Synthesis, organotropism and hepatocellular uptake of two tritium-labeled epimers of dihydromicrocystin-LR, a cyanobacterial peptide toxin analog.
Toxicon
; 28(12): 1439-46, 1990.
Article
em En
| MEDLINE
| ID: mdl-2128565
ABSTRACT
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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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeos Cíclicos
/
Fígado
/
Toxinas Marinhas
Limite:
Animals
Idioma:
En
Revista:
Toxicon
Ano de publicação:
1990
Tipo de documento:
Article
País de afiliação:
Finlândia