Kamernitskiĭ A V, Reshetova I G, Mirsalikhova N M, Uvarova N I, Atopkina L N
Bioorg Khim. 1984 May;10(5):666-9.
Transformed steroids having oxidized side chains in the D ring site and varying by polarity of the substituent at the ring A C(3)-position--acetates, glucosides or with free hydroxyls--in the concentration range 1 X 10(-4) - 1 X 10(-7) M were found to inhibit Na+, K+-ATPase. The extent of inhibition decreases with the rise in the polarity of the A region of the steroid molecule. With the compound devoid of polar groups in the D region an increase in the inhibitory activity is observed on passing from 3-acetate to 3-glucoside. The data obtained confirm the relationship between the extent of Na+, K+-ATPase inhibition and biphilicity of the molecule.
在D环位点具有氧化侧链且在A环C(3)位的取代基极性不同(乙酸酯、糖苷或具有游离羟基)的转化甾体,在1×10⁻⁴ - 1×10⁻⁷ M浓度范围内被发现可抑制Na⁺, K⁺-ATP酶。抑制程度随甾体分子A区域极性的增加而降低。对于在D区域没有极性基团的化合物,从3-乙酸酯转变为3-糖苷时观察到抑制活性增加。所获得的数据证实了Na⁺, K⁺-ATP酶抑制程度与分子双亲性之间的关系。