Inflammation Research

, Volume 60, Issue 9, pp 851–859 | Cite as

Methyl-1-hydroxy-2-naphthoate, a novel naphthol derivative, inhibits lipopolysaccharide-induced inflammatory response in macrophages via suppression of NF-κB, JNK and p38 MAPK pathways

  • Jun-Yan Zhang
  • Hong Jin
  • Guang-Fa Wang
  • Peng-Jiu Yu
  • Shao-Yu Wu
  • Zheng-Guang Zhu
  • Zhong-Huang Li
  • Yuan-Xin Tian
  • Wei Xu
  • Jia-Jie Zhang
  • Shu-Guang Wu
Original Research Paper


Objective and design

The anti-inflammatory effect of methyl-1-hydroxy-2-naphthoate (MHNA), a novel naphthol derivative, was evaluated in the lipopolysaccharide (LPS)-induced inflammatory response in murine macrophages.

Materials and methods

The release of nitric oxide (NO), interleukin-1beta (IL-1β) and interleukin-6 (IL-6) were detected by the Griess reagent and ELISA methods. The protein expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) were examined by Western blotting. The mRNA expressions of IL-1β, IL-6, iNOS and COX-2 were determined by real-time PCR. Activation of mitogen-activated protein kinases (MAPKs) and nuclear factor kappa B (NF-κB) pathways were detected by Western blotting, reporter gene assay and electrophoretic mobility shift assay.


MHNA significantly inhibited the release of NO, IL-1β and IL-6 as well as the protein expression of iNOS and COX-2 in LPS-stimulated macrophages. It also inhibited the mRNA expression of iNOS, COX-2, IL-1β and IL-6. Further studies indicated that MHNA inhibited LPS-induced increases in NF-κB DNA-binding activity and NF-κB transcriptional activity as well as IκB-α degradation and NF-κB translocation in a dose-dependent manner. Meanwhile, the activation of p38 MAPK and c-Jun N-terminal kinases (JNK) induced by LPS were decreased by MHNA.


MHNA inhibits the LPS-induced inflammatory response in murine macrophages via suppression of NF-κB and MAPKs signaling pathways activation.


Methyl-1-hydroxy-2-naphthoate Naphthol NF-κB Macrophage Inflammatory mediators 





Electrophoretic mobility shift assay


Extracellular signal-regulated kinases


Inducible nitric oxide synthase


Inhibitory kappa B






c-Jun N-terminal kinases




Mitogen-activated protein kinases


Nitric oxide


Nuclear factor kappa B


Prostaglandin E2


Tumor necrosis factor alpha



This work was supported by grants from the Science and Technology Bureau of Guangzhou (2006Z1-E6021).


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Copyright information

© Springer Basel AG 2011

Authors and Affiliations

  • Jun-Yan Zhang
    • 1
  • Hong Jin
    • 1
  • Guang-Fa Wang
    • 1
  • Peng-Jiu Yu
    • 1
  • Shao-Yu Wu
    • 1
  • Zheng-Guang Zhu
    • 1
  • Zhong-Huang Li
    • 1
  • Yuan-Xin Tian
    • 1
  • Wei Xu
    • 1
  • Jia-Jie Zhang
    • 1
  • Shu-Guang Wu
    • 1
  1. 1.School of Pharmaceutical SciencesSouthern Medical UniversityGuangzhouChina

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