Reversible anti-settlement activity against Amphibalanus (=Balanus) amphitrite, Bugula neritina, and Hydroides elegans by a nontoxic pharmaceutical compound, mizolastine.
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.
Zhou
Xiaojian
X
College of Environmental Science and Engineering, Yangzhou University, No. 131 Jiangyang Mid Road, Yangzhov, China.
Xu
Ying
Y
Jin
Cuili
C
Qian
Pei-Yuan
PY
D000818:Animals; D001562:Benzimidazoles / Q000494:pharmacology*; D001681:Biological Assay; D002013:Bryozoa / Q000187:drug effects* / Q000254:growth & development; D007814:Larva / Q000187:drug effects / Q000254:growth & development; D008386:Marine Biology; D008826:Microbial Sensitivity Tests; D011077:Polychaeta / Q000187:drug effects* / Q000254:growth & development; D001468:Thoracica / Q000187:drug effects* / Q000254:growth & development
D001562:Benzimidazoles; C076170:mizolastine