PTP1B inhibitory and anti-inflammatory effects of secondary metabolites isolated from the marine-derived fungus Penicillium sp. JF-55

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dc.contributor.authorD S Lee-
dc.contributor.authorJae-Hyuk Jang-
dc.contributor.authorW Ko-
dc.contributor.authorK S Kim-
dc.contributor.authorJ H Sohn-
dc.contributor.authorM S Kang-
dc.contributor.authorJong Seog Ahn-
dc.contributor.authorY C Kim-
dc.contributor.authorHyuncheol Oh-
dc.description.abstractProtein tyrosine phosphatase 1B (PTP1B) plays a major role in the negative regulation of insulin signaling, and is thus considered as an attractive therapeutic target for the treatment of diabetes. Bioassay-guided investigation of the methylethylketone extract of marine-derived fungus Penicillium sp. JF-55 cultures afforded a new PTP1B inhibitory styrylpyrone-type metabolite named penstyrylpyrone (1), and two known metabolites, anhydrofulvic acid (2) and citromycetin (3). Compounds 1 and 2 inhibited PTP1B activity in a dose-dependent manner, and kinetic analyses of PTP1B inhibition suggested that these compounds inhibited PTP1B activity in a competitive manner. In an effort to gain more biological potential of the isolated compounds, the anti-inflammatory effects of compounds 1-3 were also evaluated. Among the tested compounds, only compound 1 inhibited the production of NO and PGE2, due to the inhibition of the expression of iNOS and COX-2. Penstyrylpyrone (1) also reduced TNF-α and IL-1β production, and these anti-inflammatory effects were shown to be correlated with the suppression of the phosphorylation and degradation of IκB-α, NF-κB nuclear translocation, and NF-κB DNA binding activity. In addition, using inhibitor tin protoporphyrin (SnPP), an inhibitor of HO-1, it was verified that the inhibitory effects of penstyrylpyrone (1) on the pro-inflammatory mediators and NF-κB DNA binding activity were associated with the HO-1 expression. Therefore, these results suggest that penstyrylpyrone (1) suppresses PTP1B activity, as well as the production of pro-inflammatory mediators via NF-κB pathway, through expression of anti-inflammatory HO-1.-
dc.titlePTP1B inhibitory and anti-inflammatory effects of secondary metabolites isolated from the marine-derived fungus Penicillium sp. JF-55-
dc.title.alternativePTP1B inhibitory and anti-inflammatory effects of secondary metabolites isolated from the marine-derived fungus Penicillium sp. JF-55-
dc.citation.titleMarine Drugs-
dc.contributor.affiliatedAuthorJae-Hyuk Jang-
dc.contributor.affiliatedAuthorJong Seog Ahn-
dc.identifier.bibliographicCitationMarine Drugs, vol. 11, no. 4, pp. 1409-1426-
dc.subject.keywordAnti-inflammatory effect-
dc.subject.keywordHeme oxygenase-1-
dc.subject.keywordMarine-derived fungi-
dc.subject.keywordPenicillium sp.-
dc.subject.keywordPTP1B inhibitors-
dc.subject.localAnti-Inflammatory Effect-
dc.subject.localAnti-inflammatory effect-
dc.subject.localanti-inflammatory effect-
dc.subject.localAnti-inflammatory effects-
dc.subject.localHeme oxygenase-1-
dc.subject.localHeme-oxygenase 1-
dc.subject.localMarine-derived fungi-
dc.subject.localpenicillium sp.-
dc.subject.localPenicillium sp.-
dc.subject.localPTP1B inhibitor-
dc.subject.localPTP1B inhibitors-
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Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
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