枳椇子乙酸乙酯部位抗肿瘤活性成分筛选  

Screening of Antitumor Active Ingredients in Ethyl Acetate of Hovenia acerba

作　　者：张奇 刘英[1,2] 胡海峰 吴春珍[1,2] 姜锦锦 李彻[1,2] ZHANG Qi;LIU Ying;HU Hai-feng;WU Chun-zhen;JIANG Jin-jin;LI Che(Shanghai Institute of Pharmaceutical Industry,Shanghai 200040,China;Sinopharm Health Industry Institute Co.,Ltd.,Shanghai 201203,China)

机构地区：[1]上海医药工业研究院,上海200040 [2]国药集团健康产业研究院有限公司,上海201203

出　　处：《中国现代中药》2019年第6期782-785,共4页Modern Chinese Medicine

基　　金：国家中医药管理局中医药行业专项(201507004)

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13C-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(IC50)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IC50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, 1 H-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.

关 键 词：枳椇子 乙酸乙酯部位 抗肿瘤活性 二氢杨梅素 

分 类 号：R285.5[医药卫生—中药学] R284.1[医药卫生—中医学]