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Mechanisms of Toxicity of 3-Alkylpyridinium Polymers from Marine Sponge Reniera sarai
Department of Biology, Biotechnical Faculty, University of Ljubljana, Večna pot 111, 1000 Ljubljana, Slovenia
Institute of Physiology, Pharmacology and Toxicology, Veterinary Faculty, Gerbičeva 60, University of Ljubljana, Slovenia
* Author to whom correspondence should be addressed.
Received: 16 October 2007; Accepted: 31 October 2007 / Published: 13 November 2007
Abstract: Polymeric 3-alkylpyridinium salts (poly-APS) present in the marine spongeReniera sarai show a broad spectrum of biological activities. They are lytic to erythrocytesand various other mammalian cells, enabling the transfection of the latter with alien DNA.Furthermore, they show inhibitory effects to marine bacteria and can inhibit fouling ofmicro- and macroorganisms to submerged surfaces. Finally, poly-APS act as potentcholinesterase inhibitors. The kinetics of acetylcholinesterase inhibition by poly-APS invitro is complex and comprises several successive phases ending in irreversible inhibitionof the enzyme. The latter is accounted for by aggregation and precipitation of the enzyme-inhibitor complexes. Poly-APS are lethal to rats in concentrations above 2.7 mg/kg.Monitoring of the basic vital functions and histopathological analysis showed that theeffects directly ascribable to acetylcholinesterase inhibition are only observed afterapplication of lower concentrations of poly-APS. At higher concentrations, such effectswere masked by other, more pronounced and faster developing lethal effects of the toxin,such as haemolysis and platelet aggregation.
Keywords: Acetylcholinesterase inhibitor; marine sponge; polymeric alkylpyridinium salts; Reniera sarai; toxicity.
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Turk, T.; Frangež, R.; Sepčić, K. Mechanisms of Toxicity of 3-Alkylpyridinium Polymers from Marine Sponge Reniera sarai. Mar. Drugs 2007, 5, 157-167.
Turk T, Frangež R, Sepčić K. Mechanisms of Toxicity of 3-Alkylpyridinium Polymers from Marine Sponge Reniera sarai. Marine Drugs. 2007; 5(4):157-167.
Turk, Tom; Frangež, Robert; Sepčić, Kristina. 2007. "Mechanisms of Toxicity of 3-Alkylpyridinium Polymers from Marine Sponge Reniera sarai." Mar. Drugs 5, no. 4: 157-167.