2. Academic Validation
  3. Natural constituents from Cortex Mori Radicis as new pancreatic lipase inhibitors

Natural constituents from Cortex Mori Radicis as new pancreatic lipase inhibitors

  • Bioorg Chem. 2018 Oct;80:577-584. doi: 10.1016/j.bioorg.2018.07.011.
Xu-Dong Hou 1,  Guang-Bo Ge 2,  Zi-Miao Weng 3,  Zi-Ru Dai 4,  Yue-Hong Leng 1,  Le-Le Ding 3,  Ling-Ling Jin 1,  Yang Yu 3,  Yun-Feng Cao 5,  Jie Hou 6
Affiliations

Affiliations

  • 1 Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China.
  • 2 Institute of Interdisciplinary Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China.
  • 3 Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China; Institute of Interdisciplinary Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
  • 4 Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China.
  • 5 Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China; Key Laboratory of Contraceptives and Devices Research (NPFPC), Shanghai Engineer and Technology Research Center of Reproductive Health Drug and Devices, Shanghai Institute of Planned Parenthood Research, Shanghai, China.
  • 6 Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China. Electronic address: houjie@dlmedu.edu.cn.
PMID: 30032067 DOI: 10.1016/j.bioorg.2018.07.011
Abstract

Pancreatic Lipase (PL), a key Enzyme responsible for the hydrolysis of triacylglycerides in the gastrointestinal tract, has been identified as the therapeutic target for the regulation of lipid absorption. In the present study, six major constituents from a famous Chinese herbal medicine Cortex Mori Radicis (also named sangbaipi in Chinese), have been collected and their inhibitory effects on PL have been carefully investigated and well characterized by a fluorescence-based assay. The results clearly demonstrated that all tested bioactive constituents from Cortex Mori Radicis including sanggenone C (SC), sanggenone D (SD), kuwanon C (KC), kuwanon G (KG), morin and morusin displayed strong to moderate inhibitory effects towards PL with the IC50 values ranging from 0.77 μM to 20.56 μM. Further investigations on inhibition kinetics demonstrated that SC, SD, KC and KG functioned as potent and mixed inhibitors against PL-mediated 4-MU oleate hydrolysis, with the Ki values less than 5.0 μM. Furthermore, molecular docking simulations demonstrated that SD (the most potent PL inhibitor from Cortex Mori Radicis) could create strong interaction with Ser152 (the key amino acid in the catalytic triad) of PL via hydrogen bonding. All these findings provided a new powerful evidence for explaining the hypolipidemic effect of Cortex Mori Radicis, also suggested that some abundant natural compounds in this herbal medicine could be served as lead compounds for the development of new PL inhibitors.

Keywords

Cortex Mori Radicis; Inhibitory effects; Pancreatic lipase; Sanggenone C; Sanggenone D.

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