Inhibition of Na+,K+-ATPase activity by (-)-ent-Kaur-16-en-19-oic acid and its derivatives.

Planta Med

Research Centre for Bioorganic Chemistry, Department of Chemistry, Faculty of Science, Chulalongkorn University, Pathumwan, Bangkok, Thailand.

Published: June 2003

The diterpene, (-)- ent-kaur-16-en-19-oic acid, from Croton oblongifolius was identified as an Na +,K +-ATPase inhibitor. This compound exhibits an IC 50 of 2.2 x 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, (-)-16beta,17-epoxykauran-19-oic acid and (-)-17-hydroxykaur-15-en-19-oic acid were also tested and their IC 50 were 5.5 x 10 (-4), 5.0 x 10( -4), 4.8 x 10( -4) and 6.0 x 10 (-4) M, respectively.

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http://dx.doi.org/10.1055/s-2003-40636DOI Listing

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