Cardamonin, inhibits pro-inflammatory mediators in activated RAW 264.7 cells and whole blood

Syahida Ahmad, Daud A. Israf, Nordin Hj Lajis, Khozirah Shaari, Habsah Mohamed, Afiza A. Wahab, Khaizurin Ajul Arifin, Wei Yee Hoo, Nasaruddin A. Aziz, Arifah A. Kadir, Mohamad R. Sulaiman, Muhammad N. Somchit

Research output: Contribution to journalArticle

73 Citations (Scopus)

Abstract

Some chalcones, such as hydroxychalcones have been reported previously to inhibit major pro-inflammatory mediators such as nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-α (TNF-α) and reactive oxygen species production by suppressing inducible enzyme expression via inhibition of the mitogen-activated protein kinase (MAPK) pathway and nuclear translocation of critical transcription factors. In this report, the effects of cardamonin (2′,4′-dihydroxy-6′-methoxychalcone), a chalcone that we have previously isolated from Alpinia rafflesiana, was evaluated upon two cellular systems that are repeatedly used in the analysis of anti-inflammatory bioactive compounds namely RAW 264.7 cells and whole blood. Cardamonin inhibited NO and PGE2 production from lipopolysaccharide- and interferon-γ-induced RAW cells and whole blood with IC50 values of 11.4 μM and 26.8 μM, respectively. Analysis of thromboxane B2 (TxB2) secretion from whole blood either stimulated via the COX-1 or COX-2 pathway revealed that cardamonin inhibits the generation of TxB2 via both pathways with IC50 values of 2.9 and 1.1 μM, respectively. Analysis of IC50 ratios determined that cardamonin was more COX-2 selective in its inhibition of TxB2 with a ratio of 0.39. Cardamonin also inhibited the generation of intracellular reactive oxygen species and secretion of TNF-α from RAW 264.7 cells in a dose responsive manner with IC50 values of 12.8 μM and 4.6 μM, respectively. However, cardamonin was a moderate inhibitor of lipoxygenase activity when tested in an enzymatic assay system, in which not a single concentration tested was able to cause an inhibition of more than 50%. Our results suggest that cardamonin acts upon major pro-inflammatory mediators in a similar fashion as described by previous work on other closely related synthetic hydroxychalcones and strengthens the conclusion of the importance of the methoxyl moiety substitution on the 4′ or 6′ locations of the A benzene ring.

Original languageEnglish
Pages (from-to)188-194
Number of pages7
JournalEuropean Journal of Pharmacology
Volume538
Issue number1-3
DOIs
Publication statusPublished - 24 May 2006
Externally publishedYes

Fingerprint

Thromboxane B2
Inhibitory Concentration 50
Dinoprostone
Reactive Oxygen Species
Nitric Oxide
Tumor Necrosis Factor-alpha
Alpinia
Chalcones
Chalcone
Lipoxygenase Inhibitors
Enzyme Assays
cardamonin
RAW 264.7 Cells
Benzene
Mitogen-Activated Protein Kinases
Interferons
Lipopolysaccharides
Blood Cells
Anti-Inflammatory Agents
Transcription Factors

Keywords

  • Alpinia rafflesiana
  • Cardamonin
  • Inflammatory mediator
  • RAW 264.7
  • Whole blood

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Ahmad, S., Israf, D. A., Lajis, N. H., Shaari, K., Mohamed, H., Wahab, A. A., ... Somchit, M. N. (2006). Cardamonin, inhibits pro-inflammatory mediators in activated RAW 264.7 cells and whole blood. European Journal of Pharmacology, 538(1-3), 188-194. https://doi.org/10.1016/j.ejphar.2006.03.070

Cardamonin, inhibits pro-inflammatory mediators in activated RAW 264.7 cells and whole blood. / Ahmad, Syahida; Israf, Daud A.; Lajis, Nordin Hj; Shaari, Khozirah; Mohamed, Habsah; Wahab, Afiza A.; Ajul Arifin, Khaizurin; Hoo, Wei Yee; Aziz, Nasaruddin A.; Kadir, Arifah A.; Sulaiman, Mohamad R.; Somchit, Muhammad N.

In: European Journal of Pharmacology, Vol. 538, No. 1-3, 24.05.2006, p. 188-194.

Research output: Contribution to journalArticle

Ahmad, S, Israf, DA, Lajis, NH, Shaari, K, Mohamed, H, Wahab, AA, Ajul Arifin, K, Hoo, WY, Aziz, NA, Kadir, AA, Sulaiman, MR & Somchit, MN 2006, 'Cardamonin, inhibits pro-inflammatory mediators in activated RAW 264.7 cells and whole blood', European Journal of Pharmacology, vol. 538, no. 1-3, pp. 188-194. https://doi.org/10.1016/j.ejphar.2006.03.070
Ahmad, Syahida ; Israf, Daud A. ; Lajis, Nordin Hj ; Shaari, Khozirah ; Mohamed, Habsah ; Wahab, Afiza A. ; Ajul Arifin, Khaizurin ; Hoo, Wei Yee ; Aziz, Nasaruddin A. ; Kadir, Arifah A. ; Sulaiman, Mohamad R. ; Somchit, Muhammad N. / Cardamonin, inhibits pro-inflammatory mediators in activated RAW 264.7 cells and whole blood. In: European Journal of Pharmacology. 2006 ; Vol. 538, No. 1-3. pp. 188-194.
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