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维生素K与香豆素类抗凝剂:抗凝作用对抗维生素K转运抑制的依赖性

Vitamin K and coumarin anticoagulants: dependence of anticoagulant effect on inhibition of vitamin K transport.

作者信息

Lowenthal J, Birnbaum H

出版信息

Science. 1969 Apr 11;164(3876):181-3. doi: 10.1126/science.164.3876.181.

DOI:10.1126/science.164.3876.181
PMID:5774189
Abstract

Coumarin anticoagulants inhibit the release of plasma clotting factor VII by vitamin K in liver slices from vitamin K-deficient animals without inhibition of protein synthesis. When the ratio of vitamin K to coumarin anticoagulant is kept constant, but the concentrations are increased, the inhibition disappears. This suggests that the pharmacological action of coumarin anticoagulants depends on irreversible inhibition of normal vitamin K transport to its site of action. At higher concentrations of vitamin K the inhibition can be surmounted, because vitamin K can enter the cell by an alternate route that is not inhibited by coumarin anticoagulants.

摘要

香豆素类抗凝剂可抑制维生素K缺乏动物肝脏切片中维生素K诱导的血浆凝血因子VII的释放,而不抑制蛋白质合成。当维生素K与香豆素类抗凝剂的比例保持恒定,但浓度增加时,抑制作用消失。这表明香豆素类抗凝剂的药理作用取决于对正常维生素K转运至其作用位点的不可逆抑制。在较高浓度的维生素K作用下,这种抑制作用可以被克服,因为维生素K可以通过一条不受香豆素类抗凝剂抑制的替代途径进入细胞。

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Vitamin K and coumarin anticoagulants: dependence of anticoagulant effect on inhibition of vitamin K transport.维生素K与香豆素类抗凝剂:抗凝作用对抗维生素K转运抑制的依赖性
Science. 1969 Apr 11;164(3876):181-3. doi: 10.1126/science.164.3876.181.
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Use of competitive vitamin K antagonist, 2-chloro-3-phytyl-1,4-naphthoquinone, for the study of the mechanism of action of vitamin K and coumarin anticoagulants.使用竞争性维生素K拮抗剂2-氯-3-植基-1,4-萘醌研究维生素K和香豆素抗凝剂的作用机制。
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Comparison of the activity of the cis and trans isomer of vitamin K1 in vitamin K-deficient and coumarin anticoagulant-pretreated rats.维生素K缺乏和香豆素抗凝预处理大鼠中维生素K1顺式和反式异构体活性的比较。
J Pharmacol Exp Ther. 1979 Jun;209(3):330-3.
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Inhibition of vitamin K epoxidase by two non-coumarin anticoagulants.两种非香豆素类抗凝剂对维生素K环氧化酶的抑制作用。
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Reversal by vitamin K of cycloheximide inhibited biosynthesis of prothrombin in the isolated perfused rat liver.维生素K可逆转环己酰亚胺对离体灌注大鼠肝脏中凝血酶原生物合成的抑制作用。
Biochem Biophys Res Commun. 1970 Mar 27;38(6):1041-8. doi: 10.1016/0006-291x(70)90344-x.

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