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Biological and anti-inflammatory evaluation of two thiazole compounds in RAW cell line: Potential cyclooxygenase-2 specific inhibitors

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dc.contributor.author Hamade E.
dc.contributor.author Habib A.
dc.contributor.author Hachem A.
dc.contributor.author Hussein A.H.
dc.contributor.author Abbas M.
dc.contributor.author Hirz T.
dc.contributor.author Al Masri M.
dc.contributor.author Faour W.H.
dc.contributor.editor
dc.date 2012
dc.date.accessioned 2017-10-05T15:30:57Z
dc.date.available 2017-10-05T15:30:57Z
dc.date.issued 2012
dc.identifier
dc.identifier.isbn
dc.identifier.issn 15734064
dc.identifier.uri http://hdl.handle.net/10938/15290
dc.description.abstract The anti-inflammatory effect of two new thiazoles derivatives CX-32 (N-[4-(4-hydroxy-3-methoxyphenyl)-1,3-thiazol-2-yl]acetamide ) and CX-35 (4-(2-amino-1,3-thiazol-4-yl)-2-methoxyphenol), was investigated in LPS-stimulated RAW 264.7 cell line. Synthesis, structure analysis and purity of these compounds were evaluated by high performance liquid chromatography, H 1 NMR, and C13 NMR. Assessment of CX-32 and CX-35 inhibitory effect on cyclooxygenase-2 (COX-2) activity was achieved by incubating LPS-activated RAW cells with 25 μM, 50μM or 100μM of CX-32 or CX-35, respectively. Levels of secreted PGE2 were evaluated by enzyme immunoassay (EIA) and levels of COX-2 protein were measured by western blot. Finally, cell viability experiments were undertaken to assess the toxicity of each compound. Treatment of LPS-activated RAW cells with 25 μM, 50 μM, or 100 μM of CX-35 or CX-32, respectively, prevented the production of prostaglandins, but was without an effect on COX-2 protein levels. Moreover, CX-35 and CX-32 reduced PGE2 production to levels comparable to those obtained in LPS-activated RAW cells incubated with the selective COX-2 inhibitor NS 398. Furthermore, both CX-32 and CX-35 showed no toxic effects, since the viability of non-treated Hela cells was similar to Hela cells incubated with either CX-35 or CX-32. Our data demonstrated that CX-32 and CX-35 significantly blocked prostaglandin production induced during inflammatory cellular stress, possibly acting through specific COX-2 inhibition; confirmation of this hypothesis requires further investigation. © 2012 Bentham Science Publishers.
dc.format.extent
dc.format.extent Pages: (401-408)
dc.language English
dc.publisher SHARJAH
dc.relation.ispartof Publication Name: Medicinal Chemistry; Publication Year: 2012; Volume: 8; no. 3; Pages: (401-408);
dc.relation.ispartofseries
dc.relation.uri
dc.source Scopus
dc.subject.other
dc.title Biological and anti-inflammatory evaluation of two thiazole compounds in RAW cell line: Potential cyclooxygenase-2 specific inhibitors
dc.type Article
dc.contributor.affiliation Hamade, E., Département de Chimie et Biochimie, Plateforme de Recherche en Sciences et Technologies, Université Libanaise, Hadath, Lebanon
dc.contributor.affiliation Habib, A., Faculty of Medicine, American University of Beirut, Beirut, Lebanon
dc.contributor.affiliation Hachem, A., Laboratoire de Chimie Médicinale et des Produits Naturels, Département de Chimie et Biochimie, Université Libanaise, Hadath, Lebanon
dc.contributor.affiliation Hussein, A.H., Laboratoire de Chimie Médicinale et des Produits Naturels, Département de Chimie et Biochimie, Université Libanaise, Hadath, Lebanon
dc.contributor.affiliation Abbas, M., Département de Chimie et Biochimie, Plateforme de Recherche en Sciences et Technologies, Université Libanaise, Hadath, Lebanon
dc.contributor.affiliation Hirz, T., Faculty of Medicine, American University of Beirut, Beirut, Lebanon
dc.contributor.affiliation Al Masri, M., Département de Chimie et Biochimie, Plateforme de Recherche en Sciences et Technologies, Université Libanaise, Hadath, Lebanon
dc.contributor.affiliation Faour, W.H., School of Medicine, Lebanese American University, Lebanon P.O. Box 36, Byblos, Lebanon
dc.contributor.authorAddress Faour, W.H.; School of Medicine, Lebanese American University, Lebanon P.O. Box 36, Byblos, Lebanon; email: wissam.faour@lau.edu.lb
dc.contributor.authorCorporate University: American University of Beirut Medical Center; Faculty: Faculty of Medicine; Department: Biochemistry and Molecular Genetics;
dc.contributor.authorDepartment Biochemistry and Molecular Genetics
dc.contributor.authorDivision
dc.contributor.authorEmail wissam.faour@lau.edu.lb
dc.contributor.authorFaculty Faculty of Medicine
dc.contributor.authorInitials Hamade, E
dc.contributor.authorInitials Habib, A
dc.contributor.authorInitials Hachem, A
dc.contributor.authorInitials Hussein, AH
dc.contributor.authorInitials Abbas, M
dc.contributor.authorInitials Hirz, T
dc.contributor.authorInitials Al Masri, M
dc.contributor.authorInitials Faour, WH
dc.contributor.authorOrcidID
dc.contributor.authorReprintAddress Faour, WH (reprint author), Lebanese Amer Univ, Sch Med, Lebanon POB 36, Byblos, Lebanon.
