A Study on Inhibitors of Chitin Synthase in Marine Organisms

为了开发安全稳定的抗真菌抑制剂，采用80%甲醇提取26种鱼类和贝类的可食部分，并将其分为亲水性和亲脂性两部分，筛选出具有几丁质合成酶抑制活性的组分。同时测定弹性蛋白酶和胶原酶的抑制活性。主要研究结果如下：1.在几丁质合成酶抑制试验中，腹足类和双壳类的亲水性组分表现出活性，对短颈蛤的抑制率为63.6%，对淡水蛤的抑制率为62.5%.在弹性蛋白酶抑制实验中，顶壳和海螺的亲水性组分对弹性蛋白酶的抑制率为100%，牡蛎的抑制率为53.7%.在胶原酶抑制试验中，两种组分均表现出活性，但活性不强，其中亲水组分对箭乌贼的抑制率最高，为59.5%，亲脂组分对南极磷虾的抑制率最高，为65.5%，因此，鱼类和贝类对这些酶活性异常引起的疾病具有一定的干预价值。活性成分的分离和鉴定正在进行中。

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.