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Effects of Alkylidenephthalides on the Pituitrin-Induced Alternations in Isolated Guinea Pig Hearts

亞羥基隣苯二甲內酯對離體天竺鼠因垂體後葉素引起之改變的作用

摘要


亞丁基隣笨二甲內酯是川芎(Ligusticum wallichii F(下標 RANCH),繖形科)的成分,曾被證實是重要而且最具抗痙的作用,爲研究亞經基的長度對其抗虛作用的影響,我們合成四種亞羥基隣笨二甲內酯(亞乙基、亞丙基、亞丁基及亞戊基隣笨二甲內酯),本研究是爲瞭解這四種對離體天竺鼠因垂體後葉素引起之冠流量、心收縮力及心跳減少的作用。 亞丁基隣笨二甲內酯像硝基甘油,但不像氨基比林,有意義地對抗因垂體後葉素引起的冠流量減少,氨基比林無意義但輕微地增加收縮力及心跳,硝基甘油有意義地減少心跳但非心收縮力,然而,亞丁基隣苯二甲內酯有意義地減少心跳及收縮力。由以上結果及其高的粗治療係數暗示亞丁基隣苯二甲內酯可能是有用的抗心絞痛藥。

並列摘要


Butylidenephthalide, a constituent of Ligusticum wallichii F(subscript RANCH). (Umbelliferae), proved to be the most important and active In antispasmodic ettects. In order to study the influence of the length of alkylidene-group on its anti spasmodic effect, we have synthesized four alkylidenephthalides, ethylidene-, propylidene-, butylidene- and pentylidenephthalide. The present investigation is an attempt to understand the effects of these four on the pituitrin-induced decrease of coronary flow, contractility and heart rate in the isolated guinea pig hearts. Butylidenephthalide, like nitroglycerin but unlike aminophylline, significantly overcame the pituitrin-induced decrease in coronary flow. Aminophylline non-significantly but slightly increased the contractility and heart rate. Nitroglycerin significantly decreased the heart rate but not contractility. Butylidenephthalide, however, significantly decreased both, the heart rate and contractility. Therefore, bulylidenephthalide may decrease more demand of oxygen consumption than nitroglycerin in myocardium of the isolated preparations. The above results suggest that butylidenephthalide may be an useful antianginal drug owing to its high crude therapeutic ratio (Table 1). Recently we also reported the drug inhibited platelet aggregation by inhibition of cyclooxygenase and intereference of calcium mobilization.

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