Synthesis, organotropism and hepatocellular uptake of two tritium-labeled epimers of dihydromicrocystin-LR, a cyanobacterial peptide toxin analog

A1 Journal article (refereed)

Internal Authors/Editors

Publication Details

List of Authors: Meriluoto, Nygård, Dahlem, Eriksson
Publication year: 1990
Journal: Toxicon
Journal acronym: Toxicon
Volume number: 28
Issue number: 12
Start page: 1439
End page: 1446
ISSN: 0041-0101
eISSN: 1879-3150


Two tritium-labeled epimers of dihydromicrocystin-LR, a derivative of the cyanobacterial peptide hepatotoxin microcystin-LR, were synthesized by reduction with sodium boro[3H]hydride and purified with reversed-phase liquid chromatography. The epimers were hepatotoxic in mice; the i.p. LD50 was 120-135 micrograms/kg. They were concentrated in the liver and to some extent in the intestine and the kidney after an i.v. injection. Freshly isolated rat hepatocytes showed a rapid uptake of both epimers. The cellular uptake of the epimers was almost complete within 5 min at concentrations 1 microM (0.5 microM dihydromicrocystin-LR + 0.5 microM microcystin-LR) and 4 microM (0.5 microM + 3.5 microM). The uptake of the earlier eluting epimer was about three times higher than that of the later eluting epimer.

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