光叶合欢中生物碱类和邻苯二甲酸二酯类抗癌活性成分  

Alkaloidal and phthalate anticancer constituents of Albizia lucidior Nielsen.

作　　者：王元国[1] 崔承彬[1] 韩冰[2] 蔡 裴月湖[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2期65-69,共5页Chinese Journal of Medicinal Chemistry

基　　金：国家重点基础研究发展规划项目 (G19980 5 1113) ;国家杰出青年科学基金项目 (3982 5 12 6 ) ;国家教育部长江学者奖励计划资助项目

摘　　要：目的阐明光叶合欢的抗癌活性成分。方法以细胞凋亡诱导和细胞周期抑制活性为抗癌指标,采用柱色谱、薄层色谱等分离技术并结合流式细胞术,跟踪分离活性成分,利用谱学方法鉴定化学结构。结果从光叶合欢中分离鉴定了布木柴胺K(1)、(+) - 9 -去甲布木柴胺K(2 )、邻苯二甲酸二丁酯(3)、邻苯二甲酸二(2 乙基 己基)酯(4)和β-谷甾醇(5 )。化合物1～4显著诱导K5 6 2细胞凋亡,在低浓度时还将细胞周期抑制在G0 /G1期。结论化合物2为新化合物,化合物1～5为首次从该植物中分离得到,其中1～4为该植物活性成分的首例报道。Aim To explore the anticancer constituents of Albizia lucidior Nielsen.Methods The separation procedure was guided by a flow cytometric bioassay using K562 cells to examine the apoptosis-inducing and cell-cycle-inhibiting activities.Various column chromatography and preparative TLC were employed for the isolation and purification of bioactive constituents.Chemical structures of the compounds obtained were elucidated by the spectroscopic methods.Results Two alkaloids,(-)-budmunchiamine K(1)and(+)-normethyl budmunchiamine K(2),and two phthalates,phthalic acid dibutyl ester(3)and phthalic acid bis-(2-ethylhexyl)ester(4),were isolated and identified as anticancer constituents of A.lucidior together with β-sitosterol(5).Compounds 1～4 significantly inhibite the proliferation of K652 cells in SRB assay.In flow cytometric analysis,compounds 1～4 induce dramatic apoptosis(over 95%)in K562 cells at higher concentrations over 0.4 μg·mL^(-1) for compound 1,6.2 μg·mL^(-1) for compound 2,25 μg·mL^(-1) for compound 3 and 100 μg·mL^(-1) for compound 4 and at lower concentrations compounds 1～4 also inhibited the cell cycle of K562 cells at the G0/G1 phase,while compound 5 shows no activity.Conclusion Compound 2is a new compound.Compounds 1～5 are isolated from A.lucidior for the first time and compounds 1～4 are the first report as the bioactive constituents of A.lucidior.

关 键 词：药物化学 成分分离 结构鉴定 光叶合欢 抗癌 生物碱活性 (+)-9-去甲布木柴胺K 邻苯二甲酸二酯 

分 类 号：R285.5[医药卫生—中药学]