دورية أكاديمية

Biflavones from Ginkgo biloba as novel pancreatic lipase inhibitors: Inhibition potentials and mechanism.

التفاصيل البيبلوغرافية
العنوان: Biflavones from Ginkgo biloba as novel pancreatic lipase inhibitors: Inhibition potentials and mechanism.
المؤلفون: Liu PK; Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, 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., Ge GB; Institute of Interdisciplinary Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China., Li HL; School of Pharmacy, Second Military Medical University, Guohe Road, Shanghai 200433, China., Ding LL; 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., Hou XD; Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China., Leng YH; Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China., Yu Y; Institute of Interdisciplinary Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China., Hou J; Department of Biotechnology, College of Basic Medical Sciences, Dalian Medical University, Dalian 116044, China. Electronic address: houjie@nankai.edu.cn.
المصدر: International journal of biological macromolecules [Int J Biol Macromol] 2018 Oct 15; Vol. 118 (Pt B), pp. 2216-2223. Date of Electronic Publication: 2018 Jul 21.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Elsevier Country of Publication: Netherlands NLM ID: 7909578 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1879-0003 (Electronic) Linking ISSN: 01418130 NLM ISO Abbreviation: Int J Biol Macromol Subsets: MEDLINE
أسماء مطبوعة: Publication: Amsterdam : Elsevier
Original Publication: Guildford, Eng., IPC Science and Technology Press.
مواضيع طبية MeSH: Biflavonoids/*pharmacology , Enzyme Inhibitors/*pharmacology , Ginkgo biloba/*chemistry , Lipase/*antagonists & inhibitors , Pancreas/*enzymology, Animals ; Biflavonoids/chemistry ; Enzyme Inhibitors/chemistry ; Inhibitory Concentration 50 ; Kinetics ; Lipase/metabolism ; Molecular Docking Simulation ; Sus scrofa ; Thermodynamics
مستخلص: Reduction of lipid absorption has been recognized as an attractive approach for the discovery of new drugs to treat obesity and overweight. The leave extract of Ginkgo biloba has been widely used for the treatment of metabolic diseases (such as hyperlipidemia) in both eastern and western countries, but the bioactive compounds in Ginkgo biloba and the underlying mechanism have not been fully characterized. This study aimed to investigate the inhibition potentials and mechanism of major biflavones from G. biloba on pancreatic lipase (PL), a key target regulating lipid absorption. The results clearly demonstrated that all tested biflavones in G. biloba including isoginkgetin, bilobetin, ginkgetin and sciadopitysin, displayed strong to moderate inhibitory effects on PL with the IC 50 values ranging from 2.90 μM to 12.78 μM. Further investigations on both inhibition kinetic analyses and docking simulations demonstrated that isoginkgetin, bilobetin and ginkgetin were potent PL inhibitors (K i  < 2.5 μM), which could create strong interactions with the catalytic triad of PL via hydrogen bonding. These findings provided a new powerful evidence for explaining the hypolipidemic effects of G. biloba, while these newly identified PL inhibitors from G. biloba could serve as lead compounds for the development of biflavonoid-type PL inhibitors.
(Copyright © 2018 Elsevier B.V. All rights reserved.)
فهرسة مساهمة: Keywords: Ginkgo biloba; Inhibitory effects; Pancreatic lipase
المشرفين على المادة: 0 (Biflavonoids)
0 (Enzyme Inhibitors)
EC 3.1.1.3 (Lipase)
تواريخ الأحداث: Date Created: 20180717 Date Completed: 20181231 Latest Revision: 20181231
رمز التحديث: 20240829
DOI: 10.1016/j.ijbiomac.2018.07.085
PMID: 30009906
قاعدة البيانات: MEDLINE
الوصف
تدمد:1879-0003
DOI:10.1016/j.ijbiomac.2018.07.085