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Molecules 2011, 16(11), 9728-9738; doi:10.3390/molecules16119728
Article

A Curcumin Derivative, 2,6-Bis(2,5-dimethoxybenzylidene)-cyclohexanone (BDMC33) Attenuates Prostaglandin E2 Synthesis via Selective Suppression of Cyclooxygenase-2 in IFN-g/LPS-Stimulated Macrophages

1
,
2,3
,
4
,
2,5
,
2,4
 and
1,2,*
1 Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia 2 Institute of Biosciences, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia 3 Department of Food Science, Faculty of Food Science and Technology, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia 4 Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia 5 Department of Chemistry, Faculty of Sciences, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia
* Author to whom correspondence should be addressed.
Received: 26 September 2011 / Revised: 27 October 2011 / Accepted: 28 October 2011 / Published: 23 November 2011
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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 PGE2 synthesis and cyclooxygenase (COX) expression in IFN-g/LPS-stimulated macrophages. We found that BDMC33 significantly inhibited PGE2 synthesis in a concentration-dependent manner albeit at a low inhibition level with an IC50 value of 47.33 ± 1.00 µM. Interestingly, the PGE2 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-g/LPS-treated macrophage cells. Collectively, the experimental data suggest an immunodulatory action of BDMC33 on PGE2 synthesis and COX expression, making it a possible treatment for inflammatory disorders with minimal gastrointestinal-related side effects.
Keywords: anti-inflammatory; BDMC33; cyclooxygenase; PGE2; RAW264.7 anti-inflammatory; BDMC33; cyclooxygenase; PGE2; RAW264.7
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Lee, K.-H.; Abas, F.; Alitheen, N.B.M.; Shaari, K.; Lajis, N.H.; Ahmad, S. A Curcumin Derivative, 2,6-Bis(2,5-dimethoxybenzylidene)-cyclohexanone (BDMC33) Attenuates Prostaglandin E2 Synthesis via Selective Suppression of Cyclooxygenase-2 in IFN-g/LPS-Stimulated Macrophages. Molecules 2011, 16, 9728-9738.

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