In vitro and in vivo anti-inflammatory activities of Polygonum hydropiper methanol extract

Yanyan Yang, Tao Yu, Hyun Jae Jang, Se Eun Byeon, Song Yi Song, Byoung Hee Lee, Man Hee Rhee, Tae Woong Kim, Jaehwi Lee, Sungyoul Hong, Jae Youl Cho

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82 Scopus citations

Abstract

Ethnopharmacological relevance: Polygonum hydropiper L. (Polygonaceae) has been traditionally used to treat various inflammatory diseases such as rheumatoid arthritis. However, no systematic studies on the anti-inflammatory actions of Polygonum hydropiper and its inhibitory mechanisms have been reported. This study is therefore aimed at exploring the anti-inflammatory effects of 99% methanol extracts (Ph-ME) of this plant. Materials and methods: The effects of Ph-ME on the production of inflammatory mediators in RAW264.7 cells and peritoneal macrophages were investigated. Molecular mechanisms underlying the effects, especially inhibitory effects, were elucidated by analyzing the activation of transcription factors and their upstream signalling, and by evaluating the kinase activities of target enzymes. Additionally, a dextran sulphate sodium (DSS)-induced colitis model was employed to see whether this extract can be used as an orally available drug. Results: Ph-ME dose-dependently suppressed the release of nitric oxide (NO), tumour necrosis factor (TNF)-α, and prostaglandin (PG)E 2, in RAW264.7 cells and peritoneal macrophages stimulated by lipopolysaccharide (LPS). Ph-ME inhibited mRNA expression of pro-inflammatory genes such as inducible NO synthase (iNOS), cyclooxygenase (COX)-2, and TNF-α by suppressing the activation of nuclear factor (NF)-κB, activator protein (AP-1), and cAMP responsive element binding protein (CREB), and simultaneously inhibited its upstream inflammatory signalling cascades, including cascades involving Syk, Src, and IRAK1. Consistent with these findings, the extract strongly suppressed the kinase activities of Src and Syk. Based on HPLC analysis, quercetin, which inhibits NO and PGE 2 activities, was found as one of the active ingredients in Ph-ME. Conclusion: Ph-ME exerts strong anti-inflammatory activity by suppressing Src/Syk/NF-κB and IRAK/AP-1/CREB pathways, which contribute to its major ethno-pharmacological role as an anti-gastritis remedy.

Original languageEnglish
Pages (from-to)616-625
Number of pages10
JournalJournal of Ethnopharmacology
Volume139
Issue number2
DOIs
StatePublished - 31 Jan 2012

Keywords

  • Anti-inflammatory effects
  • Nitric oxide
  • Polygonaceae
  • Polygonum hydropiper L.
  • Prostaglandin E
  • Tumour necrosis factor-α

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