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Phytomedicine ; 9(7): 654-8, 2002 Oct.
Article de Anglais | MEDLINE | ID: mdl-12487331

RÉSUMÉ

The orcinol derivatives tenuiorin (1) and methyl orsellinate (2) were identified as active components of an extract from the lichen Peltigera leucophlebia (Nyl.) Gyeln. showing in vitro inhibitory activity against 15-lipoxygenase from soybeans. The compounds were subsequently tested for in vitro activity against 5-lipoxygenase from porcine leucocytes and proved to be moderately active, with IC50 values of 41.6 microM and 59.6 microM respectively. Tenuiorin is a known constituent of several Peltigera species but has not previously been isolated from P. leucophlebia. As correlation between 5-lipoxygenase inhibition and antiproliferative effects has earlier been witnessed for related lichen metabolites, tenuiorin and methyl orsellinate were further tested for antiproliferative activity on cultured human breast (T-47D)-, pancreatic (PANC-1)- and colon (WIDR) cancer cell lines. The monomeric methyl orsellinate exhibited no detectable antiproliferative activity whereas the trimeric tenuiorin caused moderate/weak reduction in [3H]-thymidine uptake of the pancreatic- and colon cancer cells, with ED50 values of 87.9 and 98.3 microM respectively.


Sujet(s)
Extrait cellulaire/pharmacologie , Lichens , Inhibiteurs de la lipoxygénase , Résorcinol/pharmacologie , Tumeurs du sein/traitement médicamenteux , Division cellulaire/effets des médicaments et des substances chimiques , Humains , Concentration inhibitrice 50 , Spectroscopie par résonance magnétique , Résorcinol/composition chimique , Résorcinol/isolement et purification , Thymidine/métabolisme , Tritium , Cellules cancéreuses en culture/effets des médicaments et des substances chimiques
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