Karsanov N V, Kipshidze N N, Sukoian G V, Guchua Z I, Tatulashvili D R, Karsanov V N, Iarovaia E V, Magaldadze V A, Turmanauli G S
Eksp Klin Farmakol. 1996 May-Jun;59(3):28-33.
The in vitro study on an isolated system of myocardial contractile proteins determined optimal concentrations of the positive inotropic action and biological activity ranges of beta-methyldigoxin (beta-MD), strophanthin K, K-strophantozide, beta-acetyldigoxin (beta-AD), milrinone, and amrinone. Optimal concentrations of the beta-MD and strophanthin K (10(-2) and 10(-6) M, respectively) significantly increased qualitatively and quantitatively the economy and thermodynamic efficiency, altered the energy transformation in the contractile protein system under the isometric contraction, whereas the beta-AD produced only the quantitative effect. However, the beta-MD and strophanthin K at concentrations exceeding the optimal one by one order lost the ability to produce the qualitative effect, retaining only the quantitative one in the actomyosin ensemble. The strophanthin K significantly increased the economy of a single actomyosin ensemble in the force generation phase and the beta-MD in the tension maintenance phase. Unlike the strophanthin K, the beta-MD did not slow down (did not worsen) the relaxation process. This provides grounds to conclude that the beta-MD produces most favorable effect on the energy transformation by myocardial contractile proteins.
对心肌收缩蛋白分离系统进行的体外研究确定了β-甲基地高辛(β-MD)、毒毛花苷K、毒毛花苷K苷、β-乙酰地高辛(β-AD)、米力农和氨力农正性肌力作用的最佳浓度以及生物活性范围。β-MD和毒毛花苷K的最佳浓度(分别为10^(-2)和10^(-6) M)在定性和定量方面均显著提高了经济性和热力学效率,改变了等长收缩下收缩蛋白系统中的能量转换,而β-AD仅产生定量效应。然而,β-MD和毒毛花苷K的浓度超过最佳浓度一个数量级时,失去了产生定性效应的能力,在肌动球蛋白总体中仅保留了定量效应。毒毛花苷K在力产生阶段显著提高了单个肌动球蛋白总体的经济性,而β-MD在张力维持阶段有此作用。与毒毛花苷K不同,β-MD不会减缓(不会恶化)舒张过程。这为得出β-MD对心肌收缩蛋白的能量转换产生最有利影响这一结论提供了依据。