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Inhibition of mammal Na + K + ‐ATPase by diterpenes extracted from the Brazilian brown alga Dictyota cervicornis

2009; Wiley; Volume: 23; Issue: 7 Linguagem: Inglês

10.1002/ptr.2600

1099-1573

Diogo Gomes Garcia, Έverson Miguel Bianco, Maria da Conceição Batista dos Santos, Renato Crespo Pereira, Mauro Velho de Castro Faria, Valéria Laneuville Teixeira, Patrícia Burth,

Echinoderm biology and ecology

Abstract The dolastane diterpenes 4‐acetoxy‐9,14‐dihydroxydolast‐1(15),7‐diene (1) and 4,7‐diacetoxy‐14‐hydroxydolast‐1(15),8‐diene (2) were isolated from specimens of the alga Dictyota cervicornis collected from the Rio de Janeiro coast, Brazil. Chemical structures of the diterpenes were assigned by 1D and 2D NMR spectral data for the first time. Both substances inhibited Na + K + ‐ATPase preparations from guinea‐pig brain or kidney, with the same inhibitory potency towards enzyme isoforms. The maximal inhibition obtained for 1 was 40% at a concentration of 0.5 m m in the incubation mixture, while it reached 80% for compound 2 at this concentration. Ouabain insensitive ATPases were inhibited by 1, but not by 2. Data comparing the inhibitory potency of these compounds with that of ouabain and oleic acid suggest a higher degree of selectivity of 2 towards the Na + K + ‐pump. Cardiac glycosides such as ouabain are used classically in the treatment of heart failure, but alterations of Na + K + ‐pump activity are also involved in several other diseases. Therefore, the study of compounds interfering with this pump activity is gaining further importance. Copyright © 2009 John Wiley & Sons, Ltd.