Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Scopadulcic Acid B, a New Tetracyclic Diterpenoid from Scoparia dulcis L. Its Structure, H+, K+-Adenosine Triphosphatase Inhibitory Activity and Pharmacokinetic Behaviour in Rats
Toshimitsu HAYASHIKana OKAMURAMasawo KAKEMIShinji ASANOMotofumi MIZUTANINoriaki TAKEGUCHIMasaru KAWASAKIYasuhiro TEZUKATohru KIKUCHINaokata MORITA
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1990 Volume 38 Issue 10 Pages 2740-2745

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Abstract

The structure of scopadulcic acid B (2, SDB), a major ingredient of the Paraguayan herb "Typycha kuratu" (Scoparia dulcis L.), was elucidated mainly by comparison of its spectral data with that of scopadulcic acid A (1). SDB inhibited both the K+-dependent adenosine triphosphatase (ATPase) activity of a hog gastric proton pump (H+, K+-ATPase) with a value of 20-30μM for IC50 and proton transport into grastric vesicles. Pharmacokinetic studies of SDB in rats indicated that plasma SDB concentrations after i.v. injection of the sodium salt of SDB (SDB-Na) were described reasonably well by a two-compartment open model with Michaelis-Menten elimination kinetics. Plasma concentrations after oral administration of SDB-Na or SDB showed a much slower decline than what was expected following the i. v. study. It was suggested that the sustained plasma level of SDB after oral administration of SDB-Na or SDB was accounted for by relatively slow but efficient gastro-intestinal absorption in rats.

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