強心性植物成分の研究(第8報)強心配糖体Proscillaridinの硝酸エステル体の合成とその薬理作用

概要

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To reduce the vascular contracting effect of the cardiac glycoside, proscillaridin (1), all kinds of its nitrates were prepared by utilizing effectively an isopropylidene function as a protective group. The pharmacological activities of proscillaridin nitrates were evaluated by the use of isolated guinea-pig papillary muscle preparations and Na^+, K^+-adenosine triphosphatase preparations from the dog kidney. Furthermore, the effect for smooth muscle using the helical strips isolated from 13-week old spontaneously hypertensive rat was examined. The positive inotropic effects and Na^+, K^+-adenosine triphosphatase inhibition activities of mononitrates (6,9,15) and dinitrates (3,4,5) were a little less potent than 1,but those of trinitrate (2) were much reduced. Every nitrate did not exhibited a vascular contracting effect but a relaxing effect. Among them, the vascular relaxing effects of 2', 3'-dinitrate (3) and 2', 4'-dinitrate (4) were more potent than those of the other nitrates.
社団法人日本薬学会の論文
1991-08-25