关龙胆抗肿瘤活性成分的研究

Study on the anti-tumor active constituents of Gentiana scabra

目的研究关龙胆Gentiana Scabra Bung中的抗肿瘤活性成分。方法采用色谱法分离关龙胆根中的化学成分,根据理化性质及波谱(MS、NMR、DEPT、1H-1H COSY、HSQC等)鉴定结构;采用MTT'法筛选分离所得化合物对宫颈癌细胞(He-la)、肝癌细胞(HepG-2)的抗肿瘤活性。结果从关龙胆中分离鉴定了10个单体化合物,分别为chirat-17(22)-en-3-one(Ⅰ)、β-谷甾醇(Ⅱ)、α-香树脂醇棕榈酸酯(Ⅲ)、chirat-16-en-3-one(Ⅳ)、chiratenol(Ⅴ)、3,4-dihydro-1H,6H,8H-naphtho[1,2-c:4,5-c',d']dipyr-ano-1,8-dione(Ⅵ)、胡萝卜苷(Ⅶ)、胆甾醇(Ⅷ)、龙胆苦苷(Ⅸ)、蔗糖(Ⅹ)。结论化合物Ⅲ、Ⅵ、Ⅷ、Ⅹ为首次从关龙胆中分离得到;化合物Ⅳ、Ⅴ、Ⅶ、Ⅹ对Hela和HepG-2细胞的增殖有一定的抑制作用。

OBJECTIVE To study the anti-tumor active constituents from Gentiana scabra Bung.METHODS The chemical constituents were isolated from the Gentiana scabra Bung by ion exchange resin.Their structures were elucidated on the basis of physico-chemical properties and spectral data（MS,NMR,DEPT,1H-1H COSY,HSQC et al）.The anti-tumor active constituents on cervical（Hela） and livercancer（HepG-2） were selected by MTT.RESULTS Ten compounds were isolated and identified form the Gectiana scabra Bung which were chirat-17（22）-en-3-one（Ⅰ）,β-sistosterol（Ⅱ）,α-Amyrinpalmitate（Ⅲ）,chirat-16-en-3-one（Ⅳ）,chiratenol（Ⅴ）,3,4-dih-ydro-1H,6H,8H-naphtho[1,2-c：4,5-c′,d′]dipyrano-1,8-dione（Ⅵ）,β-daucosterol（Ⅶ）,cholesterol（Ⅷ）,gentiopicroside（Ⅸ）,and d-sucurose（Ⅹ）.CONCLUSION Compounds Ⅲ,Ⅵ,Ⅷ and Ⅹ were isolated from this plant for the first time.Compounds Ⅳ,Ⅴ,Ⅶ and Ⅹ exhibited moderate anti-tuomr effect against Hela and HepG-2 lines.