6533b81ffe1ef96bd1278f29

RESEARCH PRODUCT

Dysidotronic acid, a new and selective human phospholipase A2 inhibitor from the sponge Dysidea sp.

Clelia GianniniCécile DebitusMiguel PayáMaria Valeria D'auriaInmaculada Posadas

subject

chemistry.chemical_classificationbiologyStereochemistryChemical structureOrganic Chemistrybiology.organism_classificationBiochemistrySpongeManoalidechemistry.chemical_compoundEnzymePhospholipase A2chemistryBiochemistryDrug Discoverybiology.proteinPotencySelectivityIC50

description

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.

https://doi.org/10.1016/s0040-4039(00)00362-2