The Anti-Inflammatory Activity of a Novel Fused-Cyclopentenone Phosphonate and Its Potential in the Local Treatment of Experimental Colitis
Joint Authors
Moradov, Dorit
Shifrin, Helena
Harel, Efrat
Nadler-Milbauer, Mirela
Weinstock, Marta
Srebnik, Morris
Rubinstein, Abraham
Source
Gastroenterology Research and Practice
Issue
Vol. 2015, Issue 2015 (31 Dec. 2015), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2015-04-09
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
A novel fused-cyclopentenone phosphonate compound, namely, diethyl 3-nonyl-5-oxo-3,5,6,6a-tetrahydro-1H-cyclopenta[c]furan-4-ylphosphonate (P-5), was prepared and tested in vitro (LPS-activated macrophages) for its cytotoxicity and anti-inflammatory activity and in vivo (DNBS induced rat model) for its potential to ameliorate induced colitis.
Specifically, the competence of P-5 to reduce TNFα, IL-6, INFγ, MCP-1, IL-1α, MIP-1α, and RANTES in LPS-activated macrophages was measured.
Experimental colitis was quantified in the rat model, macroscopically and by measuring the activity of tissue MPO and iNOS and levels of TNFα and IL-1β.
It was found that P-5 decreased the levels of TNFα and the tested proinflammatory cytokines and chemokines in LPS-activated macrophages.
In the colitis-induced rat model, P-5 was effective locally in reducing mucosal inflammation.
This activity was equal to the activity of local treatment with 5-aminosalicylic acid.
It is speculated that P-5 may be used for the local treatment of IBD (e.g., with the aid of colon-specific drug platforms).
Its mode of action involves inhibition of the phosphorylation of MAPK ERK but not of p38 and had no effect on IκBα.
American Psychological Association (APA)
Moradov, Dorit& Shifrin, Helena& Harel, Efrat& Nadler-Milbauer, Mirela& Weinstock, Marta& Srebnik, Morris…[et al.]. 2015. The Anti-Inflammatory Activity of a Novel Fused-Cyclopentenone Phosphonate and Its Potential in the Local Treatment of Experimental Colitis. Gastroenterology Research and Practice،Vol. 2015, no. 2015, pp.1-10.
https://search.emarefa.net/detail/BIM-1064352
Modern Language Association (MLA)
Moradov, Dorit…[et al.]. The Anti-Inflammatory Activity of a Novel Fused-Cyclopentenone Phosphonate and Its Potential in the Local Treatment of Experimental Colitis. Gastroenterology Research and Practice No. 2015 (2015), pp.1-10.
https://search.emarefa.net/detail/BIM-1064352
American Medical Association (AMA)
Moradov, Dorit& Shifrin, Helena& Harel, Efrat& Nadler-Milbauer, Mirela& Weinstock, Marta& Srebnik, Morris…[et al.]. The Anti-Inflammatory Activity of a Novel Fused-Cyclopentenone Phosphonate and Its Potential in the Local Treatment of Experimental Colitis. Gastroenterology Research and Practice. 2015. Vol. 2015, no. 2015, pp.1-10.
https://search.emarefa.net/detail/BIM-1064352
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1064352