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RESEARCH PRODUCT
Dysidotronic acid, a new and selective human phospholipase A2 inhibitor from the sponge Dysidea sp.
Clelia GianniniCécile DebitusMiguel PayáMaria Valeria D'auriaInmaculada Posadassubject
chemistry.chemical_classificationbiologyStereochemistryChemical structureOrganic Chemistrybiology.organism_classificationBiochemistrySpongeManoalidechemistry.chemical_compoundEnzymePhospholipase A2chemistryBiochemistryDrug Discoverybiology.proteinPotencySelectivityIC50description
Abstract A new bioactive sesquiterpenoid, named dysidotronic acid 1, with a rearranged drimane skeleton has been isolated from the sponge Dysidea sp. from Vanuatu islands, along with bolinaquinone 2. The chemical structure of 1 was determined on the basis of spectroscopic data. Dysidotronic acid significantly inhibited human synovial phospholipase A2 (PLA2) at 10 μM, with an IC50 value of 2.6 μM and a higher selectivity and potency towards this enzyme than the reference inhibitor manoalide.
year | journal | country | edition | language |
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2000-04-01 | Tetrahedron Letters |