目的 研究土家族藥物扣子七Panax japonicus var. major中三萜皂苷類成分，對其抑制腫瘤細胞增殖活性進行篩選，并初步探討化合物結構與活性的關系。方法 應用多種色譜方法對土家族藥物扣子七正丁醇部位進行分離，所分離化合物運用核磁共振方法進行結構鑒定，應用MTT法測定分離化合物對體外培養(yǎng)人腫瘤細胞增殖的影響。結果 從扣子七根莖正丁醇部位分離得到14個三萜皂苷，分別鑒定為竹節(jié)參皂苷IVa甲酯（1）、竹節(jié)參皂苷IVa丁酯（2）、竹節(jié)參皂苷IV（3）、竹節(jié)參皂苷IVa（4）、28-去糖竹節(jié)參皂苷IVa（5）、齊墩果酸-3-O-β-D-（6'-甲酯）-吡喃葡萄糖醛酸苷（6）、（24R）-珠子參苷R₁（7）、（24R）-擬人參皂苷F11（8）、（20S）-三七皂苷R₂（9）、（20S）-人參皂苷Rg₂（10）、人參皂苷Rg₁（11）、人參皂苷Re（12）、人參皂苷Rd（13）、竹節(jié)參皂苷V甲酯（14）。活性研究結果顯示，化合物5和6對胃癌BGC-823細胞、結腸癌HCT-116細胞、宮頸癌HeLa細胞及肝癌HepG2細胞均顯示了較強的活性，呈良好的劑量依賴關系，其中化合物5對BGC-823、HCT-116細胞的IC₅₀分別為9.94、14.17 μmol/L，化合物6對肝癌HepG2細胞的抑制作用最強（IC₅₀＝12.70 μmol/L）。結論 首次從扣子七中分離得到化合物6并報道了其光譜數(shù)據(jù)；其部分化學成分顯示出抗腫瘤活性，其抗腫瘤活性與齊墩果烷型皂苷密切相關，且活性強弱可能與C-28取代基有關聯(lián)，相關抗腫瘤機制值得進一步研究。

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

湖南省自然科學基金科教聯(lián)合項目（2017JJ5041）；國家自然科學基金青年基金資助項目（81703819；湖南省大學生研究性學習和創(chuàng)新性實驗計劃項目（2018-413）