Excretion of methylproscillaridin in patients with a biliary fistula.
Four patients with a biliary fistula received 0.5 mg 3H-methylproscillaridin as a single oral dose. 55% of the dose was excreted in bile, 16% in urine and 3% in faeces. More than 60% of the radioactivity excreted in bile and urine appeared within the first 24 hours. 78% of the radioactivity in bile consisted of CHCl3-insoluble metabolites of methylproscillaridin, incubation of which with beta-glucuronidase led to splitting off glucuronic acid from almost 80%. Methylproscillaridin can be regarded as the principal conjugated compound. TLC-separation of CHCl3-soluble compounds from bile showed identical running of radioactivity with methylproscillaridin, proscillaridin and scillarenin and three unknown metabolites P1, P2, and P3. In urine the CHCl3-soluble fraction averaged 16% to 34% of the total amount and was identified as methylproscillaridin, proscillaridin, scillarenin, P2 and P3. The relative composition of the total radioactivity in faeces amounted to 77% methylproscillardidin, 4% scillarenin and 12% polar metabolites.
D000368:Aged; D001646:Bile / Q000378:metabolism; D001652:Bile Ducts; D002018:Bufanolides / Q000378:metabolism*; D002404:Catheterization; D002855:Chromatography, Thin Layer; D005243:Feces / Q000032:analysis; D005260:Female; D005965:Glucuronates / Q000096:biosynthesis; D006801:Humans; D008297:Male; D008875:Middle Aged; D011442:Proscillaridin / Q000031:analogs & derivatives / Q000378:metabolism*; D013997:Time Factors
D002018:Bufanolides; D005965:Glucuronates; D011442:Proscillaridin