Flavocoxid Inhibits Phospholipase A2, Peroxidase Moieties of the Cyclooxygenases (COX), and 5-Lipoxygenase, Modifies COX-2 Gene Expression, and Acts as an Antioxidant
Joint Authors
Bitto, Alessandra
Levy, Robert M.
Squadrito, Francesco
Burnett, Bruce P.
Pillai, Lakshmi
Altavilla, Domenica
Source
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2011-06-19
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
The multiple mechanisms of action for flavocoxid relating to arachidonic acid (AA) formation and metabolism were studied in vitro.
Flavocoxid titrated into rat peritoneal macrophage cultures inhibited cellular phospholipase A2 (PLA2) (IC50 = 60 μg/mL).
In in vitro enzyme assays, flavocoxid showed little anti-cyclooxygenase (CO) activity on COX-1/-2 enzymes, but inhibited the COX-1 (IC50 = 12.3) and COX-2 (IC50 = 11.3 μg/mL) peroxidase (PO) moieties as well as 5-lipoxygenase (5-LOX) (IC50 = 110 μg/mL).
No detectable 5-LOX inhibition was found for multiple traditional and COX-2 selective NSAIDs.
Flavocoxid also exhibited strong and varied antioxidant capacities in vitro and decreased nitrite levels (IC50 = 38 μg/mL) in rat peritoneal macrophages.
Finally, in contrast to celecoxib and ibuprofen, which upregulated the cox-2 gene, flavocoxid strongly decreased expression.
This work suggests that clinically favourable effects of flavocoxid for management of osteoarthritis (OA) are achieved by simultaneous modification of multiple molecular pathways relating to AA metabolism, oxidative induction of inflammation, and neutralization of reactive oxygen species (ROS).
American Psychological Association (APA)
Burnett, Bruce P.& Bitto, Alessandra& Altavilla, Domenica& Squadrito, Francesco& Levy, Robert M.& Pillai, Lakshmi. 2011. Flavocoxid Inhibits Phospholipase A2, Peroxidase Moieties of the Cyclooxygenases (COX), and 5-Lipoxygenase, Modifies COX-2 Gene Expression, and Acts as an Antioxidant. Mediators of Inflammation،Vol. 2011, no. 2011, pp.1-11.
https://search.emarefa.net/detail/BIM-467958
Modern Language Association (MLA)
Burnett, Bruce P.…[et al.]. Flavocoxid Inhibits Phospholipase A2, Peroxidase Moieties of the Cyclooxygenases (COX), and 5-Lipoxygenase, Modifies COX-2 Gene Expression, and Acts as an Antioxidant. Mediators of Inflammation No. 2011 (2011), pp.1-11.
https://search.emarefa.net/detail/BIM-467958
American Medical Association (AMA)
Burnett, Bruce P.& Bitto, Alessandra& Altavilla, Domenica& Squadrito, Francesco& Levy, Robert M.& Pillai, Lakshmi. Flavocoxid Inhibits Phospholipase A2, Peroxidase Moieties of the Cyclooxygenases (COX), and 5-Lipoxygenase, Modifies COX-2 Gene Expression, and Acts as an Antioxidant. Mediators of Inflammation. 2011. Vol. 2011, no. 2011, pp.1-11.
https://search.emarefa.net/detail/BIM-467958
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-467958