摘要
目的:研究华中枸骨Ilex centrochinensis叶的化学成分及主要化合物抗肿瘤活性。方法:利用硅胶,sephadex LH-20,HPLC等各种色谱技术进行分离纯化,通过理化性质和NMR等波谱数据进行结构鉴定,采用MTT法对分离得到的主要单体化合物进行抗肿瘤活性评价。结果:从华中枸骨叶95%乙醇提取物的乙酸乙酯萃取物中分离得到10个化合物,分别鉴定为对苯二酚(1),(2S)-5,4'-二羟基-7,3'-二甲氧基黄烷(2),(2S)-5,4'-二羟基-7-甲氧基黄烷(3),山柰酚(4),槲皮素(5),柚皮素(6),熊果酸(7),熊果醇(8),齐墩果酸(9),β-谷甾醇(10);化合物2,3抑制人肝癌细胞系HuH7的半数有效浓度IC50分别为8.98,13.04 mg.L-1,化合物7～9抑制Caco-2细胞的IC50分别为28.52,38.28,33.04 mg.L-1。结论:1～5,7,8均为首次从该植物中分离获得,其中化合物1～3为首次从该属植物中分离得到。化合物2,3对人肝癌细胞HuH7具有较强的细胞毒活性,化合物7～9对Caco-2细胞有弱的细胞毒作用。
Objective： To investigate the chemical constituents in leaves of llex centrochinensis and their antitumor bioactivity. Method： Various chromatography techniques such as column chromatography on silica gel, Sephadex LH-20 and preparative HPLC were used to isolate and purify the compounds and their structures were identified by spectral data and physicochemical properties. Their antitumor effect was tested by MTI＂ method. Result： Ten compounds were isolated and identified as 1,4-benzenediol （1）, （2S）- 5, 4＇-dihydroxy-7,3 ＇-dimethoxyflavan （2）, （2S） -5,4＇-dihydroxy-7-methoxyflavan （ 3 ）, kaempferol （ 4 ）, quercetin （ 5 ）, naringenin （ 6）, ursolic acid （7）, uvaol （8）, oleanolic acid （9） and fl-sitosterols （10）. Conclusion： Compounds 1-5, 7, 8 were isolated from the species for the first time, among which compounds 1-3 were isolated from the llex genus for the first time. Compounds 2 and 3 showed strong cytotoxic activity against Huh7 cell lines with ICs0 values of 8.98,13.04 mg L-1, respectively. Compounds 7-9 exhibi- ted weak cytotoxic activity against Caco-2 cell lines with ICso values of 28.52, 38. 28, 33.04 mg L-1, respectively.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2013年第3期354-357,共4页
China Journal of Chinese Materia Medica
基金
湖北省自然科学基金项目(2011CDB066)
湖北省教育厅优秀中青年人才项目(Q20120109)
关键词
华中枸骨
化学成分
黄烷
细胞毒活性
Ilex centrochinensis
chemical constituents
flavane
cytoxic activity
