甜杆儿酸B，一种从甜杆儿（Scoparia dulcis L.）中提取的新型四环二萜。其结构、H⁺、K⁺ - 腺苷三磷酸酶抑制活性及在大鼠体内的药代动力学行为。
Scopadulcic acid B, a new tetracyclic diterpenoid from Scoparia dulcis L. Its structure, H+, K(+)-adenosine triphosphatase inhibitory activity and pharmacokinetic behaviour in rats.
作者信息
Hayashi T, Okamura K, Kakemi M, Asano S, Mizutani M, Takeguchi N, Kawasaki M, Tezuka Y, Kikuchi T, Morita N
机构信息
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Japan.
出版信息
Chem Pharm Bull (Tokyo). 1990 Oct;38(10):2740-5. doi: 10.1248/cpb.38.2740.
The structure of scopadulcic acid B (2, SDB), a major ingredient of the Paraguayan herb "Typychá kuratũ" (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 20-30 microM for IC50 and proton transport into gastric 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.
巴拉圭草药“Typychá kuratũ”（甜杆草，Scoparia dulcis L.）的主要成分scopadulcic酸B（2，SDB）的结构，主要是通过将其光谱数据与scopadulcic酸A（1）的光谱数据进行比较来阐明的。SDB抑制猪胃质子泵（H +，K + -ATP酶）的K（+）依赖性腺苷三磷酸酶（ATP酶）活性，IC50值为20 - 30 microM，并抑制质子转运到胃小泡中。SDB在大鼠中的药代动力学研究表明，静脉注射SDB钠盐（SDB-Na）后，血浆SDB浓度通过具有米氏消除动力学的二室开放模型得到了合理的良好描述。口服SDB-Na或SDB后血浆浓度的下降比静脉注射研究预期的要慢得多。有人认为，口服SDB-Na或SDB后SDB的血浆水平持续存在是由于大鼠胃肠道吸收相对缓慢但有效所致。
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