论文部分内容阅读
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 study the chemical constituents of Rubus caesius stems and leaves and their inhibitory activity on protein tyrosine phosphatase 1B (PTP1B). Methods The compounds were separated and purified by silica gel column chromatography, Sephadex LH-20 column chromatography and semi-preparative liquid chromatography. The structures of compounds were identified by 1H NMR. The PTP1B inhibitory activities of different extracts and monomer compounds were determined by microplate reader. Results Five compounds were isolated from the ethyl acetate fraction of Fructus Aurantii and identified as naringin (1), apigenin-7-O-β-D-glucopyranoside (2) (4), (-) - epicatechin 3-O-gallic acid (5). Two compounds were isolated from the ethyl acetate fraction of leaves and identified as leaf-like ascending Glycosides (6), ellagic acid (7). Conclusion All the compounds were isolated from Rubus nigra for the first time. PTP1B inhibitory activity was detected in different extraction sites, while compound 6 showed better PTP1B inhibitory activity (IC 50) of (27.41 ± 0.61) μg / mL, suggesting that this compound may be in the ethyl acetate fraction of leaves The main active ingredient.