千根草的化学成分研究

Study on chemical constituents from Euphorbia thymifolia

研究千根草Euphorbia thymifolia的化学成分。采用硅胶,Sephadex LH-20,MCI,ODS和制备型HPLC等色谱技术,从千根草地上部分的95%乙醇提取物中分离得到13个化合物,包括2个百里香酚类衍生物(1~2),4个生物碱(3~6),5个异香豆素(7~11)和2个鞣花酸(12~13),结构分别鉴定为:(Z)-8,9-dehydro-9,10-diisobutyryloxythymol(1),8-hydroxy-9,10-diisobutyryloxythymol(2),N-(N-benzoyl-L-phenylalanyl)-L-phenylalanol(3),aurantiamide acetate(4),1-carboethoxy-β-carboline(5),isoechinulin A(6),短叶苏木酚酸乙酯(7),euphorhirtin B(8),4,5-去氢诃子裂酸三乙酯(9),euphorhirtin G(10),pomegranatate(11),3,3′,4′-tri-O-methylellagic acid(12),3,3′-di-O-methylellagic acid(13)。化合物1为新化合物,化合物2,3和5~13均为首次从该植物中分离得到。对所有化合物进行了体外抗神经炎症活性筛选,结果显示化合物1~3和7对LPS激活的BV-2小胶质细胞释放NO具有显著抑制作用,IC50分别为0.19,12.93,7.29,25.4μmol·L^-1。

This work was launched to study on the chemical constituents from Euphorbia thymifolia.Thirteen compounds were isolated from the 95%ethanol extract of the aerial parts of E.thymifolia by column chromatographies on silica gel,Sephadex LH-20,MCI,and ODS,and preparative HPLC,including two thymol derivatives(1-2),four alkaloids(3-6),five isocoumarins(7-11),together with two ellagic acids(12-13).All the compounds are listed as follows:(Z)-8,9-dehydro-9,10-diisobutyryloxythymol(1),8-hydro-xy-9,10-diisobutyryloxythymol(2),N-(N-benzoyl-L-phenylalanyl)-L-phenylalanol(3),aurantiamide acetate(4),1-carboethoxy-β-carboline(5),isoechinulin A(6),ethyl brevifolincarboxylate(7),euphorhirtin B(8),4,5-didehydro chebulic acid triethyl ester(9),euphorhirtin G(10),pomegranatate(11),3,3′,4′-tri-O-methylellagic acid(12),3,3′-di-O-methylellagic acid(13).Compound 1 is a new compound.Except for compound 4,the others were isolated from this plant for the first time.All the compounds were screened for anti-neuroinflammatory activity in vitro,and compounds 1-3 and 7 showed significant activity with IC50 values of 0.19,12.93,7.29,25.4μmol·L^-1.