Title:Evaluation of the Effect of α-L-Guluronic Acid (G2013) on COX-1, COX-2 Activity and Gene Expression for Introducing this Drug as a Novel NSAID with Immunomodulatory Property
VOLUME: 12 ISSUE: 2
Author(s):Abbas Mirshafiey*, Seyed S. Mortazavi-Jahromi, Mahsa Taeb, Salvatore Cuzzocrea and Emanuela Esposito
Affiliation:Department of Immunology, School of Public Health, Tehran University of Medical Sciences, Tehran, Department of Immunology, School of Public Health, Tehran University of Medical Sciences, Tehran, Department of Immunology, School of Public Health, Tehran University of Medical Sciences, Tehran, Department of Chemical, Biological, Pharmacological and Environmental Sciences, University of Messina, Messina, Department of Chemical, Biological, Pharmacological and Environmental Sciences, University of Messina, Messina
Keywords:COX-1, COX-2, G2013, guluronic acid, immunomodulation, NSAIDs, PGE2.
Abstract:Background: Nonsteroidal anti-inflammatory drugs (NSAIDs) are used to treat the pathological
pain and inflammation through inhibition of cyclooxygenase (COX) enzyme and disruption of
the synthesis of prostaglandins (PGs). The α-L-guluronic acid (G2013) patented
(PCT/EP2017/067920), as a novel NSAID with the immunomodulatory property, has been shown its
positive effects in experimental models of multiple sclerosis and anti-aging.
Objective: This study was aimed to investigate the effects of G2013 on the gene expression and activity
of COX-1/COX-2 enzymes in order to introduce a novel NSAID for the treatment of inflammatory
diseases.
Method: The mRNA expression levels of COX-1/COX-2 were measured by qRT-PCR. The PGE2 concentration
in culture media was determined using ELISA method.
Results: Our results demonstrated that the low and high dose of G2013 could significantly reduce the
gene expression of COX-1 and COX-2, as compared to the control treated with LPS (p < 0.05). In addition,
data showed that 5, 50 and 500 mMol/ml doses of this drug can significantly the reduce activities
of COX-1 and COX-2, as compared to the control treated with LPS and AA (p < 0.0001).
Conclusion: This study revealed that G2013, as a novel NSAID with the immunomodulatory property,
is able to reduce the gene expression and activity of COX-1/COX-2 enzymes. According to the findings,
this agent might be categorized and introduced as a novel NSAID for the treatment of inflammatory
diseases.
