4-Isopropyl-2,6-bis(1-phenylethyl)aniline 1, an Analogue of KTH-13 Isolated from Cordyceps bassiana, Inhibits the NF-κB-Mediated Inflammatory Response
Joint Authors
Yang, Woo Seok
Kim, Jong-Hoon
Lee, Yunmi
Ratan, Zubair Ahmed
Kim, Gihyeon
Kim, Mi-Yeon
Cho, Jae Youl
Source
Issue
Vol. 2015, Issue 2015 (31 Dec. 2015), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2015-12-27
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
The Cordyceps species has been a good source of compounds with anticancer and anti-inflammatory activities.
Recently, we reported a novel compound (4-isopropyl-2,6-bis(1-phenylethyl)phenol, KTH-13) with anticancer activity isolated from Cordyceps bassiana and created several derivatives to increase its pharmacological activity.
In this study, we tested one of the KTH-013 derivatives, 4-isopropyl-2,6-bis(1-phenylethyl)aniline 1 (KTH-13-AD1), with regard to anti-inflammatory activity under macrophage-mediated inflammatory conditions.
KTH-13-AD1 clearly suppressed the production of nitric oxide (NO) and reactive oxygen species (ROS) in lipopolysaccharide (LPS) and sodium nitroprusside- (SNP-) treated macrophage-like cells (RAW264.7 cells).
Similarly, this compound also reduced mRNA expression of inducible NO synthase (iNOS) and tumor necrosis factor-α (TNF-α), as analyzed by RT-PCR and real-time PCR.
Interestingly, KTH-13-AD1 strongly diminished NF-κB-mediated luciferase activities and nuclear translocation of NF-κB family proteins.
In accordance, KTH-13-AD1 suppressed the upstream signaling pathway of NF-κB activation, including IκBα, IKKα/β, AKT, p85/PI3K, and Src in a time- and dose-dependent manner.
The autophosphorylation of Src and NF-κB observed during the overexpression of Src was also suppressed by KTH-13-AD1.
These results strongly suggest that KTH-13-AD1 has strong anti-inflammatory features mediated by suppression of the Src/NF-κB regulatory loop.
American Psychological Association (APA)
Yang, Woo Seok& Ratan, Zubair Ahmed& Kim, Gihyeon& Lee, Yunmi& Kim, Mi-Yeon& Kim, Jong-Hoon…[et al.]. 2015. 4-Isopropyl-2,6-bis(1-phenylethyl)aniline 1, an Analogue of KTH-13 Isolated from Cordyceps bassiana, Inhibits the NF-κB-Mediated Inflammatory Response. Mediators of Inflammation،Vol. 2015, no. 2015, pp.1-10.
https://search.emarefa.net/detail/BIM-1072142
Modern Language Association (MLA)
Yang, Woo Seok…[et al.]. 4-Isopropyl-2,6-bis(1-phenylethyl)aniline 1, an Analogue of KTH-13 Isolated from Cordyceps bassiana, Inhibits the NF-κB-Mediated Inflammatory Response. Mediators of Inflammation No. 2015 (2015), pp.1-10.
https://search.emarefa.net/detail/BIM-1072142
American Medical Association (AMA)
Yang, Woo Seok& Ratan, Zubair Ahmed& Kim, Gihyeon& Lee, Yunmi& Kim, Mi-Yeon& Kim, Jong-Hoon…[et al.]. 4-Isopropyl-2,6-bis(1-phenylethyl)aniline 1, an Analogue of KTH-13 Isolated from Cordyceps bassiana, Inhibits the NF-κB-Mediated Inflammatory Response. Mediators of Inflammation. 2015. Vol. 2015, no. 2015, pp.1-10.
https://search.emarefa.net/detail/BIM-1072142
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1072142