南酸枣的芳香族化合物及其体外抗肿瘤活性  

Aromatic chemical constituents of Choerospondias axillaries and their in vitro antitumor activity

作　　者：李长伟[1] 崔承彬[1] 蔡兵[2] 韩冰[2] 窦德强[3] 陈英杰[3] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850 [2]天津生物医药研究所,天津300384 [3]沈阳药科大学中药学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2005年第3期138-141,147,共5页Chinese Journal of Medicinal Chemistry

基　　金：国家重点基础研究发展规划项目(G1998051113);国家杰出青年科学基金项目(39825126);国家教育部长江学者奖励计划项目

摘　　要：目的阐明南酸枣的抗肿瘤活性成分。方法通过活性跟踪分离确定活性组分,利用各种色谱技术分离活性组分中的化学成分。根据理化性质和光谱数据鉴定结构,利用SRB法和流式细胞术评价单体化合物的抗肿瘤活性。结果从南酸枣树皮中分离鉴定了5个化合物,分别为乔松素(1)、柚皮素(2)、白杨素(3)、邻苯二甲酸二丁酯(4)和反式阿魏酸十四酯(5)。SRB法测试结果:化合物1～5在10μmol·L-1浓度下对HCT15细胞增殖的抑制率分别为21.5%(1)、37.3%(2)、33.1%(3)、20.1%(4)和17.0%(5),而在相同浓度下对HeLa细胞的抑制率分别为30.0%(1)、22.1%(2)、22.4%(3)、30.4%(4)和26.4%(5)。流式细胞术测试结果:化合物1和2对tsFT210细胞有较弱的G2M期抑制作用,化合物4在高浓度时表现坏死性细胞毒活性,而在低浓度时则具有G0G1期抑制活性。结论化合物1和3～5为首次从该属植物中分得,化合物1～5系首次报道的该植物中具有抗癌活性的5个成分。Aim To explore the antitumor constituents of Choerospondias axillaries Burtt.et Hill.Methods The separation procedure was guided by flow cytometric bioassay using tsFT210 cells to obtain antitumor active fractions.Various column chromatography and preparative TLC were used to obtain pure compounds from the active fractions.Structures of the compounds obtained were investigated by modern spectroscopic methods.Flow cytometry and SRB method were employed to evaluate antitumor activity of the compounds.Results Compounds 1～5 were isolated from the barks of Choerospondias axillaries and they were identified as pinocembrin(1),naringenin(2),chrysin(3),dibutyl phthalate(4)and tetradecyl E-ferulate(5)respectively. In SRB assay,1～5 at 10 μmol·L -1 inhibited the proliferation of human cancer HCT-15 and HeLa cells with the inhibition rates of 21.5%(1),37.3%(2),33.1%(3),20.1%(4)and 17.0%(5)for HCT-15 and 30.0%(1),22.1%(2),22.4%(3),30.4%(4)and 26.4%(5)for HeLa cells,respectively.Their IC_ 50 values were 83 μmol·L -1(1),76 μmol·L -1(2)and more than 100 μmol·L -1(3～5)on HCT-15,and 84 μmol·L -1(1)and more than 100 μmol·L -1(2～5)on HeLa cells,respectively.Flow cytometric analysis indicated that 1 and 2 slightly inhibited the cell cycle of tsFT210 cells at the G_2/M phase at higher concentration while 4 showed strong cytotoxicity at higher concentration but at lower concentration inhibited the cell cycle at the G_0/G_1 phase.Conclusion Compounds 1 and 3～5 are isolated from Choerospondias axilla-ries for the first time,and compounds 1～5 are the first report as the antitumor constituents of Choerospondias axillaries.

关 键 词：药物化学 结构鉴定 色谱法 南酸枣 黄酮 阿魏酸酯 邻苯二甲酸酯 

分 类 号：R285[医药卫生—中药学]