Synthesis of mono-carbonyl analogues of curcumin and their effects on inhibition of cytokine release in LPS-stimulated RAW 264.7 macrophages
- PMID: 20338767
- DOI: 10.1016/j.bmc.2010.03.001
Synthesis of mono-carbonyl analogues of curcumin and their effects on inhibition of cytokine release in LPS-stimulated RAW 264.7 macrophages
Abstract
Curcumin has been reported to possess multifunctional bioactivities, especially the ability to inhibit proinflammatory induction. We previously demonstrated that the mono-carbonyl analogues of curcumin possessed improved pharmacokinetic profiles both in vitro and in vivo. In this study, we synthesized and examined a series of 5-carbon linker-containing mono-carbonyl analogues of curcumin with potent inhibitory activities against TNF-alpha and IL-6 release in LPS-stimulated RAW 264.7 macrophages. Discussion and conclusions are given regarding structure-activity relationships (SAR). The two most potent analogues among the tested compounds, B75 and C12, exhibited anti-inflammatory abilities in a dose-dependent manner in macrophages. This raises the possibility that mono-carbonyl analogues of curcumin might serve as potential agents for the treatment of various inflammatory diseases.
Copyright 2010 Elsevier Ltd. All rights reserved.
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