[关键词]
[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tsFT210细胞的流式细胞术筛选模型,确定抗肿瘤活性部位;利用Sephdex LH-20、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tsFT210和K562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(Ⅰ)、大黄酚(Ⅱ)、2,6-二甲氧基对苯醌(Ⅲ)、正十六烷酸(Ⅳ)、正十八烷酸(Ⅴ)、正二十六烷酸(Ⅵ)、4,22-二烯-3-酮豆甾烷(Ⅶ)、5,22-二烯-7-酮-3β-羟基豆甾烷(Ⅶ)和β-谷甾醇(Ⅸ);活性测试结果表明化合物Ⅱ、Ⅲ对K562细胞有增殖抑制活性,其IC50值分别为52.50和25.50μg/mL,化合物Ⅳ对在30μg/mL的低浓度对tsFT210细胞具有细胞周期G2/M期抑制活性,而在100μg/mL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Ⅰ为新天然产物,中文俗名为808猩红(808Scarlet),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Ⅲ的抗肿瘤活性为首次发现,化合物Ⅱ~Ⅳ为该植物抗肿瘤活性成分为首次报道.
[Key word]
[Abstract]
0bjective 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 cornpounds by the combined use of column chromatography over Sephadex LH一20 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 2一hydroxy一3一(phenylaminocarbonyl)naphthalene一1一azobenzene(I),chrysophanol(Ⅱ),2,6一dimetmoxyl P—benzoquinone(Ⅲ),咒一hexadecanoic acid(IV),z—stearic acid(V),咒一hexacosnic acid(Ⅵ),stigmasta一4,22一dien一3一one(Ⅶ),3p—hydroxystigmasta一5,22一dien-7-one(Ⅷ),p—sitosterol(Ⅸ),respectively.Among them,ⅡandⅢinhibited the K562 cells with IC50(52.50 and 25.50/19/mL),respectively,and compound IV inhibited the cell cycle of tsFT 21 0 cells at the G2/M phase.Conclusion Compound I iS a new natural product named as 808 Scarlet andⅡ一Ⅶare isolated from S.venulosa for the first time.The antitumor activity of compoundm has been found first.CompoundsⅡ一Ⅳprovide the first example of antitumor constituents of the same plant.
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[基金项目]
国家杰出青年科学基金资助项目(39825126);国家973项目(G1998051113);教育部长江学者奖励计划基金资助