Disposition of sanguinarine in the rat

Sanguinarine is an alkaloid with known antibiotic and anti-inflammatory activity and its pharmacokinetics have been studied in the rat after a single oral dose (10 mg kg−1 body weight). Alkaloid determination in the plasma and liver was carried out by high-performance liquid chromatography-electrosp...

Full description

Saved in:
Bibliographic Details
Published in:Xenobiotica 2007-05, Vol.37 (5), p.549-558
Main Authors: Ve e a, R., Klejdus, B., Kosina, P., Orolin, J., Stiborová, M., Smr ek, S., Vi ar, J., Dvo ák, Z., Ulrichová, J., Kubá, V., Anzenbacher, P., Šimánek, V.
Format: Article
Language:English
Subjects:
Acridines - chemistry
Administration, Oral
Alkaloids - administration & dosage
Alkaloids - blood
Alkaloids - chemistry
Alkaloids - pharmacokinetics
Animals
Anti-Infective Agents - administration & dosage
Anti-Infective Agents - blood
Anti-Infective Agents - chemistry
Anti-Infective Agents - pharmacokinetics
Benzophenanthridines - administration & dosage
Benzophenanthridines - blood
Benzophenanthridines - chemistry
Benzophenanthridines - pharmacokinetics
biodistribution
dihydrosanguinarine
Isoquinolines - administration & dosage
Isoquinolines - blood
Isoquinolines - chemistry
Isoquinolines - pharmacokinetics
Male
Mass Spectrometry
pharmacokinetics
Rats
Rats, Wistar
Sanguinarine
Time Factors
Tissue Distribution
Tritium
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Sanguinarine is an alkaloid with known antibiotic and anti-inflammatory activity and its pharmacokinetics have been studied in the rat after a single oral dose (10 mg kg−1 body weight). Alkaloid determination in the plasma and liver was carried out by high-performance liquid chromatography-electrospray ionization mass spectrometry (HPLC/ESI-MS). The pharmacokinetic parameters (tmax, cmax, AUC0→t and AUC0→∞) were determined for sanguinarine and dihydrosanguinarine, the major components detected in plasma. The first step in sanguinarine metabolism in the rat was the reduction of the iminium bond resulting in formation of the less toxic dihydrosanguinarine. Both compounds were completely eliminated from the plasma and liver after 24 h and not detected in urine. After a single oral dose of 3H-sanguinarine, more than 42% of the ingested radioactivity was present in gastrointestinal tract. Benz[c]acridine, up to date the only sanguinarine metabolite referred to in the literature, was not detected in the plasma, liver or urine.
ISSN:0049-8254
1366-5928
DOI:10.1080/00498250701230542