目的 研究土家族药物扣子七Panax japonicus var. major中三萜皂苷类成分，对其抑制肿瘤细胞增殖活性进行筛选，并初步探讨化合物结构与活性的关系。方法 应用多种色谱方法对土家族药物扣子七正丁醇部位进行分离，所分离化合物运用核磁共振方法进行结构鉴定，应用MTT法测定分离化合物对体外培养人肿瘤细胞增殖的影响。结果 从扣子七根茎正丁醇部位分离得到14个三萜皂苷，分别鉴定为竹节参皂苷IVa甲酯（1）、竹节参皂苷IVa丁酯（2）、竹节参皂苷IV（3）、竹节参皂苷IVa（4）、28-去糖竹节参皂苷IVa（5）、齐墩果酸-3-O-β-D-（6'-甲酯）-吡喃葡萄糖醛酸苷（6）、（24R）-珠子参苷R₁（7）、（24R）-拟人参皂苷F11（8）、（20S）-三七皂苷R₂（9）、（20S）-人参皂苷Rg₂（10）、人参皂苷Rg₁（11）、人参皂苷Re（12）、人参皂苷Rd（13）、竹节参皂苷V甲酯（14）。活性研究结果显示，化合物5和6对胃癌BGC-823细胞、结肠癌HCT-116细胞、宫颈癌HeLa细胞及肝癌HepG2细胞均显示了较强的活性，呈良好的剂量依赖关系，其中化合物5对BGC-823、HCT-116细胞的IC₅₀分别为9.94、14.17 μmol/L，化合物6对肝癌HepG2细胞的抑制作用最强（IC₅₀＝12.70 μmol/L）。结论 首次从扣子七中分离得到化合物6并报道了其光谱数据；其部分化学成分显示出抗肿瘤活性，其抗肿瘤活性与齐墩果烷型皂苷密切相关，且活性强弱可能与C-28取代基有关联，相关抗肿瘤机制值得进一步研究。

Objective To study the active triterpenoid saponins of Tujia ethnomedicine Kouziqi (Panax japonicus var. major). The antitumor activity was screened and the relationship between the structure and activity of the compounds was discussed. Methods The ethanol extract of Kouziqi was isolated by Silica gel, ODS and MCI column chromatograph and purified by preparative HPLC. The structures were elucidated on the basis of spectroscopic analysis and compared with literatures. Using MTT assay to detect the cytotoxicity of 14 compounds in BGC-823, HCT-116, Hela, HepG-2 cells. Results A total of 14 known compounds were isolated from Tujia ethnomedicine Kouziqi and determined as chikusetsusaponin IVa methyl ester (1), chikusetsusaponin IVa butyl ester (2), chikusetsusaponin IV (3), chikusetsusaponin IVa (4), 28-desglucosylchikusetsusaponin IVa (5), oleanolic acid-3-O-β-D-(6'-methylester)-glucuronopyranoside (6), (24R)-majonoside R1 (7), (24R)-pseudoginsinoside F11 (8), (20S)-notoginsinoside-R₂ (9), (20S)-ginsenoside Rg₂ (10), ginsenoside Rg₁ (11), ginsenoside Re (12), ginsenoside Rd (13) and chikusetsusaponin-V methyl ester (14). Among the 14 compounds, compounds 5 and 6 showed dose-dependent cytotoxicity to BGC-823, HCT-116, Hela and HepG-2 cells. Compound 5 had cytotoxicity in BGC-823 and HCT-116 cells with IC₅₀ values of 9.94 and 14.17 μmol/L, respectively. Compound 6 had the best cytotoxicity in HepG-2 cells with IC₅₀ value of 12.70 μmol/L. Conclusion Compound 6 is isolated from Kouziqi for the first time and its spectral data were reported. The antineoplastic activity of Tujia ethnomedicine Kouziqi is based on the oleanolic acid-type triterpenoid saponins and related to the substituents of C-28, but the mechanism still needs to be deeply studied.

R284.1

湖南省自然科学基金科教联合项目（2017JJ5041）；国家自然科学基金青年基金资助项目（81703819；湖南省大学生研究性学习和创新性实验计划项目（2018-413）