Low-cytotoxic synthetic bromorutaecarpine exhibits anti-inflammation and activation of transient receptor potential vanilloid type 1 activities

Chi-Ming Lee, Jiun An Gu, Tin Gan Rau, Che Hsiung Yang, Wei Chi Yang, Shih Hao Huang, Feng Yen Lin, Chun Mao Lin, Sheng Tung Huang

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Rutaecarpine (RUT), the major bioactive ingredient isolated from the Chinese herb Evodia rutaecarpa, possesses a wide spectrum of biological activities, including anti-inflammation and preventing cardiovascular diseases. However, its high cytotoxicity hampers pharmaceutical development. We designed and synthesized a derivative of RUT, bromo-dimethoxyrutaecarpine (Br-RUT), which showed no cytotoxicity at 20 M. Br-RUT suppressed nitric oxide (NO) production and tumor necrosis factor-α release in concentration-dependent (020 M) manners in lipopolysaccharide (LPS)-treated RAW 264.7 macrophages; protein levels of inducible NO synthase (iNOS) and cyclooxygenase-2 induced by LPS were downregulated. Br-RUT inhibited cell migration and invasion of ovarian carcinoma A2780 cells with 048 h of treatment. Furthermore, Br-RUT enhanced the expression of transient receptor potential vanilloid type 1 and activated endothelial NOS in human aortic endothelial cells. These results suggest that the synthetic Br-RUT possesses very low cytotoxicity but retains its activities against inflammation and vasodilation that could be beneficial for cardiovascular disease therapeutics.

Original languageEnglish
Article number795095
JournalBioMed Research International
Volume2013
DOIs
Publication statusPublished - 2013

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Chemical activation
Inflammation
Cytotoxicity
Lipopolysaccharides
Evodia
Cardiovascular Diseases
Macrophages
Endothelial cells
Nitric Oxide Synthase Type II
Cyclooxygenase 2
Bioactivity
Vasodilation
Cell Movement
Nitric Oxide
Down-Regulation
Endothelial Cells
Tumor Necrosis Factor-alpha
bromorutaecarpine
vanilloid receptor subtype 1
Derivatives

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Immunology and Microbiology(all)

Cite this

Low-cytotoxic synthetic bromorutaecarpine exhibits anti-inflammation and activation of transient receptor potential vanilloid type 1 activities. / Lee, Chi-Ming; Gu, Jiun An; Rau, Tin Gan; Yang, Che Hsiung; Yang, Wei Chi; Huang, Shih Hao; Lin, Feng Yen; Lin, Chun Mao; Huang, Sheng Tung.

In: BioMed Research International, Vol. 2013, 795095, 2013.

Research output: Contribution to journalArticle

Lee, Chi-Ming ; Gu, Jiun An ; Rau, Tin Gan ; Yang, Che Hsiung ; Yang, Wei Chi ; Huang, Shih Hao ; Lin, Feng Yen ; Lin, Chun Mao ; Huang, Sheng Tung. / Low-cytotoxic synthetic bromorutaecarpine exhibits anti-inflammation and activation of transient receptor potential vanilloid type 1 activities. In: BioMed Research International. 2013 ; Vol. 2013.
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AU - Yang, Che Hsiung

AU - Yang, Wei Chi

AU - Huang, Shih Hao

AU - Lin, Feng Yen

AU - Lin, Chun Mao

AU - Huang, Sheng Tung

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