A curcumin derivative, 2,6-bis(2,5-dimethoxybenzylidene)-cyclohexanone (BDMC33) attenuates prostaglandin E2 synthesis via selective suppression of cyclooxygenase-2 in IFN-γ/LPS-stimulated macrophages.

Molecules 2011 Nov 23;16(11):9728-38. Epub 2011 Nov 23.

Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia.

Our preliminary screening had shown that the curcumin derivative [2,6-bis(2,5-dimethoxybenzylidene)cyclohexanone] or BDMC33 exhibited improved anti-inflammatory activity by inhibiting nitric oxide synthesis in activated macrophage cells. In this study, we further investigated the anti-inflammatory properties of BDMC33 on PGE(2 )synthesis and cyclooxygenase (COX) expression in IFN-γ/LPS-stimulated macrophages. We found that BDMC33 significantly inhibited PGE(2) synthesis in a concentration-dependent manner albeit at a low inhibition level with an IC(50) value of 47.33 ± 1.00 µM. Interestingly, the PGE(2) inhibitory activity of BDMC33 is not attributed to inhibition of the COX enzyme activities, but rather BDMC33 selectively down-regulated the expression of COX-2. In addition, BDMC33 modulates the COX expression by sustaining the constitutively COX-1 expression in IFN-γ/LPS-treated macrophage cells. Collectively, the experimental data suggest an immunodulatory action of BDMC33 on PGE(2) synthesis and COX expression, making it a possible treatment for inflammatory disorders with minimal gastrointestinal-related side effects.

Download full-text PDF

Source
http://www.mdpi.com/1420-3049/16/11/9728
Publisher Site
http://dx.doi.org/10.3390/molecules16119728DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6264440PMC
November 2011

Publication Analysis

Top Keywords

cox expression
12
pge2 synthesis
12
macrophage cells
8
curcumin derivative
8
bdmc33 pge2
8
bdmc33
8
ifn-γ/lps-stimulated macrophages
8
expression
5
synthesis
5
albeit low
4
concentration-dependent manner
4
experimental data
4
manner albeit
4
collectively experimental
4
cells collectively
4
level ic50
4
inhibition level
4
synthesis concentration-dependent
4
low inhibition
4
expression ifn-γ/lps-stimulated
4

Similar Publications