Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Synthetic chalcone derivatives inhibit cytokine secretion via inhibition of ERK and JNK pathways in human U937 macrophage

Lee Jian Sian, Malina Jasamai, Nor Syafinaz Yaakob, Norsyahida Mohd Fauzi

Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz 50300, Kuala Lumpur, Malaysia;

For correspondence:- Norsyahida Fauzi Email: drnorsyahida@ukm.edu.my

Accepted: 20 March 2019 Published: 30 April 2019

Citation: Sian LJ, Jasamai M, Yaakob NS, Fauzi NM. Synthetic chalcone derivatives inhibit cytokine secretion via inhibition of ERK and JNK pathways in human U937 macrophage. Trop J Pharm Res 2019; 18(4):753-759 doi: 10.4314/tjpr.v18i4.11

© 2019 The authors.
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Abstract

Purpose: To investigate the inhibitory effects of a chalcone derivative on lipopolysaccharide (LPS)-induced interleukin (IL)-6 and IL-8 secretions and on LPS-induced mitogen-activated protein kinases (MAPK) and nuclear factor kappa B (NF-κB) activation in human U937 macrophage-like cell line.

Methods: The effects of chalcone derivative on LPS-induced secretion of IL-6 and IL-8 in endothelial cells were determined by enzyme-linked immunosorbent assay while the effects of chalcone on the activation of MAPK and NF-kB pathway were determined by Western blotting.

Results: The results showed that 3-(5-methyl-furan-2-yl)-naphthalen-1-yl-propenone (compound 1) significantly inhibited the secretion of LPS-induced IL-6 and IL-8 in U937 macrophages. This compound also demonstrated significant suppression of c-Jun N-terminal kinases (JNK) and extracellular signal-regulated kinases (ERK) phosphorylation. However, the compound did not reverse the degradation of inhibitor kappa B alpha (IκBα) and did not inhibit the phosphorylation of NF-κB subunit and P-38 MAPK.

Conclusion: Compound 1 inhibits the secretion of cytokines via the inhibition of ERK and JNK pathways. These results suggest that chalcone derivative could act as an antiinflammatory agent by altering cytokine secretion and inflammatory pathways.

Keywords: Inflammation, Chalcone derivative, Cytokines, MAPK, NF-_4;B, Macrophage