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dc.contributor.authorQuynh Vo, Nhu Ngoc-
dc.contributor.authorNomura, Yuhta-
dc.contributor.authorMuranaka, Toshiya-
dc.contributor.authorFukushima, Ery Odette-
dc.date.accessioned2020-01-07T14:42:30Z-
dc.date.available2020-01-07T14:42:30Z-
dc.date.issued2019-
dc.identifier.citationVo, N. N. Q., Nomura, Y., Muranaka, T., & Fukushima, E. O. (2019). Structure-Activity Relationships of Pentacyclic Triterpenoids as Inhibitors of Cyclooxygenase and Lipoxygenase Enzymes. Journal of Natural Products. https://doi.org/10.1021/acs.jnatprod.9b00538-
dc.identifier.urihttp://repositorio.ikiam.edu.ec/jspui/handle/RD_IKIAM/328-
dc.identifier.urihttps://doi.org/10.1021/acs.jnatprod.9b00538-
dc.description.abstractPentacyclic triterpenes may be active agentsand provide a rich natural resource of promising compoundsfor drug development. The inhibitory activities of 29 naturaloleanane and ursane pentacyclic triterpenes were evaluatedagainst four major enzymes involved in the inflammatoryprocess: 5-LOX, 15-LOX-2, COX-1, and COX-2. It was foundthat 3-O-acetyl-β-boswellic acid potently inhibited human 15-LOX-2 (IC50= 12.2±0.47μM). Analysis of the structure−activity relationships revealed that the presence of a hydroxygroup at position 24 was beneficial in terms of both 5-LOXand COX-1 inhibition. Notably, the introduction of acarboxylic acid group at position 30 was important for dual5-LOX/COX inhibitory activity; furthermore, its combination with a carbonyl group at C-11 considerably increased 5-LOXinhibition. Also, the presence of anα-hydroxy group at C-2 or a carboxylic acid group at C-23 markedly suppressed the 5-LOXactivity. The presentfindings reveal that the types and configurations of polar moieties at positions C-2, -3, -11, -24, and -30 areimportant structural aspects of pentacyclic triterpenes for their potential as anti-inflammatory lead compounds.es
dc.language.isoenes
dc.publisherAmerican Chemical Societyes
dc.relation.ispartofseriesPRODUCCIÓN CIENTÍFICA-ARTÍCULOS;A-IKIAM-000215-
dc.rightsopenAccesses
dc.rightsAtribución-NoComercial-SinDerivadas 3.0 Estados Unidos de América*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/3.0/us/*
dc.subjectEntacyclices
dc.subjectTriterpenoidses
dc.subjectInhibitors Enzymeses
dc.subjectCyclooxygenase and Lipoxygenasees
dc.titleStructure−Activity Relationships of Pentacyclic Triterpenoids as Inhibitors of Cyclooxygenase and Lipoxygenase Enzymeses
dc.typeArticlees
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