橡胶籽种壳的化学成分研究  

Chemical constituents of the seed shell of Hevea brasiliensis

作　　者：任风芝[1] 陈书红[1] 李丽红[1] 张雪霞[1] 郑智慧[1] 董爱华[1] 

机构地区：[1]华北制药集团新药研究开发有限责任公司微生物药物国家研究工程中心,石家庄050015

出　　处：《中国新药杂志》2012年第19期2311-2315,共5页Chinese Journal of New Drugs

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。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 inhib- itors. Results： Nine compounds were isolated and identified as vanillin（ 1）, coniferaldehyde （2）, erythro-guaiacyl- glycerol-13-coniferyl aldehyde ether（3）, threo-guaiacylglycerol-13-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 mol·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 ceils, and compounds 5 - 9 were reported as human leukocyte elastase inhibitors for the first time.

关 键 词：橡胶 种壳 化学成分 木脂素 抗肿瘤 人白细胞弹性蛋白酶抑制剂 

分 类 号：R932[医药卫生—生药学]