Next Article in Journal
Study on the Rationality for Antiviral Activity of Flos Lonicerae Japonicae-Fructus Forsythiae Herb Couple Preparations Improved by Chito-Oligosaccharide via Integral Pharmacokinetics
Previous Article in Journal
Protein Stability and Unfolding Following Glycine Radical Formation
Article Menu
Issue 4 (April) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(4), 656; doi:10.3390/molecules22040656

Synthetic Fluororutaecarpine Inhibits Inflammatory Stimuli and Activates Endothelial Transient Receptor Potential Vanilloid-Type 1

1
Graduate Institute of Medical Sciences, College of Medicine, Taipei Medical University, Taipei 11031, Taiwan
2
Institute of Chemical Engineering, College of Engineering, National Taipei University of Technology, Taipei 10608, Taiwan
3
Department of Food and Beverage Management, Taipei College of Maritime Technology, Taipei 11174, Taiwan
4
Department of Internal Medicine, School of Medicine, College of Medicine, Taipei Medical University, Taipei 11031, Taiwan
5
Department of Biochemistry, School of Medicine, College of Medicine, Taipei Medical University, Taipei 11031, Taiwan
6
Institute of Biochemical and Biomedical Engineering, College of Engineering, National Taipei University of Technology, Taipei 10608, Taiwan
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 24 March 2017 / Revised: 14 April 2017 / Accepted: 18 April 2017 / Published: 19 April 2017
View Full-Text   |   Download PDF [5249 KB, uploaded 24 April 2017]   |  

Abstract

The natural product, rutaecarpine (RUT), is the main effective component of Evodia rutaecarpa which is a widely used traditional Chinese medicine. It has vasodilation, anticoagulation, and anti-inflammatory activities. However, further therapeutic applications are limited by its cytotoxicity. Thus, a derivative of RUT, 10-fluoro-2-methoxyrutaecarpine (F-RUT), was designed and synthesized that showed no cytotoxicity toward RAW264.7 macrophages at 20 μM. In an anti-inflammation experiment, it inhibited the production of nitric oxide (NO) and tumor necrosis factor (TNF)-α in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages; cyclooxygenase (COX)-2 and inducible NO synthase (iNOS) induced by LPS were also downregulated. After 24 h of treatment, F-RUT significantly inhibited cell migration and invasion of ovarian A2780 cells. Furthermore, F-RUT promoted expressions of transient receptor potential vanilloid type 1 (TRPV1) and endothelial (e)NOS in human aortic endothelial cells, and predominantly reduced the inflammation in ovalbumin/alum-challenged mice. These results suggest that the novel synthetic F-RUT exerts activities against inflammation and vasodilation, while displaying less toxicity than its lead compound. View Full-Text
Keywords: inflammation; fluoro-rutaecarpine; iNOS; TRPV-1; eNOS inflammation; fluoro-rutaecarpine; iNOS; TRPV-1; eNOS
Figures

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Supplementary material

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Lee, C.-M.; Gu, J.-A.; Rau, T.-G.; Wang, C.; Yen, C.-H.; Huang, S.-H.; Lin, F.-Y.; Lin, C.-M.; Huang, S.-T. Synthetic Fluororutaecarpine Inhibits Inflammatory Stimuli and Activates Endothelial Transient Receptor Potential Vanilloid-Type 1. Molecules 2017, 22, 656.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top