دورية أكاديمية
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Natural constituents from Cortex Mori Radicis as new pancreatic lipase inhibitors.

التفاصيل البيبلوغرافية
العنوان: Natural constituents from Cortex Mori Radicis as new pancreatic lipase inhibitors.
المؤلفون: Hou XD; Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China., Ge GB; 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., Weng ZM; 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., Dai ZR; 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., Leng YH; Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China., Ding LL; 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., Jin LL; Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China., Yu Y; 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., Cao YF; 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., Hou J; Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China. Electronic address: houjie@dlmedu.edu.cn.
المصدر: Bioorganic chemistry [Bioorg Chem] 2018 Oct; Vol. 80, pp. 577-584. Date of Electronic Publication: 2018 Jul 17.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Elsevier Country of Publication: United States NLM ID: 1303703 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1090-2120 (Electronic) Linking ISSN: 00452068 NLM ISO Abbreviation: Bioorg Chem Subsets: MEDLINE
أسماء مطبوعة: Publication: Amsterdam : Elsevier
Original Publication: New York, London, Academic Press.
مواضيع طبية MeSH: Benzene Derivatives/*pharmacology , Benzofurans/*pharmacology , Chromones/*pharmacology , Drugs, Chinese Herbal/*pharmacology , Enzyme Inhibitors/*pharmacology , Flavonoids/*pharmacology , Lipase/*antagonists & inhibitors, Animals ; Benzene Derivatives/chemistry ; Benzofurans/chemistry ; Chromones/chemistry ; Drugs, Chinese Herbal/chemistry ; Enzyme Inhibitors/chemistry ; Flavonoids/chemistry ; Lipase/metabolism ; Molecular Docking Simulation ; Morus/chemistry ; Pancreas/enzymology ; Swine
مستخلص: 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 IC 50 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 K i 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.
(Copyright © 2018 Elsevier Inc. All rights reserved.)
فهرسة مساهمة: Keywords: Cortex Mori Radicis; Inhibitory effects; Pancreatic lipase; Sanggenone C; Sanggenone D
المشرفين على المادة: 0 (Benzene Derivatives)
0 (Benzofurans)
0 (Chromones)
0 (Drugs, Chinese Herbal)
0 (Enzyme Inhibitors)
0 (Flavonoids)
0 (Mulberrin)
0 (sanggenon D)
62596-29-6 (morusin)
75629-19-5 (kuwanon G)
80651-76-9 (sanggenone C)
8NFQ3F76WR (morin)
EC 3.1.1.3 (Lipase)
تواريخ الأحداث: Date Created: 20180723 Date Completed: 20190422 Latest Revision: 20190529
رمز التحديث: 20231215
DOI: 10.1016/j.bioorg.2018.07.011
PMID: 30032067
قاعدة البيانات: MEDLINE
الوصف
تدمد:1090-2120
DOI:10.1016/j.bioorg.2018.07.011