Dorantes A L, Aldana I, Pastelín G, Escalante B
Departamento de Farmacología, Instituto Nacional de Cardiología Ignacio Chávez, México, D.F.
Arch Inst Cardiol Mex. 1994 Nov-Dec;64(6):511-5.
It has been shown that, changes in the structure of the cardiac glycoside, are related to changes in their biological effects. In the present study we compared the effects of two structurally different digitalis compound (ouabain and ouabagenin), on K+ induced vascular relaxation as an index of the Na+K+ ATPase activity. Ouabain was the most potent compound tested, and had vasoconstrictor effect on the rat aortic rings, as, well as inhibitory effect on the K(+)-induced relaxation. Ouabagenin did not affect either the vascular tone or K(+)-induced relaxation. It is well known that changes in the part of the structure of the cardiac glycoside that contain the sugar, are important to maintain some of their biological effects. In this paper we demonstrate that elimination of the 1-rhamnose in ouabagenin reduces its vascular effects associated to the inhibition of the Na+ K+ ATPase pump.
已经表明,强心苷结构的变化与其生物学效应的变化有关。在本研究中,我们比较了两种结构不同的洋地黄化合物(哇巴因和哇巴因苷元)对钾离子诱导的血管舒张的影响,以此作为钠钾ATP酶活性的指标。哇巴因是所测试的最有效的化合物,对大鼠主动脉环有血管收缩作用,同时对钾离子诱导的舒张有抑制作用。哇巴因苷元既不影响血管张力,也不影响钾离子诱导的舒张。众所周知,强心苷中含有糖的结构部分的变化对于维持其某些生物学效应很重要。在本文中,我们证明了哇巴因苷元中1-鼠李糖的消除降低了其与抑制钠钾ATP酶泵相关的血管效应。