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Abstract
Curcumin is a natural active product that has various pharmacological activities such as anti-inflammatory effects. Here, we report the synthesis and evaluation of 34 monocarbonyl curcumin analogs as novel anti-inflammatory agents. Among the analogs, the symmetrical heterocyclic type displayed the strongest inhibition of lipopolysaccharide (LPS)-stimulated expression of pro-inflammatory cytokines in macrophages. Analogs S1–S5 and AS29 reduced tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) production in a dose-dependent manner and also displayed excellent stability and low cytotoxicity in vitro. In addition, analog S1 dose-dependently inhibited LPS-induced extracellular signal-regulated kinase (ERK) phosphorylation. Furthermore, analogs S1 and S4 displayed a significant protective effect on LPS-induced septic death in mouse models, with 40% and 50% survival rates, respectively. These data demonstrate that the heterocyclic monocarbonyl curcumin analogs have potential therapeutic effects in acute inflammatory diseases.
Acknowledgments
Financial support was provided by the National Natural Science Fund of China (Grants 21272179, 81272462, and 81202462); Project of Zhejiang Provincial Key Constructive Subject (Traditional Chinese Medicine, Grant 2012-XK-A28); Qianjiang Talent Project of Zhejiang Province (Grant 2013R10020), and the Zhejiang Key Group Project in Scientific Innovation (Grant 2010R50042).
Disclosure
The authors report no conflicts of interest in this work.