80 沖縄産海綿より単離した酵素阻害物質

概要

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In the course of our studies on physiologically active marine natural products, we have examined extracts of various marine organisms for inhibitory activity against pharmacologically important enzymes. As a result, the extracts of several species of the Okinawan marine sponges were found to show potent inhibitory or excitatory effects in the bioassay systems. We followed the activities and obtained the following substances. From the orange sponge Agelas nakamurai Hoshino, agelasidines and agelasines, sesqui- and diterpenes having polar functionalities were isolated. We examined these compounds and the related compounds for inhibitory activity against Na, K-ATPase. Both the hydrophorbic terpenoid part and polar functionalities were important for the activity. New bromotyrosine derivatives, purealin and lipopurealin were obtained from the sponge Psammaplysilla purea. These compounds inhibited enzymic reactions of ATPases. Among them, purealin activated myosin K,EDTA-ATPase and enhanced superprecipitation. Xestoquine, novel pentacyclic quinone was isolated from the sponge Xestospongia sapra with a known quinone, halenaquinone. The compound strongly inhibited Na, K-ATPase and phosphodiesterase, which resulted in cardiotonic activity.
天然有機化合物討論会の論文
1985-09-07