dc.contributor.authorResearcherID
dc.contributor.authorUniversity American University of Beirut Medical Center
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dc.description.citedCount 1
dc.description.citedTotWOSCount 1
dc.description.citedWOSCount 1
dc.format.extentCount 8
dc.identifier.articleNo
dc.identifier.coden MCEHA
dc.identifier.pubmedID 22530893
dc.identifier.scopusID 84863643068
dc.identifier.url
dc.publisher.address EXECUTIVE STE Y26, PO BOX 7917, SAIF ZONE, 1200 BR SHARJAH, U ARAB EMIRATES
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dc.relation.ispartofConferenceCode
dc.relation.ispartofConferenceDate
dc.relation.ispartofConferenceHosting
dc.relation.ispartofConferenceLoc
dc.relation.ispartofConferenceSponsor
dc.relation.ispartofConferenceTitle
dc.relation.ispartofFundingAgency
dc.relation.ispartOfISOAbbr Med. Chem.
dc.relation.ispartOfIssue 3
dc.relation.ispartOfPart
dc.relation.ispartofPubTitle Medicinal Chemistry
dc.relation.ispartofPubTitleAbbr Med. Chem.
dc.relation.ispartOfSpecialIssue
dc.relation.ispartOfSuppl
dc.relation.ispartOfVolume 8
dc.source.ID WOS:000305295000010
dc.type.publication Journal
dc.subject.otherAuthKeyword Cyclooxygenase inhibitors
dc.subject.otherAuthKeyword Drug design
dc.subject.otherAuthKeyword Inflammation
dc.subject.otherAuthKeyword Medicinal chemistry
dc.subject.otherAuthKeyword Prostaglandins
dc.subject.otherAuthKeyword Thiazoles
dc.subject.otherChemCAS n (2 cyclohexyloxy 4 nitrophenyl)methanesulfonamide, 123653-11-2
dc.subject.otherChemCAS prostaglandin E2, 363-24-6
dc.subject.otherChemCAS 4-(2-amino-1,3-thiazol-4-yl)-2-methoxyphenol
dc.subject.otherChemCAS Acetamides
dc.subject.otherChemCAS Anti-Inflammatory Agents, Non-Steroidal
dc.subject.otherChemCAS Cyclooxygenase 2, 1.14.99.1
dc.subject.otherChemCAS Cyclooxygenase 2 Inhibitors
dc.subject.otherChemCAS Lipopolysaccharides
dc.subject.otherChemCAS N-(4-(4-hydroxy-3-methoxyphenyl)-1,3-thiazol-2-yl)acetamide
dc.subject.otherChemCAS Thiazoles
dc.subject.otherIndex 4 (2 amino 1,3 thiazol 4 yl) 2 methoxyphenol
dc.subject.otherIndex antiinflammatory agent
dc.subject.otherIndex cyclooxygenase 2 inhibitor
dc.subject.otherIndex n (2 cyclohexyloxy 4 nitrophenyl)methanesulfonamide
dc.subject.otherIndex n[4 (4 hydroxy 3 methoxyphenyl) 1,3 thiazol 2 yl]acetamide
dc.subject.otherIndex prostaglandin E2
dc.subject.otherIndex unclassified drug
dc.subject.otherIndex animal cell
dc.subject.otherIndex animal experiment
dc.subject.otherIndex animal model
dc.subject.otherIndex animal tissue
dc.subject.otherIndex antiinflammatory activity
dc.subject.otherIndex article
dc.subject.otherIndex carbon nuclear magnetic resonance
dc.subject.otherIndex cell stress
dc.subject.otherIndex cell viability
dc.subject.otherIndex controlled study
dc.subject.otherIndex drug purity
dc.subject.otherIndex drug screening
dc.subject.otherIndex drug synthesis
dc.subject.otherIndex enzyme immunoassay
dc.subject.otherIndex HeLa cell
dc.subject.otherIndex high performance liquid chromatography
dc.subject.otherIndex human
dc.subject.otherIndex human cell
dc.subject.otherIndex leukemia cell line
dc.subject.otherIndex male
dc.subject.otherIndex mouse
dc.subject.otherIndex nonhuman
dc.subject.otherIndex priority journal
dc.subject.otherIndex proton nuclear magnetic resonance
dc.subject.otherIndex structure analysis
dc.subject.otherIndex Western blotting
dc.subject.otherIndex Acetamides
dc.subject.otherIndex Animals
dc.subject.otherIndex Anti-Inflammatory Agents, Non-Steroidal
dc.subject.otherIndex Cell Survival
dc.subject.otherIndex Cells, Cultured
dc.subject.otherIndex Cyclooxygenase 2
dc.subject.otherIndex Cyclooxygenase 2 Inhibitors
dc.subject.otherIndex Dose-Response Relationship, Drug
dc.subject.otherIndex HeLa Cells
dc.subject.otherIndex Humans
dc.subject.otherIndex Lipopolysaccharides
dc.subject.otherIndex Macrophages
dc.subject.otherIndex Mice
dc.subject.otherIndex Structure-Activity Relationship
dc.subject.otherIndex Thiazoles
dc.subject.otherKeywordPlus ACTIVATED PROTEIN-KINASE
dc.subject.otherKeywordPlus NECROSIS-FACTOR-ALPHA
dc.subject.otherKeywordPlus COX-2 INHIBITORS
dc.subject.otherKeywordPlus SYNOVIAL FIBROBLASTS
dc.subject.otherKeywordPlus MESSENGER-RNA
dc.subject.otherKeywordPlus OSTEOARTHRITIS
dc.subject.otherKeywordPlus NSAID
dc.subject.otherKeywordPlus INTERLEUKIN-1-BETA
dc.subject.otherKeywordPlus EXPRESSION
dc.subject.otherKeywordPlus STABILITY
dc.subject.otherWOS Chemistry, Medicinal


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