走马胎中的三萜皂苷类成分及其体外抗肿瘤活性研究

Triterpenoid Saponins and the Antitumor Activity from the Rhizome of Ardisia Gigantifolia Stapf

目的研究走马胎根茎的三萜皂苷类成分及其体外抗肿瘤活性。方法采用溶剂萃取和柱色谱方法分离纯化,根据理化性质和波谱学数据鉴定化合物结构。采用MTT法测试三萜皂苷化合物的抗肿瘤活性。结果分离得到了7个三萜皂苷类化合物,包括3β-O-{β-D-吡喃木糖基-(1→2)β--D吡-喃葡萄糖基-(1→4)α--L吡-喃阿拉伯糖基}西-克拉敏A(1);3β-O-{α-L吡-喃鼠李糖基-(1→3)-[β-D-吡喃木糖基-(1→2)]β--D吡-喃葡萄糖基-(1→4-[β-D吡-喃葡萄糖-(1→2)]α--L-吡喃阿拉伯糖基}-西克拉敏A(2);lysikoianoside(3);3β-O-β-L吡-喃鼠李糖基-(1→3)-[β-D-吡喃葡萄糖基-(1→3)-β-D-吡喃木糖基-(1→2)]β--D-吡喃葡萄糖基-(1→4)-[β-D-吡喃葡萄糖基-(1→2)]α--L吡-喃阿拉伯糖基-西克拉敏A(4),3β-O-{β-L吡-喃鼠李糖基-(1→3)-[β-D吡-喃木糖基-(1→2)]β--D吡-喃葡萄糖基-(1→4)-[β-D-6-O乙-酰氧基-吡喃葡萄糖基(1→2)]α--L-吡喃阿拉伯糖基}-西克拉敏A(5),Ard isiacrisp in A(6)和3β-o-{α-L-rhamnopyranosyl-(1→3)-[β-D-xylopyranose-(1→2)]β--D-glucopyranosyl-(1→4)α--L-arab inopyranosyl}-3β-hydroxy-13β,28-epoxy-oleanan-16-oxo-30-al(7)。结论化合物1和3为首次从该植物中分离得到,化合物7首次从该属植物中分离得到。其中化合物2对BCG-823,EJ和Hepg2细胞有较好的抑制活性(IC50分别为0.29,9.99和2.03μg/m l)。化合物3对EJ细胞有选择性抑制作用(IC50为7.20μg/m l),化合物7对Hepg2细胞有选择性抑制活性(IC50为8.53μg/m l)。

Objective To study triterpenoid saponins and the antitumor activity of the 60% ethanol extract of the rhizome of Ardisia gigantifolia Stapf.Methods The chemical components were isolated by solvent extraction and column chromatography and their structures were identified on the basis of physical-chemical constants and spectral data.The antitumor activities of the compounds were screened by MTT methods.Results Seven triterpenoid saponins were isolated and identified as 3β-O-{β-D-xylopyranosyl-（1→2）-β-D-glucopyr-anosyl-（1→4）-α-L-arabinopyranosyl}-3β-hydroxy-13β,28-epoxy-16β-hydroxy-30-al（1）;cyclamiretin A 3β-O-α-L-rhamnopyranosyl（1→3）-[β-D-xylopyranosyl-（1→2）]-β-D-glucopyranosyl-（1→4）-[β-D-glucopyranosyl（1→2）]-α-L-arabinopyranoside（2）;lysikoianoside（3）;cyclamiretin A 3β-O-α-L-rhamnopyranosyl-（1→3）-[β-D-glucopyranosyl-（1→3）-β-D-xylopyranosyl-（1→2）]-β-D-glucopyranosyl-（1→4）-[β-D-glucopyranosyl-（1→2）]-α-L-arabinopyranoside（4）,3β-O-{α-L-rhamnopyranosyl-（1→3）-[β-D-xylopyranosyl-（1→2）]-β-D-galactopyranosyl-（1→4）-[β-D-6-O-acetyl-glucopranosyl-（1→2）]-α-L-arabinopyranoside}-cyclamiretin A（5）,Ardisiacri-dpin A（6） and 3β-o-{α-L-rhamnopyranosyl-（1→3）-[β-D-xylopyranose-（1→2）]-β-D-glucopyranosyl-（1→4）-α-L-arabinopyranosyl}-3β-hydroxy-13β,28-epoxyoleanan-16-oxo-30-al（7）.Conclusion Compound 1 and 3 were obtained from this plant and 7 from this genus for the first time.Among the compounds,No.2 showed cytotoxic activity of 0.29,9.99 and 2.03 μg/ml（IC50） in BCG-823,EJ and Hepg2 cells respectively.Compound 3 showed selective cytotoxic activity to EJ cells（IC50 7.20 μg/ml）.Compound 7 showed cytotoxic activity of 8.53 μg/ml（IC50） in Hepg2 cells.