Inhibition of Na⁺,K⁺-ATPase Activity by (-)-ent-Kaur-16-en-19-oic Acid and its Derivatives

Abstract

The diterpene, (-)-ent-kaur-16-en-19-oic acid, from Croton oblongifolius was identified as an Na⁺,K⁺-ATPase inhibitor. This compound exhibits an IC₅₀ of 2.2 × 10^-5 M against crude enzyme Na⁺,K⁺-ATPase from rat brain. The semi-synthetic derivatives, (-)-methyl kaur-16-en-19-oate, (-)-kaur-16-en-19-ol, (-)-16β,17-epoxykauran-19-oic acid and (-)-17-hydroxykaur-15-en-19-oic acid were also tested and their IC₅₀ were 5.5 × 10^-4, 5.0 × 10^-4, 4.8 × 10^-4 and 6.0 × 10^-4 M, respectively.

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