【摘要】 目的:研究橡胶籽种壳的化学成分。方法:通过LH-20和ODS-C18硅胶柱层析以及高压制备液相(HPLC)等色谱方法对橡胶籽种壳的化学成分进行分离,根据理化性质和光谱学数据鉴定化合物结构;采用MTT法评价分离产物对小鼠黑色素瘤细胞B16增殖的作用;应用人白细胞弹性蛋白酶(HLE)抑制剂高通量筛选模型评价分离产物的活性。结果:从橡胶种籽壳中得到9个化合物,分别鉴定为vanillin(1)、coniferal-dehyde(2)、erythro-guaiacylglycerol-β-coniferyl aldehyde ether(3)、threo-guaiacylglycerol-β-coniferyl aldehyde e-ther(4)、(-)-balanophonin(5)、isoamericanol A(6)、americanol A(7)、erythro-guaiacylglycerol-β-O-4’-de-hydrodisinapyl ether(8)、buddlenol A(9);化合物9对小鼠黑色素瘤细胞B16的增殖抑制作用较强,IC50值为20.6μmol.L-1;化合物5～9对人白细胞弹性蛋白酶有抑制活性,其IC50值分别为168,45.5,57.6,171和115μmol.L-1。结论:所有化合物均首次从该植物中得到,化合物9对B16肿瘤细胞的抗肿瘤活性以及化合物5～9的HLE抑制活性均首次报道。更多还原

【Abstract】 Objective: To study the chemical constituents of the seed shell of Hevea brasiliensis.Methods: The compounds were isolated by chromatography on silica gel,LH-20,ODS-C18 and HPLC.Their structures were identified by physicochemical and spectral analysis.MTT assays in vitro were used to explore the inhibitory effect of these compounds on B16 cancer cells,and a high through-put screening method was used to explore the HLE inhibitors.Results: Nine compounds were isolated and identified as vanillin(1),coniferaldehyde(2),erythro-guaiacylglycerol-β-coniferyl aldehyde ether(3),threo-guaiacylglycerol-β-coniferyl aldehyde ether(4),(-)-balanophonin(5),isoamericanol A(6),americanol A(7),erythro-Guaiacylglycerol-β-O-4′-dehydrodisinapyl ether(8),and buddlenol A(9).Compound 9 showed anti-tumor activity against B16 cancer cells with IC50 value of 20.6 μmol·L-1.Compounds 5~9 showed inhibitory activity against human leukocyte elastase with IC50 values of 168,45.5,57.6,171 and 115 μmol·L-1,respectively.Conclusion: All compounds were isolated from this plant for the first time.Compound 9 showed inhibitory activity on B16 cancer cells,and compounds 5~9 were reported as human leukocyte elastase inhibitors for the first time.更多还原