目的 研究旋覆花Inula japonica花序的化学成分及其体外抗肝癌活性。方法 采用多种色谱技术分离纯化，通过HRESIMS、NMR、IR、UV等波谱学方法及计算NMR和ECD确定新化合物的绝对构型，并采用MTT法和克隆形成实验评价化合物对人肝癌HepG2细胞的增殖抑制作用。结果 从旋覆花90%乙醇提取物的醋酸乙酯部位中分离鉴定出6个倍半萜二聚体，分别鉴定为旋覆花倍半萜二聚体内酯T（1）、双旋覆花内酯E（2）、旋覆花倍半萜二聚体内酯U（3）、双旋覆花内酯D（4）、双旋覆花内酯I（5）和双旋覆花内酯X（6），其中化合物1和3为新化合物。活性结果显示，化合物1～6对HepG2细胞均表现出较强的细胞毒性，半数抑制浓度（median inhibition concentration，IC₅₀）值在2.61～13.94 μmol/L；进一步研究表明，化合物1和3能以剂量相关性方式显著抑制细胞活力并减少集落形成数量。结论 化合物1和3为具有抗肝癌活性的新倍半萜二聚体内酯，可作为潜在的抗肿瘤先导化合物供深入研究。

Objective To investigate the chemical constituents from the inflorescences of Inula japonica and their in vitro anti-hepatocellular carcinoma activity. Methods The compounds were isolated and purified by multiple chromatographic techniques.. Their structures were identified by HRESIMS, NMR, IR, UV spectroscopic methods, and the absolute configurations of new compounds were determined by calculated NMR and ECD. The inhibitory effects of the compounds on the proliferation of HepG2 cells were evaluated by MTT assay and colony formation assay. Results Six sesquiterpenoid dimers were isolated from the ethyl acetate fraction of the 90% ethanol extract of I. japonica, among which compounds 1 (inujaponolide T) and 3 (inujaponolide U) were identified as new compounds. The bioactivity screening results showed that compounds 1—6exhibited potent cytotoxicity against HepG2 cells, with IC₅₀ values ranging from 2.61 to 13.94 μmol/L. Furthermore, compounds 1 and 3 inhibited the cell viability and reduced the colony formation of HepG2 cells in a dose-dependent manner. Conclusion Compounds 1 and 3 are new sesquiterpenoid dimers with anti-hepatocellular carcinoma activity, and may serve as potential antitumor lead compounds for further in-depth investigation.

R284.1

云南省地方高校基础研究专项面上项目（202301AO070134）；云南省教育厅科学研究基金青年项目（2024J0889）；省级大学生创新创业训练计划（S202511390017，S202611390065）