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海绵代谢产物阿吉拉辛 D 及其合成类似物对改进型藤壶的防污活性。

Antifouling activity of the sponge metabolite agelasine D and synthesised analogs on Balanus improvisus.

作者信息

Sjögren Martin, Dahlström Mia, Hedner Erik, Jonsson Per R, Vik Anders, Gundersen Lise-Lotte, Bohlin Lars

机构信息

Division of Pharmacognosy, Department of Medicinal Chemistry, Biomedical Centre, Uppsala University, Uppsala, Sweden.

出版信息

Biofouling. 2008;24(4):251-8. doi: 10.1080/08927010802072753.

Abstract

This study reports a screening study for antifouling (AF) activity of the natural compound agelasine D isolated from marine sponges of the genus Agelas and 20 synthesised analogs of agelasines and agelasimines. Agelasine D, together with two of the analogs, ie AV1003A and AKB695, displayed a strong inhibitory effect on settlement of Balanus improvisus cypris larvae. Agelasine D had an EC50 value of 0.11 microM while the two analogs AV1033A and AKB695 had EC50 values of 0.23 and 0.3 microM, respectively. None of these three compounds affected larval mortality as was the case with several of the analogs tested. Moreover, the effect of AV1033A and AKB695 was reversible. When cyprids after 24 h exposure to the compounds were transferred to fresh seawater, the settlement frequency compared with the controls was completely recovered. The properties of the agelasine D analogs AV1003A and AKB695 make them highly attractive candidates as AF agents in future marine coatings.

摘要

本研究报告了一项针对从艾氏海绵属海洋海绵中分离出的天然化合物艾氏菌素D以及20种艾氏菌素和艾氏胺合成类似物的防污(AF)活性的筛选研究。艾氏菌素D与其中两种类似物AV1003A和AKB695一起,对改进型藤壶无节幼虫的附着表现出强烈的抑制作用。艾氏菌素D的半数有效浓度(EC50)值为0.11微摩尔,而两种类似物AV1033A和AKB695的EC50值分别为0.23和0.3微摩尔。这三种化合物均未影响幼虫死亡率,其他几种受试类似物也是如此。此外,AV1033A和AKB695的作用是可逆的。当无节幼虫在接触这些化合物24小时后转移到新鲜海水中时,与对照组相比,附着频率完全恢复。艾氏菌素D类似物AV1003A和AKB695的特性使其成为未来海洋涂料中极具吸引力的防污剂候选物。

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