Metabolism and excretion of methylproscillaridin by man.
0.5 mg 3H-proscillaridin-4-methylether was administered orally to 5 healthy males. Maximum plasma levels of total radioactivity were reached after one to two hours. In two subjects a second peak was observed between 6 and 12 hours. The plasma half life of total radioactivity was 51 hours. 20% and 56% respectively of the dose were eliminated in urine and faeces during the following 7 days. 55% of the total radioactivity in plasma, 80% in urine and 20% in faeces consisted of CHC13-insoluble compounds. 50-60% of the latter in plasma and urine could be hydrolysed by beta-glucuronidase. More than 90% of the split products were identified as conjugates of methylproscillaridin. TLC-separation of the CHC13-soluble fractions of plasma and urine yielded two unidentified metabolites, P2 and P3, as the main compounds, besides methylproscillaridin, proscillaridin and scillarenin. In faeces more than 90% of the non-polar fraction was identified as methylproscillaridin. Shortly after administration of 3H-methylproscillaridin, the radioactivity in plasma consisted mainly of CHC13-insoluble conjugates and of the metabolite P2.
D000328:Adult; D002018:Bufanolides / Q000031:analogs & derivatives*; D002855:Chromatography, Thin Layer; D005965:Glucuronates / Q000096:biosynthesis; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D008297:Male; D011442:Proscillaridin / Q000031:analogs & derivatives* / Q000378:metabolism
D002018:Bufanolides; D005965:Glucuronates; D011442:Proscillaridin