摘要
目的:研究筛选枳椇子Hovenia acerba Lindl.乙酸乙酯部位中具有抗肿瘤活性的化合物。方法:利用乙酸乙酯萃取枳椇子60%乙醇水提取物,并采用300~400目硅胶与制备级HPLC对其萃取物进行分离纯化,最终得到4个化合物,通过MTT法筛选发现其中ZJZ-Z2具有最优的活性,通过ESI-MS、~1H-NMR和~(13)C-NMR检测,并通过与相关文献对比,初步推测该化合物为二氢杨梅素(dihydromyricelin),体内实验证明ZJZ-Z2具有体内抗肿瘤活性。结果:通过MTT法分别对枳椇子乙酸乙酯部位硅胶分离得到的12个组分进行测定,发现其中第4组分对肿瘤细胞Huh-7、OS-RC-2的半数抑制率(IC_(50))分别为70.4、69.8μg·mL~(-1);进一步分离纯化得到的ZJZ-Z2对肿瘤细胞OS-RC-2、Huh-7、HCT-116、CFPAC-1的IC_(50)分别为33.8、63.9、46.8、55.1μg·mL~(-1),且对H22荷瘤小鼠模型表现出一定的抑瘤作用。结论:枳椇子乙酸乙酯部位具有抗肿瘤活性,其主要的抗肿瘤活性成分为二氢杨梅素。
Objective:To study the anti-tumor activity constituents in the ethyl acetate extract of Hovenia acerba.Methods:60% ethanol aqueous extract of H.acerba was extracted with ethyl acetate and purified with 300-400 mesh silica gel and preparative grade HPLC.The chemical structures of the isolated compounds were determined by ESI-MS,~1H-NMR and ~(13)C-NMR.Results:Twelve components were isolated from the ethyl acetate fraction of H.acerba.Four compounds were obtained and found that ZJZ-Z2 had the best activity.The compounds were dihydromyricelin.The in vivo experiments showed that ZJZ-Z2 had antitumor activity.By MTT method,IC_(50) of the fourth component to Huh-7 and OS-RC-2 was 70.4 μg·mL~(-1) and 69.8 μg·mL~(-1) Further separation and purification to obtain ZJZ-Z2,which half-inhibition rate(IC_(50))to tumor cells OS-RC-2,Huh-7,HCT-116,CFPAC-1 was 33.8 μg·mL~(-1),63.9 μg·mL~(-1),46.8 μg·mL~(-1),55.1 μg·mL~(-1),and it is found that they had a certain anti-tumor effect to H22 tumor-bearing model mice.Conclusion:The ethyl acetate fraction of H.acerba has antitumor activity,and the main active ingredient is dihydromyricetin.
引文
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