Literature DB >> 22153874

Marine sponge Hymeniacidon sp. amphilectane metabolites potently inhibit rat brain microglia thromboxane B2 generation.

Alejandro M S Mayer1, Edward Avilés, Abimael D Rodríguez.   

Abstract

The effects of five Hymeniacidon sp. amphilectane metabolites (1-5) and two semi-synthetic analogs (6 and 7) on thromboxane B(2) (TXB(2)) and superoxide anion (O(2)(-)) generation from Escherichia coli LPS-activated rat brain microglia were investigated. All Hymeniacidon sp. metabolites and analogs potently inhibited TXB(2) (IC(50)=0.20-4.69μM) with low lactate dehydrogenase release and minimal mitochondrial dehydrogenase inhibition. While a lack of O(2)(-) inhibition would suggest that Hymeniacidon sp. metabolites and derivatives inhibit TXB(2) synthesis by a cyclooxygenase-dependent mechanism, their pharmacologic potency and limited in vitro cytotoxicity warrants further investigation to develop them as lead compounds to modulate enhanced TBX(2) release by activated microglia in neuroinflammatory disorders.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22153874      PMCID： PMC3272584          DOI： 10.1016/j.bmc.2011.10.086

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  12 in total

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2.  Escherichia coli lipopolysaccharide potentiation and inhibition of rat neonatal microglia superoxide anion generation: correlation with prior lactic dehydrogenase, nitric oxide, tumor necrosis factor-alpha, thromboxane B2, and metalloprotease release.

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3.  Monamphilectine A, a potent antimalarial β-lactam from marine sponge Hymeniacidon sp: isolation, structure, semisynthesis, and bioactivity.

Authors:  Edward Avilés; Abimael D Rodríguez
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Journal:  Neuropharmacology       Date:  2000-08-23       Impact factor: 5.250

5.  Activated microglia are the principal glial source of thromboxane in the central nervous system.

Authors:  D Giulian; M Corpuz; B Richmond; E Wendt; E R Hall
Journal:  Neurochem Int       Date:  1996-07       Impact factor: 3.921

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7.  Microdialysis measurements of PGD2, TXB2 and 6-KETO-PGF1 alpha in rat CA1 hippocampus during transient cerebral ischemia.

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Review 8.  Therapeutic implications of microglia activation by lipopolysaccharide and reactive oxygen species generation in septic shock and central nervous system pathologies: a review.

Authors:  A M Mayer
Journal:  Medicina (B Aires)       Date:  1998       Impact factor: 0.653

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6.  Dactyloditerpenol acetate, a new prenylbisabolane-type diterpene from Aplysia dactylomela with significant in vitro anti-neuroinflammatory activity.

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10.  Amphilectene Diterpene Isonitriles and Formamido Derivatives from the Hainan Nudibranch Phyllidia Coelestis.

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  10 in total

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