May 1, 1977

Cardenolide analogues. VI. The metabolism of the prodrug diacetylcymarol in the rat

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
J Boutagy, R Thomas


1. Diacetylcymarol is an acetylated glycoside which is better absorbed than the parent glycoside, cymarol. 2. Diacetyl[19-3H]cymarol was rapidly metabolized and excreted by the rat following intraperitoneal administration. 3. The drug was metabolized extensively to polar compounds with the principal pathway involving loss of the C-19 acetyl group and probable demethylation of the sugar. 4. The bulk of the radioactive material was excreted in the bile and there was little reabsorption. 5. The results show that acetylation was successful in converting the poorly absorbed glycoside, cymarol, into a derivative that was rapidly absorbed from the peritoneal cavity. 6. Following or during absorption, the biologically inactive diacetylcymarol was converted to polar derivatives with potential therapeutic activity. However, subsequent elimination was so rapid that little therapeutic benefit could be expected.

  • References2
  • Citations


  • References2
  • Citations


  • This paper may not have been cited yet.

Mentioned in this Paper

Metabolic Process, Cellular
Biochemical Pathway
Cardiac Glycosides
Entire Peritoneal Cavity

About this Paper

Related Feeds

Cardiac Glycosides

Cardiac glycosides are a diverse family of naturally derived compounds that bind to and inhibit na+/k+-atpase. Discover the latest research on cardiac glycosides heres.