Inhibition of Na+,K+-ATPase activity by (-)-ent-Kaur-16-en-19-oic acid and its derivatives.
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.
Ngamrojnavanich
Nattaya
N
Research Centre for Bioorganic Chemistry, Department of Chemistry, Faculty of Science, Chulalongkorn University, Pathumwan, Bangkok, Thailand.
Sirimongkon
Supaporn
S
Roengsumran
Sophon
S
Petsom
Amorn
A
Kamimura
Hishashi
H
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000201:enzymology; D029802:Croton; D004224:Diterpenes / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D020128:Inhibitory Concentration 50; D008517:Phytotherapy; D024301:Plant Bark; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D018547:Plant Stems; D051381:Rats; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors*
D004224:Diterpenes; D004791:Enzyme Inhibitors; D010936:Plant Extracts; C014341:argyrophilic acid; D000254:Sodium-Potassium-Exchanging ATPase