密脉鹅掌柴的化学成分及其抗肿瘤活性  

Chemical constituents of Schefflera venulosa and their antitumor activities

作　　者：刘睿[1] 顾谦群[1] 崔承彬[1,2] 韩冰[3] 蔡兵[3] 刘红兵[1] 

机构地区：[1]海洋药物教育部重点实验室,中国海洋大学海洋药物与食品研究所,山东青岛266003 [2]军事医学科学院毒物药物研究所,天津300384 [3]天津生物医药研究所

出　　处：《中草药》2005年第3期328-332,共5页Chinese Traditional and Herbal Drugs

基　　金：国家杰出青年科学基金资助项目 (3 982 5 12 6) ;国家 973项目 (G19980 5 1113 ) ;教育部长江学者奖励计划基金资助

摘　　要：目的　阐明民间用于癌症治疗的密脉鹅掌柴Schefflera venulosa的化学成分及其抗肿瘤活性。方法　用小鼠乳腺癌ts FT2 10细胞的流式细胞术筛选模型,确定抗肿瘤活性部位;利用Sephadex L H- 2 0、硅胶等柱色谱,分离活性部位的化学成分;根据理化性质和波谱数据鉴定化合物的化学结构,用流式细胞术和SRB法初步评价化合物对ts FT2 10和K5 6 2细胞的抗肿瘤活性。结果　从密脉鹅掌柴活性部位分离鉴定了9个化合物:2 -羟基- 3苯胺羰基- 1-偶氮苯基-萘( )、大黄酚( )、2 ,6 -二甲氧基对苯醌( )、正十六烷酸( )、正十八烷酸( )、正二十六烷酸( )、4 ,2 2 -二烯- 3-酮豆甾烷( )、5 ,2 2 -二烯- 7-酮- 3β-羟基豆甾烷( )和β-谷甾醇( ) ;活性测试结果表明化合物 、对K5 6 2细胞有增殖抑制活性,其IC50 值分别为5 2 .5 0和2 5 .5 0μg/m L ,化合物 对在30μg/m L的低浓度对ts FT2 10细胞具有细胞周期G2 /M期抑制活性,而在10 0 μg/m L 的高浓度时却呈现显著的细胞周期G2 /M期抑制和细胞凋亡诱导活性。结论　化合物 为新天然产物,中文俗名为80 8猩红(80 8Scarlet) ,除β-谷甾醇外,其余均系首次从密脉鹅掌柴中分离得到。化合物 的抗肿瘤活性为首次发现,化合物 ～ 为该植物抗肿瘤活性成分为首次报道。Objective To investigate the antitumor constituents from Schefflera venulosa, a Chinese folk medicine used for the treatment of cancer. Methods Bioactive fractions were obtained from the crude extract of S. venulosa, and the chemical constituents of the fraction were investigated to obtain pure compounds by the combined use of column chromatography over Sephadex LH-20 method. The structures of the obtained compounds were elucidated by spectroscopic method and the antitumor activities were assayed using mouse tsFT210 cells and K562 cell line by flow cytometry and SRB method. Results Nine pure compounds were isolated from the bioactive fractions of the crude extract of S. venulosa and they were identified as 2-hydroxy-3-(phenylaminocarbonyl)naphthalene-1-azobenzene (Ⅰ), chrysophanol (Ⅱ), 2, 6-dimetmoxyl p-benzoquinone (Ⅲ), n-hexadecanoic acid (Ⅳ), n-stearic acid (Ⅴ), n-hexacosnic acid (Ⅵ), stigmasta-4, 22-dien-3-one (Ⅶ), 3β-hydroxystigmasta-5, 22-dien-7-one (Ⅷ), β-sitosterol (Ⅸ), respectively. Among them, Ⅱ and Ⅲ inhibited the K562 cells with IC 50 (52.50 and 25.50 μg/mL), respectively, and compound Ⅳ inhibited the cell cycle of tsFT210 cells at the G 2/M phase. Conclusion Compound Ⅰ is a new natural product named as 808 Scarlet and Ⅱ-Ⅷ are isolated from S. venulosa for the first time. The antitumor activity of compound Ⅲ has been found first. Compounds Ⅱ-Ⅳ provide the first example of antitumor constituents of the same plant.

关 键 词：密脉鹅掌柴 偶氮化合物 醌类化合物 脂肪酸类 抗肿瘤活性 

分 类 号：R284.2[医药卫生—中药学]