4.7 Article

Discovery and evaluation of piperid-4-one-containing mono-carbonyl analogs of curcumin as anti-inflammatory agents

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 11, Pages 3058-3065

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.03.057

Keywords

Curcumin; Mono-carbonyl analogue of curcumin; IL-6; Anti-inflammation; Sepsis

Funding

  1. National Natural Science Funding of China [21272179, 81102310, 81272462]
  2. High-Level Innovative Talent Funding of Zhejiang Department of Health
  3. Project of Wenzhou Sci-Tech Bureau [Y20120061]
  4. Zhejiang Natural Science Funding [LY12H16003]
  5. Zhejiang Department of Health [2012KYA129]
  6. Zhejiang Zhejiang Key Group Project in Scientific Innovation [2010R50042]
  7. China Postdoctoral Science Foundation [20090461121, 201003591]

Ask authors/readers for more resources

We previously reported the design and discovery of three series of 5-carbon linker-containing mono-carbonyl analogs of curcumin (MCACs) as excellent anti-inflammatory agents. In continuation of our ongoing research, we designed and synthesized the fourth series of MCACs, whose central linker is a piperid-4-one. Their inhibitory effects against IL-6 production were evaluated in lipopolysaccharide (LPS)-stimulated macrophages. Among them, compounds F8, F29, F33, F35, and F36 exhibited the IC50 values under 5 mu M. The structure-activity relationship was discussed. Mechanistically, F35 and F36 dose-dependently prevented LPS-induced NF-kappa B and ERK activation. Finally, pretreatment with F35 and F36 significantly protected the C57B/L6 mice from LPS-induced septic death. Together, these data present a series of new analogs of curcumin as promising anti-inflammatory agents. (C) 2013 Elsevier Ltd. All rights reserved.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.7
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available