In vitro inhibition of [3H]-angiotensin II binding on the human AT1 receptor by proanthocyanidins from Guazuma ulmifolia bark

被引:37
作者
Caballero-George, C
Vanderheyden, PML
De Bruyne, T
Shahat, AA
Van den Heuvel, H
Solis, PN
Gupta, MP
Claeys, M
Pieters, L
Vauquelin, G
Vlietinck, AJ
机构
[1] Univ Antwerp, UIA, Dept Pharmaceut Sci, B-2610 Antwerp, Belgium
[2] Free Univ Brussels, Dept Mol & Biochem Pharmacol, VUB, Rhode St Genese, Belgium
[3] Univ Panama, Sch Pharm, Ctr Pharmacognost Res Panamanian Flora, CIFLORPAN, Panama City, Panama
关键词
proanthocyanidins; AT(1) receptor; CHO cells; Guazuma ulmifolia; Sterculiaceae; radioligand-binding;
D O I
10.1055/s-2002-36344
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
A bioassay-guided fractionation of the 70% acetone extract of the bark of Guazuma ulmifolia Lam. on the inhibition of angiotensin 11 binding to the AT, receptor led to the isolation and identification of bioactive oligomeric and polymeric proanthocyanidins consisting mainly of (-)-epicatechin units. The displacement of [H-3]-angiotensin 11 binding was dose-dependent and correlated with the degree of polymerization of the different fractions containing proanthocyanidins. A strong displacement was seen for the residual fraction suggesting that the most active substances corresponding to the highly polymerized proanthocyanidins. Angiotensin 11 AT(1) receptor binding might be considered as a potentially interesting biological activity of proanthocyanidins contributing to the very broad spectrum of biological activities of the condensed tannins.
引用
收藏
页码:1066 / 1071
页数:6
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