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Magnolia officinalis Extract Contains Potent Inhibitors against PTP1B and Attenuates Hyperglycemia in dbdb Mice
Joint Authors
Sun, Jing
Wang, Yongsen
Fu, Xueqi
Chen, Yingli
Wang, Deli
Li, Wannan
Xing, Shu
Li, Guodong
Source
Issue
Vol. 2015, Issue 2015 (31 Dec. 2015), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2015-05-07
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
Protein tyrosine phosphatase 1B (PTP1B) is an established therapeutic target for type 2 diabetes mellitus (T2DM) and obesity.
The aim of this study was to investigate the inhibitory activity of Magnolia officinalis extract (ME) on PTP1B and its anti-T2DM effects.
Inhibition assays and inhibition kinetics of ME were performed in vitro.
3T3-L1 adipocytes and C2C12 myotubes were stimulated with ME to explore its bioavailability in cell level.
The in vivo studies were performed on db/db mice to probe its anti-T2DM effects.
In the present study, ME inhibited PTP1B in a reversible competitive manner and displayed good selectivity against PTPs in vitro.
Furthermore, ME enhanced tyrosine phosphorylation levels of cellular proteins, especially the insulin-induced tyrosine phosphorylations of insulin receptor β-subunit (IRβ) and ERK1/2 in a dose-dependent manner in stimulated 3T3-L1 adipocytes and C2C12 myotubes.
Meanwhile, ME enhanced insulin-stimulated GLUT4 translocation.
More importantly, there was a significant decrease in fasting plasma glucose level of db/db diabetic mice treated orally with 0.5 g/kg ME for 4 weeks.
These findings indicated that improvement of insulin sensitivity and hypoglycemic effects of ME may be attributed to the inhibition of PTP1B.
Thereby, we pioneered the inhibitory potential of ME targeted on PTP1B as anti-T2DM drug discovery.
American Psychological Association (APA)
Sun, Jing& Wang, Yongsen& Fu, Xueqi& Chen, Yingli& Wang, Deli& Li, Wannan…[et al.]. 2015. Magnolia officinalis Extract Contains Potent Inhibitors against PTP1B and Attenuates Hyperglycemia in dbdb Mice. BioMed Research International،Vol. 2015, no. 2015, pp.1-10.
https://search.emarefa.net/detail/BIM-1054336
Modern Language Association (MLA)
Sun, Jing…[et al.]. Magnolia officinalis Extract Contains Potent Inhibitors against PTP1B and Attenuates Hyperglycemia in dbdb Mice. BioMed Research International No. 2015 (2015), pp.1-10.
https://search.emarefa.net/detail/BIM-1054336
American Medical Association (AMA)
Sun, Jing& Wang, Yongsen& Fu, Xueqi& Chen, Yingli& Wang, Deli& Li, Wannan…[et al.]. Magnolia officinalis Extract Contains Potent Inhibitors against PTP1B and Attenuates Hyperglycemia in dbdb Mice. BioMed Research International. 2015. Vol. 2015, no. 2015, pp.1-10.
https://search.emarefa.net/detail/BIM-1054336
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1054336