硫代强心甾内酯 I：3β-硫氰酸根合-14β-羟基-5β-强心甾-20(22)-烯内酯的合成及生物学作用
Thiocardenolides I: synthesis and biological actions of 3beta-thiocyanato-14beta-hydroxy-5beta-card-20(22)-enolide.
作者信息
Abramson H N, Huang C L, Wu T F, Tobin T
出版信息
J Pharm Sci. 1976 May;65(5):765-8. doi: 10.1002/jps.2600650541.
PMID:132523
Abstract
The synthesis of a 3beta-thiocyanatocardenolide is described. The compound exhibited about 0.1 times the cardiotonic effect of digitoxyigenin in the isolated frog heart preparation. At a dosage of 20 mg/kg in the intact rat, it elicited ECG changes similar to those seen with a 10-mg/kg dose of digitoxigenin. Studies also revealed the new cardenolide to be a reversible inhibitor of sodium- and potassium-activated adenosine triphosphatase.
摘要
描述了一种3β-硫氰基强心甾内酯的合成。该化合物在离体蛙心制备中表现出约为洋地黄毒苷元强心作用的0.1倍。在完整大鼠中，以20mg/kg的剂量给药时，它引起的心电图变化与10mg/kg剂量的洋地黄毒苷元所引起的变化相似。研究还表明，这种新的强心甾内酯是钠钾激活的三磷酸腺苷酶的可逆抑制剂。
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