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Low-Cytotoxic Synthetic Bromorutaecarpine Exhibits Anti-Inflammation and Activation of Transient Receptor Potential Vanilloid Type 1 Activities
Joint Authors
Lin, Feng-Yen
Lin, Chun-Mao
Lee, Chi-Ming
Gu, Jiun-An
Rau, Tin-Gan
Yang, Che-Hsiung
Yang, Wei-Chi
Huang, Shih-Hao
Huang, Sheng-Tung
Source
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-11-28
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
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.
American Psychological Association (APA)
Lee, Chi-Ming& Gu, Jiun-An& Rau, Tin-Gan& Yang, Che-Hsiung& Yang, Wei-Chi& Huang, Shih-Hao…[et al.]. 2013. Low-Cytotoxic Synthetic Bromorutaecarpine Exhibits Anti-Inflammation and Activation of Transient Receptor Potential Vanilloid Type 1 Activities. BioMed Research International،Vol. 2013, no. 2013, pp.1-8.
https://search.emarefa.net/detail/BIM-1030925
Modern Language Association (MLA)
Lee, Chi-Ming…[et al.]. Low-Cytotoxic Synthetic Bromorutaecarpine Exhibits Anti-Inflammation and Activation of Transient Receptor Potential Vanilloid Type 1 Activities. BioMed Research International No. 2013 (2013), pp.1-8.
https://search.emarefa.net/detail/BIM-1030925
American Medical Association (AMA)
Lee, Chi-Ming& Gu, Jiun-An& Rau, Tin-Gan& Yang, Che-Hsiung& Yang, Wei-Chi& Huang, Shih-Hao…[et al.]. Low-Cytotoxic Synthetic Bromorutaecarpine Exhibits Anti-Inflammation and Activation of Transient Receptor Potential Vanilloid Type 1 Activities. BioMed Research International. 2013. Vol. 2013, no. 2013, pp.1-8.
https://search.emarefa.net/detail/BIM-1030925
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1030925