A Study on Inhibitors of Chitin Synthase in Marine Organisms

为了开发安全、稳定的抗真菌感染的抑制剂，用80%甲醇提取了26种鱼和贝类的可食部分，并将其分成亲水组分和亲脂组分，对其几丁质合成酶抑制活性进行了筛选。同时测定了弹性蛋白酶和胶原酶的抑制活性。研究结果如下：1.在甲壳素合成酶抑制实验中，腹足类和双壳类亲水组分具有一定的抑制率，对文蛤的抑制率为63.6%，对淡水对虾的抑制率为62.5%。在弹性酶抑制实验中，顶壳和螺体的亲水性部分显示出100%的抑制率，其次是牡蛎的53.7%。在胶原酶抑制实验中，两种组分均表现出较强的抑制活性，其中亲水性组分对箭鱼的抑制率最高达59.5%，对南极磷虾的抑制率最高达65.5%，因此，鱼和贝类对这两种酶活性异常引起的疾病的干预具有一定的价值。主动原则(S)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.