A Novel Naturally Occurring Salicylic Acid Analogue Acts as an Anti-Inflammatory Agent by Inhibiting Nuclear Factor-kappaB Activity in RAW264.7 Macrophages

2012 ◽  
Vol 9 (3) ◽  
pp. 671-677 ◽  
Author(s):  
Tiantai Zhang ◽  
Lan Sun ◽  
Rui Liu ◽  
Dan Zhang ◽  
Xi Lan ◽  
...  
1957 ◽  
Vol 79 (20) ◽  
pp. 5577-5578 ◽  
Author(s):  
F. A. Kuehl ◽  
T. A. Jacob ◽  
O. H. Ganley ◽  
R. E. Ormond ◽  
M. A. P. Meisinger

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4424
Author(s):  
Jin Kyu Kang ◽  
Chang-Gu Hyun

Coumarins are natural products with promising pharmacological activities owing to their anti-inflammatory, antioxidant, antiviral, anti-diabetic, and antimicrobial effects. Coumarins are present in many plants and microorganisms and have been widely used as complementary and alternative medicines. To date, the pharmacological efficacy of 4-hydroxy-7-methoxycoumarin (4H-7MTC) has not been reported yet. Therefore, in this study, we investigated the anti-inflammatory effects of 4H-7MTC in LPS-stimulated RAW264.7 cells as well as its mechanisms of action. Cells were treated with various concentrations of 4H-7MTC (0.3, 0.6, 0.9, and 1.2 mM) and 40 μM L-N6-(1-iminoethyl)-L-lysine (L-NIL) were used as controls. LPS-stimulated RAW264.7 cells showed that 4H-7MTC significantly reduced nitric oxide (NO) and prostaglandin E2 (PGE2) production without cytotoxic effects. In addition, 4H-7MTC strongly decreased the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX-2). Furthermore, 4H-7MTC reduced the production of proinflammatory cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6. We also found that 4H-7MTC strongly exerted its anti-inflammatory actions by downregulating nuclear factor kappa B (NF-κB) activation by suppressing inhibitor of nuclear factor kappa B alpha (IκBα) degradation in macrophages. Moreover, 4H-7MTC decreased phosphorylation of extracellular signal-regulated kinase (ERK1/2) and c-Jun N-terminal kinase/stress-activated protein kinase (JNK), but not that of p38 MAPK. These results suggest that 4H-7MTC may be a good candidate for the treatment or prevention of inflammatory diseases such as dermatitis, psoriasis, and arthritis. Ultimately, this is the first report describing the effective anti-inflammatory activity of 4H-7MTC.


Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3232 ◽  
Author(s):  
Ning Li ◽  
Shabana Khan ◽  
Shi Qiu ◽  
Xing-Cong Li

The natural product phloroglucinol-based derivatives representing monoacyl-, diacyl-, dimeric acyl-, alkylated monoacyl-, and the nitrogen-containing alkylated monoacylphloro- glucinols were synthesized and evaluated for inhibitory activities against the inflammatory mediators such as inducible nitric oxide synthase (iNOS) and nuclear factor kappaB (NF-κB). The diacylphloroglucinol compound 2 and the alkylated acylphloroglucinol compound 4 inhibited iNOS with IC50 values of 19.0 and 19.5 µM, respectively, and NF-κB with IC50 values of 34.0 and 37.5 µM, respectively. These compounds may serve as leads for the synthesis of more potent anti-inflammatory compounds for future drug discovery.


2013 ◽  
Vol 550 ◽  
pp. 162-167 ◽  
Author(s):  
Jin-A. Shin ◽  
Ji-Sun Hwang ◽  
Song-Yi Kim ◽  
Sei-Kwan Oh ◽  
Ghilsoo Nam ◽  
...  

2014 ◽  
Vol 127 ◽  
pp. 290-298 ◽  
Author(s):  
Sherry L. Spinelli ◽  
Xia Xi ◽  
David H. McMillan ◽  
Collynn F. Woeller ◽  
Mary E. Richardson ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document