A Study on Inhibitors of Chitin Synthase in Marine Organisms

为了开发安全稳定的真菌感染抑制剂，以80%的MeOH提取26种鱼类和贝类的可食用部位，并将其分成亲水和亲脂两部分，筛选其几丁质合成酶抑制活性。同时测定了弹性酶和胶原酶的抑制活性。得到的结果如下：1。在甲壳素合成酶抑制实验中，腹足类和双壳类亲水性组分均有活性，其中短颈蛤和淡水蛤的抑制率分别为63.6%和62.5%。在弹性酶抑制实验中，顶壳和海螺亲水性组分的抑制率为100%，牡蛎亲水性组分的抑制率为53.7%。在胶原酶抑制实验中，亲水性部分对箭鱿鱼的抑制率最高，为59.5%，亲脂性部分对南极磷虾的抑制率最高，为65.5%。因此，鱼类和贝类对干预由这些酶的异常活动引起的疾病具有一定的价值。隔离和识别活动原理正在进行中。

In order to develop safe and stable inhibitors against fungal infection, edible parts of 26 species of fish and shellfish were extracted with 80% MeOH and partitioned into hydrophilic and lipophilic fractions, for which chitin synthase inhibitory activities were screened. Inhibitory activities of elastase and collagenase were also assayed. The results obtained are as follows:1. In the chitin synthase inhibitory assay, the hydrophilic fractions of gastropods and bivalves showed activities, with the inhibition level of 63.6% in short-neck clam and 62.5% in freshwater clam.2. In the elastase inhibitory assay, the hydrophilic fractions of top shell and whelk showed 100% inhibition, followed by 53.7% in oyster.3. In the collagenase inhibitory assay, both fractions showed activities, though not so potent, the highest inhibition of the hydrophilic fractions being 59.5% in arrow squid and that of lipophilic fractions 65.5% in Antarctic krill.Therefore, fish and shellfish can be of some value for the intervention of diseases resulting from aberrant activities of these enzymes. The isolation and identification of the active principle(s) are in progress.