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Planta Med 2013; 79(16): 1489-1494
DOI: 10.1055/s-0033-1350898
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Georg Thieme Verlag KG Stuttgart · New York

Catechol Conjugates Are In Vivo Metabolites of Salicis cortex

Susanne Knuth
1   University of Regensburg, Institute of Pharmacy, Department of Pharmaceutical Biology, Regensburg, Germany
,
Rania M. Abdelsalam
2   Cairo University, Faculty of Pharmacy, Department of Pharmacology, Cairo, Egypt
,
Mohamed T. Khayyal
2   Cairo University, Faculty of Pharmacy, Department of Pharmacology, Cairo, Egypt
,
Frank Schweda
3   University of Regensburg, Institute of Physiology, Regensburg, Germany
,
Jörg Heilmann
1   University of Regensburg, Institute of Pharmacy, Department of Pharmaceutical Biology, Regensburg, Germany
,
Martin Georg Kees
4   Charité University Hospital, Campus Benjamin Franklin, Department of Anesthesiology and Intensive Care, Berlin, Germany
5   Freie Universität Berlin, Institute of Pharmacy, Department of Clinical Pharmacy and Biochemistry, Berlin, Germany
,
Georg Mair
6   Intensive Care Unit, Bezirksklinikum Regensburg, Regensburg, Germany
,
Frieder Kees
7   University of Regensburg, Institute of Pharmacy, Department of Pharmacology and Toxicology, Regensburg, Germany
,
Guido Jürgenliemk
1   University of Regensburg, Institute of Pharmacy, Department of Pharmaceutical Biology, Regensburg, Germany
› Author Affiliations
Further Information

Publication History

received 22 April 2013
revised 22 August 2013

accepted 27 August 2013

Publication Date:
21 October 2013 (online)

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Abstract

After oral administration of 100 mg/kg b. w. (235.8 µmol/kg) salicortin to Wistar rats, peak serum concentrations of 1.43 mg/L (13.0 µM) catechol were detected after 0.5 h in addition to salicylic acid by HPLC-DAD after serum processing with β-glucuronidase and sulphatase. Both metabolites could also be detected in the serum of healthy volunteers following oral administration of a willow bark extract (Salicis cortex, Salix spec., Salicaceae) corresponding to 240 mg of salicin after processing with both enzymes. In humans, the cmax (1.46 mg/L, 13.3 µM) of catechol was reached after 1.2 h. The predominant phase-II metabolite in humans and rats was catechol sulphate, determined by HPLC analysis of serum samples processed with only one kind of enzyme. Without serum processing with glucuronidase and sulphatase, no unconjugated catechol could be detected in human and animal serum samples. As catechol is described as an anti-inflammatory compound, these results may contribute to the elucidation of the mechanism of the action of willow bark extract.

Key words

Salix - Salicaceae - catechol - salicortin - metabolism - conjugates - salicylic acid - pharmacokinetic study - in vivo

Supporting Information

 

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