New Hydroxycinnamic Acid Esters as Novel 5-Lipoxygenase Inhibitors That Affect Leukotriene Biosynthesis
Joint Authors
Touaibia, Mohamed
Blanchard, Sébastien
Cormier, Marc
Lassalle-Claux, Grégoire
Doucet, Marco S.
Boudreau, Luc H.
Surette, Marc E.
Source
Issue
Vol. 2017, Issue 2017 (31 Dec. 2017), pp.1-12, 12 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2017-06-07
Country of Publication
Egypt
No. of Pages
12
Main Subjects
Abstract EN
Leukotrienes are inflammatory mediators that actively participate in the inflammatory response and host defense against pathogens.
However, leukotrienes also participate in chronic inflammatory diseases.
5-lipoxygenase is a key enzyme in the biosynthesis of leukotrienes and is thus a validated therapeutic target.
As of today, zileuton remains the only clinically approved 5-lipoxygenase inhibitor; however, its use has been limited due to severe side effects in some patients.
Hence, the search for a better 5-lipoxygenase inhibitor continues.
In this study, we investigated structural analogues of caffeic acid phenethyl ester, a naturally-occurring 5-lipoxygenase inhibitor, in an attempt to enhance the inhibitory activity against 5-lipoxygenase and determine structure-activity relationships.
These compounds were investigated for their ability to attenuate the biosynthesis of leukotrienes.
Compounds 13 and 19, phenpropyl and diphenylethyl esters, exhibited significantly enhanced inhibitory activity when compared to the reference molecules caffeic acid phenethyl ester and zileuton.
American Psychological Association (APA)
Boudreau, Luc H.& Lassalle-Claux, Grégoire& Cormier, Marc& Blanchard, Sébastien& Doucet, Marco S.& Surette, Marc E.…[et al.]. 2017. New Hydroxycinnamic Acid Esters as Novel 5-Lipoxygenase Inhibitors That Affect Leukotriene Biosynthesis. Mediators of Inflammation،Vol. 2017, no. 2017, pp.1-12.
https://search.emarefa.net/detail/BIM-1188624
Modern Language Association (MLA)
Boudreau, Luc H.…[et al.]. New Hydroxycinnamic Acid Esters as Novel 5-Lipoxygenase Inhibitors That Affect Leukotriene Biosynthesis. Mediators of Inflammation No. 2017 (2017), pp.1-12.
https://search.emarefa.net/detail/BIM-1188624
American Medical Association (AMA)
Boudreau, Luc H.& Lassalle-Claux, Grégoire& Cormier, Marc& Blanchard, Sébastien& Doucet, Marco S.& Surette, Marc E.…[et al.]. New Hydroxycinnamic Acid Esters as Novel 5-Lipoxygenase Inhibitors That Affect Leukotriene Biosynthesis. Mediators of Inflammation. 2017. Vol. 2017, no. 2017, pp.1-12.
https://search.emarefa.net/detail/BIM-1188624
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1188624