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
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