College of Environmental Science and Engineering, Yangzhou University, No. 131 Jiangyang Mid Road, Yangzhov, China.
Biofouling. 2009 Nov;25(8):739-47. doi: 10.1080/08927010903154724.
Mizolastine, an antihistamine pharmaceutical, was found to significantly inhibit larval settlement of the barnacle Amphibalanus (=Balanus) amphitrite, the bryozoan Bugula neritina, and the polychaete Hydroides elegans with EC(50) values of 4.2, 11.2, and 4.1 microg ml(-1), respectively. No toxicity against the larvae of these three species was observed at the concentration range tested during incubations with mizolastine. To determine whether the anti-settlement activity of mizolastine is reversible, recovery bioassays using these three species were conducted. More than 70% of the larvae that had been exposed for 4 h to mizolastine at concentrations four-fold greater than their respective EC(50) values completed normal metamorphosis. The results of the recovery bioassay provide evidence that the anti-settlement effect of mizolastine is reversible in addition to being nontoxic. The anti-settlement activities of several intermediates of the synthesis process of mizolastine were also examined. One of the intermediates, 2-chloro-1-(4-fluorobenzyl)-1H-benzo[d]imidazole, inhibited larval settlement and metamorphosis with low toxicity. These results may improve the understanding of the key functional group responsible for the anti-settlement activity of mizolastine.
咪挫斯汀，一种抗组胺类药物，被发现能显著抑制藤壶（= 藤壶） Amphibalanus (=Balanus) amphitrite、苔藓虫 Bugula neritina 和多毛类 Hydroides elegans 的幼虫附着，EC(50) 值分别为 4.2、11.2 和 4.1μg ml(-1)。在与咪挫斯汀孵育的测试浓度范围内，对这三种幼虫均未观察到毒性。为了确定咪挫斯汀的抗附着活性是否可逆，对这三种幼虫进行了恢复生物测定。暴露于咪挫斯汀浓度是其各自 EC(50) 值的四倍达 4 小时的幼虫中，有超过 70%的幼虫完成了正常变态。恢复生物测定的结果表明，除了无毒之外，咪挫斯汀的抗附着作用也是可逆的。还检查了咪挫斯汀合成过程中的几个中间体的抗附着活性。其中一个中间体，2-氯-1-(4-氟苄基)-1H-苯并[d]咪唑，具有低毒性，能抑制幼虫附着和变态。这些结果可能有助于更好地了解咪挫斯汀抗附着活性的关键功能基团。
