Copyright © 2010 John Wiley & Sons, Ltd. Biomed. Chromatogr. 2010; 24: 878–886 Research Article Received 4 August 2009, Revised 21 October 2009, Accepted 2 November 2009 Published online in Wiley InterScience: 19 January 2010 (www.interscience.wiley.com) DOI 10.1002/bmc.1380 New protocol to obtain spirolides from Alexandrium ostenfeldii cultures with high recovery and purity Paz Otero a , Amparo Alfonso a , Carmen Alfonso a , Mercedes R. Vieytes b , M. Carmen Louzao a , Ana M. Botana c and Luis M. Botana a * ABSTRACT: The aim of this work was to develop a method to purify large amounts of spirolide toxins from cultures of Alexandrium ostenfeldii. The dinoagellates grew in batches under controlled conditions of salinity, light and temperature. Analysis of the cultures demonstrated the existence of neurotoxins associated with paralytic shellsh poisoning toxins and two spirolides, 13-desmethyl spirolide C and 13,19-didesmethyl spirolide C. The protocol designed presents several stages of extraction, separation between spirolides and paralytic shellsh poisoning toxins, and cleanup in solid-phase extraction. Finally, the purication of spirolides was conducted by a preparative high-performance liquid chromatography system coupled to a mass spectrometer detector. The purity and the amount of both toxins in each step was monitored by analytical liquid chromatographic–mass spectrometry. Large amounts of 13-desMeC, 97% pure, and 13,19-didesMeC, 99% pure, were obtained. A novel and ecient method to separate and purify spirolide toxins from large amounts of phytoplankton is provided. The protocol proposed shows, for the rst time, a complete and detailed methodology to separate and purify spirolide toxins with high purity, recovery, repeatability and stability. Copyright © 2010 John Wiley & Sons, Ltd. Keywords: spirolides; purication, 13-desmethyl spirolide C; 13,19-didesmethyl spirolide C; LC-MS; analytical and preparative methodology * Correspondence to: L. M. Botana, Departamento de Farmacología, Facultad de Veterinaria, Universidad de Santiago de Compostela, 27002 Lugo, Spain. E-mail: luis.botana@usc.es a Departamento de Farmacología, Facultad de Veterinaria, Universidad de Santiago de Compostela, 27002 Lugo, Spain b Departamento de Fisiología, Facultad de Veterinaria, Universidad de Santiago de Compostela, 27002 Lugo, Spain c Departamento de Química Analítica, Facultad de Ciencias, Universidad de Santiago de Compostela, 27002 Lugo, Spain Abbreviations used: dcGTX, decarbamoylgonyautoxins; dcSTX, decarbamoylsaxitoxin; GTX, gonyautoxins; NEO, neosaxitoxin; PSP, paralytic shellsh poisoning; STX, saxitoxin; TFA, triuoroacetic acid. Introduction Spirolides are macrocyclic polyether compounds that belong to the cyclic imine group. This group includes other lipophilic com- pounds such as gymnodimine, pinnatoxins, prorocentrolide, pte- riatoxins and espiro-prorocentrimine (MacKinnon et al., 2004, 2006a, b). Spirolides are the most common cyclical imine toxins due to their widespread global distribution. They were rst iden- tied in extracts of the digestive glands of mussels (Mytilus edulis) and scallops (Placopecten magellanicus) from the Atlantic coast of Nova Scotia, Canada, in 1991 (Meilert and Brimble, 2006). That year, routine toxin monitoring of bivalve molluscs in this location revealed a toxic response in mice after intraperitoneal injections of shellsh extracts. The clinical manifestations included abdomi- nal muscle spasms, piloerection, ataxia, tail whipping and, imme- diately prior to death, neurological symptoms, comprising convulsions and cramps. Chemical investigations demonstrated that the toxicity was due to a new class of toxins which were called spirolides. Spirolide toxins have now been detected in shellsh from a number of other locations around the world. In Europe, these toxins were found in Spain (Villar Gonzalez et al., 2006), Italy (Ciminiello et al., 2006), Scotland (John et al., 2003), Norway (Aasen et al., 2005) and Denmark (MacKinnon et al., 2006b). The dinoagellate identied as the producer of spirolides, in all these coasts, was Alexandrium ostenfeldii. Many studies report this organism to be the main origin of spirolides, although this dino- agellate may produce toxins associated with paralytic shellsh poisoning (PSP). There have been no reports of toxic eects in humans due to ingestion of spirolides. However, general symptoms such as tach- ycardia and gastric distress were reported following contami- nated shellsh consumption from Nova Scotia during the spring and summer of 1991, when spirolides were detected in mollusc from this region (Richard et al., 2001; Sleno and Volmer, 2005). Although the mechanism of action of spirolides in cells are not yet well understood, it has been suggested that the muscarinic acetylcholine receptors might be implicated in its mode of action (Gill et al., 2003). Nuclear magnetic resonance (NMR) and mass spectrometry (MS) methods were used to achieve the structure elucidation of spirolides (Aasen et al., 2005; Ciminiello et al., 2006, 2007; Hu et al., 878