1-(2,3-Dibenzimidazol-2-ylpropyl)-2-methoxybenzene Is a Syk Inhibitor with Anti-Inflammatory Properties
Abstract
:1. Introduction
2. Results
2.1. DBMB Suppressed the Production of Pro-Inflammatory Mediators
2.2. DBMB Inhibited Inflammatory Responses at the Transcriptional Level
2.3. The NF-κB Signaling Cascade Was Modulated by DBMB
3. Discussion
4. Materials and Methods
4.1. Materials
4.2. Cell Culture
4.3. NO and PGE2 Production
4.4. Cell Viability Test
4.5. mRNA Analysis by Quantitative Real-Time PCR
4.6. Preparation of Total Lysates, Nuclear Extracts, and Immunoblotting
4.7. Transfection of DNA and Luciferase Reporter Gene Activity Assay
4.8. In Vitro Syk Kinase Assay Using Immunoprecipitated Proteins
4.9. Immunoprecipitation
4.10. Statistical Analysis
5. Conclusions
Acknowledgments
Author Contributions
Conflicts of Interest
Abbreviations
MTT | (3-4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide |
DBMB | 1-(2,3-dibenzimidazol-2-ylpropyl)-2-methoxybenzene |
COX-2 | cyclooxygenase-2 |
FBS | fetal bovine serum |
Indo | indomethacin |
iNOS | inducible nitric oxide synthase |
IKK | IκB kinase |
LPS | lipopolysaccharide |
PAMPs | pathogen-associated molecular patterns |
PBS | phosphate-buffered saline |
PRRs | pattern recognition receptors |
PI3K | phosphoinositide-3-kinase |
PDK1 | phosphoinositide-dependent kinase-1 |
Akt | protein kinase B |
PKC | protein kinase C |
TLRs | toll-like receptors |
TNF | tumor necrosis factor |
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- Sample Availability: Samples of the compound, 1-(2,3-dibenzimidazol-2-ylpropyl)-2-methoxybenzene, are available from the authors.
Name (Real-time PCR) | Sequence (5′ to 3′) | |
---|---|---|
iNOS | F | GGAGCCTTTAGACCTCAACAGA |
R | TGAACGAGGAGGGTGGTG | |
TNF-α | F | TGCCTATGTCTCAGCCTCTTC |
R | GAGGCCATTTGGGAACTTCT | |
COX-2 | F | GGGAGTCTGGAACATTGTGAA |
R | GCACATTGTAAGTAGGTGGACTGT | |
IFN-β | F | TCCAAGAAAGGACGAACATTCG |
R | GAGGCCATTTGGGAACTTCT | |
GAPDH | F | CAATGAATACGGCTACAGCAAC |
R | AGGGAGATGCTCAGTGTTGG |
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Kim, E.; Son, Y.-J.; Yang, Y.; Shen, T.; Kim, I.; Aravinthan, A.; Kim, J.-H.; Cho, J.Y. 1-(2,3-Dibenzimidazol-2-ylpropyl)-2-methoxybenzene Is a Syk Inhibitor with Anti-Inflammatory Properties. Molecules 2016, 21, 508. https://doi.org/10.3390/molecules21040508
Kim E, Son Y-J, Yang Y, Shen T, Kim I, Aravinthan A, Kim J-H, Cho JY. 1-(2,3-Dibenzimidazol-2-ylpropyl)-2-methoxybenzene Is a Syk Inhibitor with Anti-Inflammatory Properties. Molecules. 2016; 21(4):508. https://doi.org/10.3390/molecules21040508
Chicago/Turabian StyleKim, Eunji, Young-Jin Son, Yanyan Yang, Ting Shen, Ikyon Kim, Adithan Aravinthan, Jong-Hoon Kim, and Jae Youl Cho. 2016. "1-(2,3-Dibenzimidazol-2-ylpropyl)-2-methoxybenzene Is a Syk Inhibitor with Anti-Inflammatory Properties" Molecules 21, no. 4: 508. https://doi.org/10.3390/molecules21040508