湖北旋覆花化学成分及抗结核活性研究

为进一步研究湖北旋覆花花序中的化学成分及抗结核活性。实验采用硅胶柱色谱、反相硅胶柱色谱以及制备型高相液相等方法进行了成分系统研究,肉汤二倍稀释法测定化合物的体外抗结核分支杆菌活性。从其花序中分离得到10个化合物。应用波谱学方法分别鉴定为:7,8-epoxy-9-(isobutyryloxy)thymolisobutyrate(1)、10-(2-methylbutyloxy)-8,9-epoxythymolisobutyrate(2)、stigmasterol(3)、ayapin(4)、ergolide(5)、5,10-epi-2,3-dihydroaromatin(6)、xanthalongin(7)、bigelovin(8)、carpesiolin(9)、aromaticin(10)。化合物1、2、5、6、8～10均为首次从该植物中分离得到。其中化合物5～10均为倍半萜类化合物。化合物5、6、8～10对结核分枝杆菌细胞株具有较好的抑制活性,最小抑制浓度MIC值分别为10.00、30.00、5.00、3.15、3.15μM,9和10的活性效果显著。

Chemical constituents and anti-tuberculosis activity in vitro from flowers of Inula hupehensis Ling

To investigate chemical constituents and anti-tuberculosis activity in vitro from the flowers of Inula hupehensis Ling,various chromatographic techniques,including silica gel column chromatography,ODS and preparative HPLC were used.Anti-tuberculosis activity in vitro was determined by double broth dilution method.Ten compounds were isolated.Their structures were identified on the basis of NMR,MS as 7,8-epoxy-9-(isobutyryloxy)thymolisobutyrate ( 1 ),10-(2-methylbutyloxy)-8,9-epoxythymolisobutyrate ( 2),stigmasterol (3),ayapin (4),ergolide (5 ),5,10-epi-2,3-dihydroaromatin ( 6),xanthalongin (7),bigelovin (8),carpesiolin (9),aromaticin (10).Compounds 1,2,5,6,8-10 were isolated from this plant for the first time.Compounds 5-10 are sesquiterpenoids.Compounds 5,6,8-10 have coninhibitory activity against mycobacterium tuberculosis cell lines.Minimal inhibition concentration MIC as follows:10.00,30.00,5.00,3.15,3.15 μM.