دورية أكاديمية

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

التفاصيل البيبلوغرافية
العنوان: 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
المؤلفون: Mirshafiey, Abbas, Mortazavi-Jahromi, Seyed S., Taeb, Mahsa, Cuzzocrea, Salvatore, Esposito, Emanuela
المساهمون: Mirshafiey, Abba, Mortazavi-Jahromi, Seyed S., Taeb, Mahsa, Cuzzocrea, Salvatore, Esposito, Emanuela
بيانات النشر: Bentham Science Publishers Ltd
سنة النشر: 2018
المجموعة: Università degli Studi di Messina: IRIS
مصطلحات موضوعية: COX-1, COX-2, G2013, Guluronic acid, Immunomodulation, NSAID, PGE2, Adult, Anti-Inflammatory Agents, Non-Steroidal, Cells, Cultured, Cyclooxygenase 1, Cyclooxygenase 2, Female, Gene Expression Regulation, Human, Immunologic Factor, Inflammation, Leukocytes, Mononuclear, Male, Middle Aged, RNA, Messenger, Uronic Acid, Immunology and Allergy, Drug Discovery3003 Pharmaceutical Science
الوصف: 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 alpha-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 PGE(2) 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.
نوع الوثيقة: article in journal/newspaper
وصف الملف: STAMPA
اللغة: English
العلاقة: info:eu-repo/semantics/altIdentifier/pmid/29879894; info:eu-repo/semantics/altIdentifier/wos/WOS:000452805000008; volume:12; issue:2; firstpage:162; lastpage:168; numberofpages:7; journal:RECENT PATENTS ON INFLAMMATION & ALLERGY DRUG DISCOVERY; http://hdl.handle.net/11570/3134260Test; info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-85053837506; http://www.eurekaselect.com/162888Test
DOI: 10.2174/1872213X12666180607121809
الإتاحة: https://doi.org/10.2174/1872213X12666180607121809Test
http://hdl.handle.net/11570/3134260Test
http://www.eurekaselect.com/162888Test
حقوق: info:eu-repo/semantics/openAccess
رقم الانضمام: edsbas.CBD87951
قاعدة البيانات: BASE