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中国药学(英文版) ›› 2020, Vol. 29 ›› Issue (5): 305-313.DOI: 10.5246/jcps.2020.05.028

• 【研究论文】 •    下一篇

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

范靖然1,2, 董泽源2, 匡易2, 周艳霞2, 乔雪2, 叶敏2*   

  1. 1. 北京中医药大学 中药学院, 北京 100029
    2. 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
  • 收稿日期:2020-03-14 修回日期:2020-04-15 出版日期:2020-05-31 发布日期:2020-05-10
  • 通讯作者: Tel.: +86-10-82801516, Fax: +86-10-82802024, E-mail: yemin@bjmu.edu.cn
  • 基金资助:
    National Natural Science Foundation of China (Grant No. 81891010/81891011), National Mega-project for Innovative Drugs (Grant No. 2018ZX09711001-008-003), and Science & Technology Department of Xinjiang Uygur Autonomous Region (Grant No. 2018AB012).

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

Jingran Fan1,2, Zeyuan Dong2, Yi Kuang2, Yanxia Zhou2, Xue Qiao2, Min Ye2*   

  1. 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
  • Received:2020-03-14 Revised:2020-04-15 Online:2020-05-31 Published:2020-05-10
  • Contact: Tel.: +86-10-82801516, Fax: +86-10-82802024, E-mail: yemin@bjmu.edu.cn
  • Supported by:
    National Natural Science Foundation of China (Grant No. 81891010/81891011), National Mega-project for Innovative Drugs (Grant No. 2018ZX09711001-008-003), and Science & Technology Department of Xinjiang Uygur Autonomous Region (Grant No. 2018AB012).

摘要:

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12为新化合物, 其结构采用1D2D NMRHR-MS等技术进行鉴定。分别筛选11个化合物对PTP1Bα-葡萄糖苷酶的抑制活性, 发现化合物1210PTP1B酶有较好的抑制活性, IC50值分别是1.434.713.79 μM; 化合物2410抑制α-葡萄糖苷酶的IC50值分别是13.6111.1317.48 μM

关键词: 地上部分, PTP1B酶, α-葡萄糖苷酶, 乌拉尔甘草

Abstract:

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 1D, 2D NMR and HR-MS data analyses. Compounds 1, 2 and 10 showed potent inhibitory activities against PTP1B, with IC50 values of 1.43, 4.71 and 3.79 μM, respectively. Compounds 2, 4 and 10 inhibited α-glucosidase with IC50 values of 13.61, 11.13 and 17.48 μM, respectively. 

Key words: The aerial parts, PTP1B, α-Glucosidase, Glycyrrhiza uralensis

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