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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。
Objective: To study the chemical composition of rubber seed shell. Methods: The chemical constituents of rubber seed shell were separated by column chromatography on silica gel column (LH-20), ODS-C18 column and high pressure liquid chromatography (HPLC). The structures of the compounds were identified by physico-chemical properties and spectroscopic data. The effect of the isolated product on the proliferation of mouse melanoma B16 cells was evaluated. The high-throughput screening model of human leukocyte elastase (HLE) inhibitor was used to evaluate the activity of the isolated products. RESULTS: Nine compounds were identified from the rubber seed shell and identified as vanillin (1), coniferal-dehyde (2), erythro-guaiacylglycerol-β-coniferyl aldehyde ether (3), threo-guaiacylglycerol-β -coniferyl aldehyde e (-) - balanophonin (5), isoamericanol A (6), americanol A (7), erythro-guaiacylglycerol-β-O-4’-de- hydrodisinapyl ether (8), buddlenol A ) .Compound 9 had a stronger inhibitory effect on the proliferation of mouse melanoma cell line B16 with an IC50 value of 20.6 μmol·L-1. Compounds 5 to 9 had inhibitory activity on human leukocyte elastase with IC50 values of 168, 45.5, 57.6, 171 and 115 μmol.L-1. CONCLUSION: All the compounds were obtained from this plant for the first time. The antitumor activity of compound 9 against B16 tumor cells and the inhibitory activity against HLE of compounds 5 to 9 were all reported for the first time.