[关键词]
[摘要]
目的 研究毛叶藜芦Veratrum grandiflorum根茎的化学成分及其抗肿瘤活性。方法 采用硅胶柱色谱、C-18反相柱色谱进行分离纯化,运用MS、NMR等波谱技术鉴定化合物的结构,采用MTT法测定化合物1~6对人肝癌HepG2细胞的细胞毒活性,采用流式细胞术检测化合物3对HepG2细胞凋亡的影响。结果 从毛叶藜芦根茎中分离得到了8个甾体生物碱类化合物,分别鉴定为(3S,15S)-3β-当归酰基-15α-乙酰基棋盘花胺(1)、表红介芬胺(2)、藜芦胺(3)、介芬胺(4)、3-当归酰基棋盘花胺(5)、藜芦托素(6)、veramitaline(7)、veralkamine(8)。结论 化合物1为1个新化合物,化合物7、8为首次从该植物中分离得到,化合物3对HepG2细胞具有中等强度的细胞毒活性,半数抑制浓度(IC50)值为(13.70±0.99)μmol/L,并且能够诱导HepG2细胞发生早期凋亡。
[Key word]
[Abstract]
Objective To study the chemical constituents of the roots and rhizomes of Veratrum grandiflorum and its antitumor activities. Methods The compounds were isolated and purified by silica gel, C-18 reversed phase column chromatography, and their structures were identified by MS and NMR analyses. The cytotoxic activities of compounds 1-6 against HepG2 (human liver cancer cell line) were evaluated by MTT method. The effect of compound 3 on cell apoptosis of HepG2 was detected by flow cytometry. Results Eight steroidal alkaloids were isolated and their structures were identified as (3S,15S)-3β-angeloyl-15α-acetylzygadenine (1), epirubijervine (2), veratramine (3), jervine (4), 3-angeloylzygadenine (5), veratrosine (6), veramitaline (7) and veralkamine (8). Conclusion Compound 1 is a new alkaloid, compounds 7-8 are isolated from this plant for the first time. Compound 3 showed moderate cytotoxic activity against human tumor cell line HepG2 with IC50 value of (13.70±0.99) μmol/L, and induced early apoptosis of HepG2 cells.
[中图分类号]
R284.1
[基金项目]