东京枫杨的甾体等化学成分及其体外抗肿瘤活性

Chemical constituents of Pterocarya tonkinesis and their antitumor activity in vitro

目的阐明民间用于肿瘤治疗的东京枫杨[Pterocarya tonkinesis(Franch.)Dode.]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Sephadex LH-20和硅胶等柱色谱和重结晶等技术,分离精制活性部位的化学成分;根据理化性质和波谱数据鉴定化学结构,用流式细胞术评价抗肿瘤活性结果从东京枫杨茎皮的活性部位分离鉴定了(24S)-麦角甾-4,6,8(14),22-四烯-3-酮(1)、豆甾醇(2)、(24R)-5α-豆甾烷-3,6-二酮(3)、alnin- canone(4)和棕榈酸(5)等5个化合物。其中,化合物1和5对tsFT210细胞示有细胞周期抑制和细胞凋亡诱导活性结论化合物1-5均为首次从枫杨属植物中分离得到,化合物1和5作为东京枫杨的抗肿瘤活性成分属首次报道。

OBJECTIVE: To investigate the antitumor constituents of Pterocarya tonkinesis (Franch.) Dode. METHODS: Bioactive fractions were obtained from the crude extract of P. tonkinesis through a bioassay-guided fractionation and the chemical constituents of the fraction were investigated and purified by the combined use of column chromatography with Sephadex LH-20 and silica gel and recrystallization method. The structures of the compounds obtained were elucidated by spectroscopic methods and the antitumor activity was assayed by flow cytometry using mouse tsFT210 cells. RESULTS: Five pure compounds were isolated from the bioactive fractions and identified as (24S)-ergosta-4,6,8 (14), 22-tetraen-3-one (1), stigmasterol (2), (24R)-5α-stigmastane-3, 6-dione (3), alnincanone (4) and palmitic acid (5), respectively, compound 1 and 5 inhibited the cell cycle of tsFT210 cells at the G2/M phase and induced apoptosis in tsFT210 cells, while compound 2∼4 showed no effect in the present bioassay. CONCLUSION: Compound 1∼5 were all isolated from the genus Pterocarya for the first time, 1 and 5 were reported as the antitumor constituents of this plant Dode. for the first time.