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BioMed Research International
Volume 2013, Article ID 795095, 8 pages
http://dx.doi.org/10.1155/2013/795095
Research Article

Low-Cytotoxic Synthetic Bromorutaecarpine Exhibits Anti-Inflammation and Activation of Transient Receptor Potential Vanilloid Type 1 Activities

1Graduate Institute of Medical Sciences, College of Medicine, Taipei Medical University, No. 250, Wu-xing Street, Taipei 110, Taiwan
2Institute of Chemical Engineering, College of Engineering, National Taipei University of Technology, Taipei, Taiwan
3Department of Food and Beverage Management, Taipei College of Maritime Technology, Taipei, Taiwan
4Department of Internal Medicine, School of Medicine, Taipei Medical University, No. 250, Wu-xing Street, Taipei 110, Taiwan
5Department of Biochemistry, College of Medicine, Taipei Medical University, No. 250, Wu-xing Street, Taipei 110, Taiwan
6Orthopedics Research Center, Taipei Medical University Hospital, Taipei, Taiwan
7Institute of Biochemical and Biomedical Engineering, College of Engineering, National Taipei University of Technology, Taipei, Taiwan

Received 12 September 2013; Accepted 29 October 2013

Academic Editor: Joen-Rong Sheu

Copyright © 2013 Chi-Ming Lee et al. 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.

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 μM. Br-RUT suppressed nitric oxide (NO) production and tumor necrosis factor-α release in concentration-dependent (0~20 μM) 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 0~48 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.