Pharmacokinetic of 3H-deacetylasperulosidic acid in mice

Johannes Westendorf, Simla Basar-Maurer, Thomas Hackl, Edzard Schwedhelm


Background: An investigation was conducted to determine the fate of the iridoid derivative deacetylasperulosidic acid (DAA) after oral application to mice.

Methods: DAA was extracted from Morinda citrifolia leaf and purified by preparative HPLC. The identity was verified by MS and NMR spectroscopy. A sample of DAA was radioactively labelled with tritium and applied to mice by gavage. The pharmacokinetic of the radioactivity was investigated in blood, organs, urine and feces. Metabolites were isolated in blood and urine by HPLC and identified by LC-MS.  In vitro incubation of DAA with mouse duodenum and liver homogenate and human fecal bacteria was performed and possible metabolites were separated with HPLC.

Results: DAA was rapidly absorbed and excreted mainly via the kidneys with a half-life of 30 minutes. Radioactivity was present in all organs with highest concentrations in kidney and liver.  Almost 100% of the radioactivity isolated from urine and organs could be identified as unchanged DAA. Additionally, no metabolism could be observed after in vitro incubation of DAA with mouse small intestine or liver homogenate, however, a total breakdown of the molecule was observed after incubation of DAA with human intestinal bacteria.

Conclusions:The absorption and excretion of glycosides such as DAA in mammals without hydrolysis is possibly a defense mechanism of animals against the toxicity of these compounds. 

Key words: Deacetylasperulosidic acid, DAA, tritium label, pharmacokinetic,iridoid, metabolism

Full Text: [Abstract] [Full Article]

DOI: 10.31989/ffhd.v6i8.261


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