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Open AccessArticle

Identification of Marine Neuroactive Molecules in Behaviour-Based Screens in the Larval Zebrafish

Department of Neurology, National Key Clinical Department and Key Discipline of Neurology, Guangdong Key Laboratory for Diagnosis and Treatment of Major Neurological Diseases, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China
School of Chemistry & Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao 999078, China
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Mar. Drugs 2014, 12(6), 3307-3322;
Received: 30 January 2014 / Revised: 19 May 2014 / Accepted: 19 May 2014 / Published: 30 May 2014
(This article belongs to the Special Issue Advances and New Perspectives in Marine Biotechnology)
PDF [1485 KB, uploaded 24 February 2015]


High-throughput behavior-based screen in zebrafish is a powerful approach for the discovery of novel neuroactive small molecules for treatment of nervous system diseases such as epilepsy. To identify neuroactive small molecules, we first screened 36 compounds (136) derived from marine natural products xyloketals and marine isoprenyl phenyl ether obtained from the mangrove fungus. Compound 1 demonstrated the most potent inhibition on the locomotor activity in larval zebrafish. Compounds 3742 were further synthesized and their potential anti-epilepsy action was then examined in a PTZ-induced epilepsy model in zebrafish. Compound 1 and compounds 39, 40 and 41 could significantly attenuate PTZ-induced locomotor hyperactivity and elevation of c-fos mRNA in larval zebrafish. Compound 40 showed the most potent inhibitory action against PTZ-induced hyperactivity. The structure-activity analysis showed that the OH group at 12-position played a critical role and the substituents at the 13-position were well tolerated in the inhibitory activity of xyloketal derivatives. Thus, these derivatives may provide some novel drug candidates for the treatment of epilepsy. View Full-Text
Keywords: behavior-based screen; zebrafish; PTZ; c-fos behavior-based screen; zebrafish; PTZ; c-fos

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Long, S.-M.; Liang, F.-Y.; Wu, Q.; Lu, X.-L.; Yao, X.-L.; Li, S.-C.; Li, J.; Su, H.; Pang, J.-Y.; Pei, Z. Identification of Marine Neuroactive Molecules in Behaviour-Based Screens in the Larval Zebrafish. Mar. Drugs 2014, 12, 3307-3322.

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