目的:分离鉴定戴氏虫草发酵菌粉的抗肿瘤化学成分。方法:采用液体深层发酵制备戴氏虫草菌体,进而应用硅胶、Sephadex LH-20柱、MCI等分离纯化方法,经反复柱层析、高效液相色谱正反相系统等对戴氏虫草菌抗肿瘤的有效部位氯仿萃取部位进行分离,利用EI、ESI及1D/2D-NMR等技术对获得的化合物进行结构鉴定,并采用SRB法测定体外抗肿瘤细胞毒性。结果:从戴氏虫草发酵菌粉中分离并鉴定出6个化合物,分别为:5α,8α-麦角甾-6,22-二烯-3β-醇(1)、麦角甾醇(2)、腺嘌呤核苷(3)、烟曲霉酸(4)、脱乙酰细胞松弛素C(5)和接柄胞素D(6)。化合物2对人胃腺癌细胞SGC-7901的IC_50为5.99μmol/L,不到临床一线药物顺铂IC50值的50%,且对正常细胞的毒性小。结论:从戴氏虫草发酵菌粉的抗肿瘤有效部位中分离并鉴定得到6个化合物,其中,化合物1、5和6为首次从戴氏虫草中分离得到。化合物1、2和4具有抗肿瘤细胞毒活性,为该有效部位中的主要抗肿瘤有效成分。
Objective: To seperate and identify the chemicals from the antitumor fraction of Cordyceps taii mycelia powder.Methods: The mycelia of Cordyceps taii were prepared by the submerged fermentation technique.Chemical entities in the antitumor fraction of Cordyceps taii were isolated and purified by using different column chromatographies(silica gel,Sephadex LH-20 and MCI),and semi-preparative HPLC method.Theirs chemical structures were then identified by different spectrum techniques such as EI,ESI and 1D /2D-NMR,etc.The cytotoxic activity was investigated by the Sulforhodamine B( SRB) assay.Results: Six compounds,such as 5α,8α-epidioxyergosta-6,22-dien-3β-ol(1),ergosterol(2),adenine nucleoside(3),helvolic acid(4),deacetylcytochalasin C(5) and zygosporin D(6),were identified.The IC_50 value of compound 2 against human gastric cancer cell line SGC-7901 was 5.99 μmol / L,which was less than the half value of cisplatin,and had lower cytotoxicity to normal cells in comparison with cisplatin.Conclusion: Six compounds have been isolated from the antitumor fraction of Cordyceps taii mycelia powder,of which compounds 1,5 and 6 are isolated from Cordyceps taii for the first time.Compounds 1,2 and 4 have cytotoxic activities against cancer cells,and should be the main antitumor compounds of Cordyceps taii.