条叶龙胆中环烯醚萜类化学成分及细胞毒活性研究

摘要

Objective:To study the iridoids in Gentiana manshurica and their cytotoxic activity aiming at the new antitumor drug discovery.Methods:Phytochemical investigation and cytotoxic activity were carried out.Results:Nine iridoids were obtained and elucidated as rehmachingiioside A (1),rehmachingiioside E (2),6-keto-8-acetylharpagide (3),6,7-dehydro8-acetylharpagide (4),scrodentoside A (5),morinlongoside C (6),3'-O-β-D-glucopyranosyl sweroside (7),rehmaglutoside B (8),and rehmaglutoside C (9).Among them,compounds 1,4,5,and 8 exhibited anti-tumor activity against HepG2 cell with IC50values of 13.6,12.0,7.5,and 9.0 μmol · L-1,respectively.Conclusion:The compound 1-9 were isolated from G.manshurica for the first time.%目的:利用植物化学和现代谱学分析相结合的手段,针对性地开展条叶龙胆中特征性成分——环烯醚萜类化学成分的研究,并对所分离得到的环烯醚萜类单体成分进行细胞毒活性试验,为新的抗肿瘤药物研发提供物质基础.方法:运用现代植物化学的研究手段对条叶龙胆进行针对性的提取、分离,并利用包括核磁共振(1D,2D NMR)、质谱等多种谱学手段对其进行结构鉴定,采用MTF方法测定各单体环烯醚萜类化合物的细胞毒活性.结果:从条叶龙胆乙醇提取物中分离得到了9个环烯醚萜类成分,分别鉴定为天目地黄苷A(1),天目地黄苷E(2),6-酮基-8-乙酰钩果草苷(3),6,7-去氢-8-乙酰钩果草苷(4),齿叶玄参苷A(5),大花木巴戟苷C(morinlongoside C,6),3'-O-β-D-吡喃葡萄糖基獐牙菜苷(7),地黄新苷B(8)和地黄新苷C(9).采用MTT方法对化合物1～9进行细胞毒活性评价,结果显示化合物1、4、5、8对人源肝癌细胞HepG2增殖具有抑制活性,IC50值分别为13.6、12.0、7.5、9.0μmol·L-.结论:环烯醚萜类化合物1～9均为从该植物中首次分离得到,且发现了对人源肝癌细胞HepG2增殖有一定抑制活性的环烯醚萜类成分.