HK-1提取物的细胞毒作用均比天然虫草提取物的作用强,其中以醋酸乙酯提取物的细胞毒作用最强。虫草菌HK-1醋酸乙酯提取物对4种肿瘤细胞的细胞毒作用均比天然虫草醋酸乙酯提取物的作用强;体内实验也表明虫草菌HK-1醋酸乙酯提取物可以抑制肿瘤的生长。对提取物化学成分的分析表明麦角甾醇和腺苷可能是虫草菌HK-1中具有抗肿瘤活性的成分。结论人工虫草菌HK-1比天然虫草具有更强的抗肿瘤活性,是有开发潜力的抗肿瘤候选药物。

Objective To compare the antitumor effects and chemical components of the extracts in cultivated Cordyceps sinensis (Cs) fungus HK-1 and natural Cs. Methods The cultivated Cs fungus HK-1 and natural Cs were extracted with petroleum ether (PE), ethyl acetate (EtOAc), ethanol (EtOH), and water. The cytotoxicity of all the extracts was observed with MTT assay on breast cancer cell line MCF-7, mouse melanoma cell line B16, human premyelocytic leukemia cell line HL-60, and human hepatocellular carcinoma cell line Hep G2. The antitumor activity in vivo of the extract was further studied with animal model. The chemical constituents in the extracts were analyzed by HPLC. Results All of the extracts from the cultivated Cs fungus HK-1 had much stronger cytotoxicity on B16 than those from natural Cs, and the EtOAc extract had the most potent activity. The activity of EtOAc extract from the cultivated Cs fungus HK-1 was more potent than that from natural Cs on all the four cancer cell lines. EtOAc extract from the cultivated Cs fungus HK-1 also can inhibit the growth of tumor in vivo. Chemical components of all extracts were analyzed and ergosterol and adenosine were found to be potential compounds. Conclusion The cultivated Cs fungus HK-1 has stronger antitumor activity than natural Cs and is a potential source of antitumor compounds.

香港理工大学资助项目(G-YD28andASDfund)