Chemical constituents of the aerial parts of Glycyrrhiza uralensis and their inhibitory activities against PTP1B andα-glucosidase  

乌拉尔甘草地上部分的化学成分及其PTP1B与α-葡萄糖苷酶抑制活性研究

作　　者：Jingran Fan Zeyuan Dong Yi Kuang Yanxia Zhou Xue Qiao Min Ye 范靖然;董泽源;匡易;周艳霞;乔雪;叶敏(北京中医药大学中药学院,北京100029;北京大学药学院天然药物及仿生药物国家重点实验室,北京100191)

机构地区：[1]School of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 100029,China [2]State Key Laboratory of Natural and Biomimetic Drugs,School of Pharmaceutical Sciences,Peking University Health Science Center,Beijing 100191,China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2020年第5期305-313,共9页中国药学（英文版）

基　　金：National Natural Science Foundation of China(Grant No.81891010/81891011);National Mega-project for Innovative Drugs(Grant No.2018ZX09711001-008-003);Science&Technology Department of Xinjiang Uygur Autonomous Region(Grant No.2018AB012).

摘　　要：In the present study,a total of 11 compounds were isolated from the aerial parts of Glycyrrhiza uralensis,including two new compounds,glycyuralin Q(1)and glycyuralin R(2),and nine known compounds,including licoriphenone(3),orobol(4),trifoliol(5),7,2′,4′-trihydroxy-5-methoxy-3-arylcoumarin(6),11-hydroxy-9(Z),12(Z)-octadecadienoic acid(7),11-hydroxy-9(E),12(E)-octadecadienoic acid(8),licoricone(9),glycyrin(10),and 2′-hydroxyformononetin(11).Structures of the new compounds were identified by 1 D,2 D NMR and HR-MS data analyses.Compounds 1,2 and 10 showed potent inhibitory activities against PTP1 B,with IC50 values of 1.43,4.71 and 3.79μM,respectively.Compounds 2,4 and 10 inhibitedα-glucosidase with IC50 values of 13.61,11.13 and 17.48μM,respectively.从乌拉尔甘草地上部分分离得到11个化合物,分别是glycyuralin Q(1),glycyuralin R(2),licoriphenone(3),奥洛波尔(4),trifoliol(5),7,2′,4′-三羟基-5-甲氧基-3-香豆素(6),11-羰基-9(Z),12(Z)-十八碳二烯酸(7),11-羰基-9(E),12(E)-十八碳二烯酸(8),甘草利酮(9),格里西轮(10),2′-羟基刺芒柄花素(11)。其中1和2为新化合物,其结构采用1D、2D NMR及HR-MS等技术进行鉴定。分别筛选11个化合物对PTP1B及α-葡萄糖苷酶的抑制活性,发现化合物1、2和10对PTP1B酶有较好的抑制活性,其IC50值分别是1.43、4.71和3.79μM;化合物2、4和10抑制α-葡萄糖苷酶的IC50值分别是13.61、11.13和17.48μM。

关 键 词：The aerial parts PTP1B Α-GLUCOSIDASE Glycyrrhiza uralensis 

分 类 号：R284[医药卫生—中药学]