Pancreatic lipase inhibitory constituents from Fructus Psoraleae.
10.1016/S1875-5364(20)30043-1
- Author:
Xu-Dong HOU
1
;
Li-Lin SONG
2
,
3
;
Yun-Feng CAO
4
;
Yi-Nan WANG
5
;
Qi ZHOU
1
;
Sheng-Quan FANG
5
;
Da-Chang WU
1
;
Shi-Zhu ZANG
1
;
Lu CHEN
1
;
Yue BAI
1
;
Guang-Bo GE
6
;
Jie HOU
7
Author Information
1. College of Basic Medical Sciences, Dalian Medical University, Dalian 116000, China.
2. Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116000, China
3. Translational Medicine Center, Yueyang Hospital of Integrated Traditional Chinese and Western Medicine & Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai 200000, China.
4. Dalian Runsheng Kangtai Medical Laboratory Co. Ltd., Dalian 116000, China.
5. Translational Medicine Center, Yueyang Hospital of Integrated Traditional Chinese and Western Medicine & Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai 200000, China.
6. Translational Medicine Center, Yueyang Hospital of Integrated Traditional Chinese and Western Medicine & Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai 200000, China. Electronic address: geguangbo@dicp.ac.cn.
7. College of Basic Medical Sciences, Dalian Medical University, Dalian 116000, China. Electronic address: houjie@dlmedu.edu.cn.
- Publication Type:Journal Article
- Keywords:
Bavachalcone;
Fructus Psoraleae;
Inhibition potential;
Isobavachalcone;
Pancreatic lipase
- From:
Chinese Journal of Natural Medicines (English Ed.)
2020;18(5):369-378
- CountryChina
- Language:English
-
Abstract:
Pancreatic lipase (PL), a crucial enzyme in the digestive system of mammals, has been proven as a therapeutic target to prevent and treat obesity. The purpose of this study is to evaluate and characterize the PL inhibition activities of the major constituents from Fructus Psoraleae (FP), one of the most frequently used Chinese herbs with lipid-lowering activity. To this end, a total of eleven major constituents isolated from Fructus Psoraleae have been obtained and their inhibition potentials against PL have been assayed by a fluorescence-based assay. Among all tested compounds, isobavachalcone, bavachalcone and corylifol A displayed strong inhibition on PL (IC < 10 μmol·L). Inhibition kinetic analyses demonstrated that isobavachalcone, bavachalcone and corylifol A acted as mixed inhibitors against PL-mediated 4-methylumbelliferyl oleate (4-MUO) hydrolysis, with the K values of 1.61, 3.77 and 10.16 μmol·L, respectively. Furthermore, docking simulations indicated that two chalcones (isobavachalcone and bavachalcone) could interact with the key residues located in the catalytic cavity of PL via hydrogen binding and hydrophobic interactions. Collectively, these finding provided solid evidence to support that Fructus Psoraleae contained bioactive compounds with lipid-lowering effects via targeting PL, and also suggested that the chalcones in Fructus Psoraleae could be used as ideal leading compounds to develop novel PL inhibitors.
