粉防己根的化学成分及抗肝纤维化活性研究

Chemical constituents from the roots of Stephania tetrandra and their anti-liver fibrosis activity

研究粉防己根的化学成分和抗肝纤维化活性。采用硅胶、Sephadex LH-20、ODS和半制备HPLC对粉防己根的乙醇提取物进行分离纯化得到13个化合物。根据化合物的理化性质和波谱数据鉴定其结构,分别为cyclanoline(1)、coclaurine(2)、5-hydroxymethyl-1-[2-(4-hydroxyphenyl)-ethyl]-1H-pyrrole-2-carbaldehyde(3)、isosalsoline(4)、thalifoline(5)、northalifoline(6)、2-甲基-3-羟基吡啶(7)、(+)-lyoniresinol(8)、icariside B5(9)、丁香酸(10)、对羟基苯乙酸(11)、对羟基苯甲酸(12)、对羟基苯乙酸甲酯(13)。化合物1~13为首次从该植物中分离得到,在千金藤属植物中化合物3、4、6~9也未见报道。初步评价了化合物1~13的抗肝纤维化活性,化合物2、5、6、10~12对TGF-β1诱导的LX-2细胞增殖具有显著抑制作用。

The chemical constituents from roots of Stephania tetrandra and their anti-liver fibrosis activity were studied.The roots of Stephania tetrandra were extracted with EtOH,and the extractions were separated on column chromatography of silica gel,Sephadex LH-20,ODS and semi-preparative HPLC to yield 13 compounds.According to the physical and chemical properties and spectral data,13 compounds were identified as cyclanoline(1),coclaurine(2),5-hydroxymethyl-1-[2-(4-hydroxyphenyl)-ethyl]-1H-pyrrole-2-carbaldehyde(3),isosalsoline(4),thalifoline(5),northalifoline(6),2-methyl-3-hydrox ypyridine(7),(+)-lyoniresinol(8),icariside B5(9),syringic acid(10),4-hydroxyphenylacetic acid(11),4-hydroxybenzoic acid(12),p-hydroxyphenylacetic acid methyl ester(13).Compounds 1-13 are isolated from this plant for the first time.And compounds 3,4,6-9 have never been reported before from the genus Stephania.The compounds 1-13 were preliminarily examined for anti-liver fibrosis activity.Compounds 2,5,6,10-12 showed antiproliferative activities in LX-2 induced by TGF-β1.