ATP-Binding Pocket-Targeted Suppression of Src and Syk by Luteolin Contributes to Its Anti-Inflammatory Action
Joint Authors
Jeong, Deok
Lee, Jeong-Oog
Kim, Mi-Yeon
Cho, Jae Youl
Source
Issue
Vol. 2015, Issue 2015 (31 Dec. 2015), pp.1-12, 12 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2015-07-05
Country of Publication
Egypt
No. of Pages
12
Main Subjects
Abstract EN
Luteolin is a flavonoid identified as a major anti-inflammatory component of Artemisia asiatica.
Numerous reports have demonstrated the ability of luteolin to suppress inflammation in a variety of inflammatory conditions.
However, its exact anti-inflammatory mechanism has not been fully elucidated.
In the present study, the anti-inflammatory mode of action in activated macrophages of luteolin from Artemisia asiatica was examined by employing immunoblotting analysis, a luciferase reporter gene assay, enzyme assays, and an overexpression strategy.
Luteolin dose-dependently inhibited the secretion of nitric oxide (NO) and prostaglandin E2 (PGE2) and diminished the levels of mRNA transcripts of inducible NO synthase (iNOS), tumor necrosis factor- (TNF-) α, and cyclooxygenase-2 (COX-2) in lipopolysaccharide- (LPS-) and pam3CSK-treated macrophage-like RAW264.7 cells without displaying cytotoxicity.
Luteolin displayed potent NO-inhibitory activity and also suppressed the nuclear translocation of NF-κB (p65 and p50) via blockade of Src and Syk, but not other mitogen-activated kinases.
Overexpression of wild type Src and point mutants thereof, and molecular modelling studies, suggest that the ATP-binding pocket may be the luteolin-binding site in Src.
These results strongly suggest that luteolin may exert its anti-inflammatory action by suppressing the NF-κB signaling cascade via blockade of ATP binding in Src and Syk.
American Psychological Association (APA)
Lee, Jeong-Oog& Jeong, Deok& Kim, Mi-Yeon& Cho, Jae Youl. 2015. ATP-Binding Pocket-Targeted Suppression of Src and Syk by Luteolin Contributes to Its Anti-Inflammatory Action. Mediators of Inflammation،Vol. 2015, no. 2015, pp.1-12.
https://search.emarefa.net/detail/BIM-1072668
Modern Language Association (MLA)
Lee, Jeong-Oog…[et al.]. ATP-Binding Pocket-Targeted Suppression of Src and Syk by Luteolin Contributes to Its Anti-Inflammatory Action. Mediators of Inflammation No. 2015 (2015), pp.1-12.
https://search.emarefa.net/detail/BIM-1072668
American Medical Association (AMA)
Lee, Jeong-Oog& Jeong, Deok& Kim, Mi-Yeon& Cho, Jae Youl. ATP-Binding Pocket-Targeted Suppression of Src and Syk by Luteolin Contributes to Its Anti-Inflammatory Action. Mediators of Inflammation. 2015. Vol. 2015, no. 2015, pp.1-12.
https://search.emarefa.net/detail/BIM-1072668
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1072668