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[摘要]
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19.6 μmol/L,化合物8对BGC823及HeLa细胞的IC50分别为16.2和15.8 μmol/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。
[Key word]
[Abstract]
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 16.2 μmol/L, respectively, and on human cervical cancer cell lines (Hela) with the IC50 value of 19.6 and 15.8 μmol/L, respectively. Conclusion Compound 1 is a new triterpenoid glycoside and named as rosalaevioside, compound 3 is isolated from R. laevigata for the first time, 7 and 8 show moderate cytotoxicities against BGC823 and Hela cells.
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[基金项目]
湖南省自然科学基金项目(2016JJ6118);湖南省中医药管理局中医科研项目(201673);侗医药研究湖南省重点实验室平台建设(2017CT5025);湖南中医药大学中药学开放基金项目(ZY201503)