Abstract

Biofouling is a widespread phenomenon in oceans worldwide. With increasing human development and activities in open and coastal waters, and due to the environmental impact of AF organotins and copper-based paint, the demand for nontoxic antifouling (AF) paints is increasing. Various bioassays for antimicrobial activity, anti-biofilm formation and anti-barnacle settlement were established to evaluate the possibility of using marine natural products as AF agents. A series of natural products, isolated from the marine-derived fungi Trichoderma atroviride and T. reesei, were evaluated for their AF activity. One pyrone-type compound (1) demonstrated significant inhibitory activities toward barnacle cyprid settlement. Furthermore, a series of pyrone analogues (S1–S6) were synthesized, and their bioactivities were evaluated in the established systems. The results showed that compounds S5 and S6 exhibited a broad spectrum of bioactivities, such as anti-barnacle settlement, anti-biofilm formation and antimicrobial activities.

摘要

生物污损是在全世界海洋中普遍存在的现象。随着人类在开放水域和沿海水域的发展和活动的增加，以及由于AF有机锡和铜基涂料对环境的影响，对无毒防污（AF）涂料的需求正在增加。建立了各种针对微生物活性，抗生物膜形成和藤壶沉降的生物测定方法，以评估将海洋天然产物用作AF制剂的可能性。评估了从海洋真菌木霉阿魏病毒和里氏木霉分离的一系列天然产物的AF活性。一种吡喃酮类化合物（1）对藤壶状塞浦路斯的沉降表现出显着的抑制活性。此外，还有一系列的吡喃酮类似物（合成了S1 – S6），并在已建立的系统中评估了它们的生物活性。结果表明，化合物S5和S6具有广泛的生物活性，例如抗藤壶沉降，抗生物膜形成和抗菌活性。