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目的:研究红凉伞Ardisia Crenata的化学成分及其抗肿瘤转移活性。方法:采用硅胶柱色谱、凝胶柱色谱和HPLC制备色谱方法分离纯化得到单体化合物,采用有机波谱方法鉴定化合物结构,进一步以Transwell趋化实验方法测定化合物抗肿瘤转移作用。结果:从红凉伞乙醇提取物中分离得到9个化合物,分别为5-羟甲基糠醛(1),乙基-β-D-吡喃果糖苷(2),丁香酸(3),正丁基-β-D-呋喃果糖苷(4),正丁基-α-D-呋喃果糖苷(5),甲基-α-D-呋喃果糖苷(6),岩白菜素(7),百两金皂苷B(8),车叶草酸(9)。抗肿瘤转移实验结果表明化合物1~9均有明确的抗肿瘤转移作用,其中化合物1,5和8的抗肿瘤转移活性较强,化合物5在质量浓度0.8 mg.L-1下对人乳腺癌细胞MDA-MB-231趋化抑制率达到93.8%。结论:化合物2~6和9均为首次从该植物中分离得到;化合物1~9均具有明确的抗肿瘤转移作用,其中化合物1,5和8的抗肿瘤转移活性较强。
Objective: To study the chemical constituents of Ardisia Crenata and its antitumor activity. Methods: The compounds were separated and purified by silica gel column chromatography, gel column chromatography and HPLC preparative chromatography. The structures of compounds were identified by the organic spectral method. The anti-tumor metastatic activity of the compounds was further determined by Transwell chemotaxis assay. Results: Nine compounds were isolated from the ethanol extract of red umbrella. They were 5-hydroxymethylfurfural (1), ethyl-β-D-fructopyranoside (4), n-Butyl-α-D-fructofuranoside (5), Methyl-α-D-fructofuranoside (6), Bergenin (7) One hundred two gold saponin B (8), car leaf oxalic acid (9). Anti-tumor metastasis experiments showed that compounds 1 to 9 have a clear anti-tumor metastatic effect, in which compounds 1, 5 and 8 have strong antitumor activity. Compound 5 is effective against human breast cancer at a concentration of 0.8 mg.L-1 Chemotactic inhibition rate of cells MDA-MB-231 reached 93.8%. CONCLUSION: Compounds 2 to 6 and 9 were isolated from this plant for the first time. Compounds 1 to 9 all had definite antitumor activity. Among them, compounds 1, 5 and 8 showed strong antitumor activity.