[乙酰水杨酸和吲哚美辛与内过氧化物前列腺素合成酶的相互作用机制]
[Mechanisms of interaction of acetylsalicylic acid and indomethacin with endoperoxide prostaglandin synthetase].
作者信息
Muratov V K, Igumnova N D, Basevich V V, Churiukanov V V, Mevkh A T
出版信息
Farmakol Toksikol. 1983 Sep-Oct;46(5):44-8.
A study was made of the character and kinetics of interaction of acetylsalicylic acid and indomethacin with endoperoxide prostaglandin synthetase (PGH-synthetase) of sheep vesicular glands and human platelets. Enzymatic activity of PGH-synthetase was determined polarographically with the aid of Clark's electrodes. Acetylsalicylic acid was found to inhibit PGH-synthetase of sheep vesicular glands and human platelets at concentrations of the order of 1 x 10(-6) and 1 x 10(-4) M, whereas indomethacin at concentrations of 1 x 10(-6) and 1 x 10(-7) M, respectively. Acetylsalicylic acid inhibited PGH-synthetase from sheep vesicular glands and that from human platelets at an equal rate. Indomethacin inhibited the enzyme from sheep vesicular glands to a higher degree. Indomethacin reversibly interacted with PGH-synthetase. Meanwhile acetylsalicylic acid inhibited this enzyme irreversibly.
对乙酰水杨酸和吲哚美辛与绵羊精囊和人血小板的内过氧化物前列腺素合成酶（PGH合成酶）相互作用的特性及动力学进行了研究。借助克拉克电极通过极谱法测定PGH合成酶的酶活性。发现乙酰水杨酸在1×10⁻⁶和1×10⁻⁴ M左右的浓度下抑制绵羊精囊和人血小板的PGH合成酶，而吲哚美辛分别在1×10⁻⁶和1×10⁻⁷ M的浓度下抑制。乙酰水杨酸以相同速率抑制绵羊精囊和人血小板的PGH合成酶。吲哚美辛对绵羊精囊的该酶抑制程度更高。吲哚美辛与PGH合成酶可逆性相互作用。同时，乙酰水杨酸不可逆地抑制该酶。
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