黑果悬钩子化学成分及其PTP1B抑制活性的研究  

Chemical constituents from Rubus caesius and their inhibitory activities on PTP 1B

作　　者：古丽米热.阿力木 沈海涛[1] 郭寒[1] 徐文斌[1] 葛娟[1] 何大俊[1] 

机构地区：[1]石河子大学生命科学学院,新疆石河子832000

出　　处：《中草药》2017年第3期448-452,共5页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金青年科学基金项目(31200259);石河子大学优秀中青年骨干教师培养支持计划项目(3152SMXY04024)

摘　　要：目的研究黑果悬钩子Rubus caesius茎叶的化学成分及其对蛋白酪氨酸磷酸酶1B(PTP1B)的抑制活性。方法利用硅胶柱色谱、Sephadex LH-20柱色谱、半制备液相等色谱方法进行分离纯化,根据核磁共振波谱鉴定化合物结构,利用酶标仪测定不同萃取部位和单体化合物的PTP1B抑制活性。结果从黑果悬钩子茎的醋酸乙酯部位分离得到5个化合物,分别鉴定为柚皮苷(1)、芹菜素-7-O-β-D-吡喃葡萄糖苷(2)、异槲皮苷(3)、金丝桃苷(4)、(-)-表儿茶素3-O-没食子酸(5);从叶的醋酸乙酯部位分离得到2个化合物,分别鉴定为类叶升麻苷(6)、鞣花酸(7)。结论所有化合物均为首次从黑果悬钩子中分离得到。不同的萃取部位均有一定的PTP1B抑制活性,化合物6表现出较好的PTP1B抑制活性,IC_(50)为(27.41±0.61)μg/m L,推测该化合物可能是叶的醋酸乙酯部位中主要活性成分。Objective To investigate the chemical constituents from the stem and leaves of Rubus caesius and the inhibitory activities on PTP 1B. Methods Compounds were separated and purified by silica gel column chromatography, Sephadex LH-20 column chromatography, and preparative liquid chromatography. Their structures were identified by spectral methods. The PTP1 B inhibitory activities were screened by microplate reader. Results Five compounds were obtained from the stems of R. caesius respectively, elucidated as naringin（1）, apigenin-7-O-β-D-glucopyranoside（2）, isoquercitrin（3）, hyperoside（4）, and（-）-epicatechin 3-O-gallate（ECG）（5）, and two compounds were obtained from the leaves respectively, elucidated as acteoside（6） and ellagic acid（7） respectively. Conclusion Compounds 1—7 are isolated from this plant for the first time. Different fractions and compounds showed different PTP1 B inhibitory activities and acteoside showed high PTP1 B inhibitory activity with the IC50 value of（27.41 ± 0.61） μg/m L. This compound may be the main active composition of leaves ethyl acetate fraction.

关 键 词：黑果悬钩子 柚皮苷 芹菜素-7-O-β-D-吡喃葡萄糖苷 异槲皮苷 金丝桃苷 类叶升麻苷 鞣花酸 蛋白酪氨酸磷酸酶1B 

分 类 号：R284.1[医药卫生—中药学]