金樱根中1个新的乌苏烷型三萜皂苷

目的研究蔷薇科植物金樱子Rosa laevigata根的化学成分。方法采用硅胶、Sephadex LH-20、ODS柱色谱、重结晶及半制备液相分离和纯化,根据理化性质和波谱数据鉴定化合物的结构,并运用MTT法对所分离化合物对人宫颈癌HeLa、人胃腺癌BGC823、人结肠癌HCT-116及人肝癌HepG-2细胞的细胞毒活性进行检测。结果从金樱根乙醇提取物中分离得到了9个化合物,分别鉴定为2α,3β,11α,19α-四羟基乌苏-12-烯-28-羧酸-β-D-吡喃葡萄糖基酯(1)、野鸦椿酸(2)、2α,3β,19α-三羟基乌苏-23-醛-12-烯-28-羧酸-β-D-吡喃葡萄糖基酯(3)、野蔷薇苷(4)、苦莓苷F1(5)、2α,3β,19α-三羟基齐墩果-12-烯-28-羧酸-β-D-吡喃葡萄糖基酯(6)、桦木酸(7)、β-谷甾醇(8)和儿茶素(9);其中化合物7对BGC823及HeLa细胞的半数抑制浓度(IC50)分别为19.0和19.6μmol/L,化合物8对BGC823及HeLa细胞的IC50分别为16.2和15.8μmol/L。结论化合物1为新化合物,命名为金樱子皂苷,化合物3为首次从该植物中分离到,化合物7和8对BGC823及HeLa细胞显示出中等强度的细胞毒活性。

A ursane type triterpenoid glycoside from roots of Rosa laevigata

Objective To isolate and elucidate the constituents of the roots of Rosa laevigata.Methods The constituents were isolated by chromatography on silica gel,Sephadex LH-20,ODS,semi-preparation HPLC and recrystallization.The structures were elucidated based on the chemical evidence and spectroscopic data,and all compounds were evaluated for cytotoxic activity on Hela,BGC 823,HCT-116 and HepG-2 cells by MTT assay.Results Nine compounds were obtained:2α,3β,11α,19α-tetra hydroxyurs-12-en-28-oic acid-β-D-glucopyranosyl ester(1),euscaphic acid(2),pinfaensin(3),rosamultin(4),niga-ichigoside F1(5),arjunetin(6),betulic acid(7),β-sitosterol(8),catechin(9).Compounds 7 and 8 showed cytotoxicities against human gastric cancer cells(BGC 823)with the IC50 values of 19.0 and 16.2μmol/L,respectively,and on human cervical cancer cell lines(Hela)with the IC50 value of 19.6 and 15.8μmol/L,respectively.Conclusion Compound 1 is a new triterpenoid glycoside and named as jinyingzhinoside,compound 3 is isolated from R.laevigata for the first time,7 and 8 show moderate cytotoxicities against BGC823 and Hela cells.