Abstract
Tritium-labelled dihydro derivatives of the cyanobacterial peptide hepatotoxin nodularin were prepared by reduction with sodium boro[3H]hydride. The optimised reaction gave two dihydronodularin stereoisomers which were purified by high-performance liquid chromatography with a mobile phase of methanol-0.7% sodium sulfate (6:4) and a C(18) stationary phase. The specific activities of the stereoisomers were 1780-1807 dis min(-1) ng(-1). The radiolabelled dihydronodularins were tested for stability and used for toxicokinetic studies in mice. Liver was the main site of toxin accumulation.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Chemical and Drug Induced Liver Injury / etiology
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Chemical and Drug Induced Liver Injury / metabolism
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Chromatography, High Pressure Liquid
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Cyanobacteria Toxins
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Cyanobacteria*
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Female
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Isotope Labeling
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Liver / drug effects
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Liver / metabolism
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Marine Toxins / chemical synthesis*
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Marine Toxins / pharmacokinetics
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Marine Toxins / toxicity
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Mice
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Mice, Inbred BALB C
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Peptides, Cyclic / chemical synthesis*
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Peptides, Cyclic / chemistry*
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Peptides, Cyclic / pharmacokinetics
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Peptides, Cyclic / toxicity
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Stereoisomerism
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Tritium / chemistry
Substances
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Cyanobacteria Toxins
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Marine Toxins
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Peptides, Cyclic
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nodularin
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Tritium
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dihydronodularin