Catechol Conjugates Are In Vivo Metabolites of Salicis
                    cortex

Susanne Knuth; Rania M. Abdelsalam; Mohamed T. Khayyal; Frank Schweda; Jörg Heilmann; Martin Georg Kees; Georg Mair; Frieder Kees; Guido Jürgenliemk

doi:10.1055/s-0033-1350898

Planta Medica, Table of Contents

Planta Med 2013; 79(16): 1489-1494
DOI: 10.1055/s-0033-1350898

Rapid Communications

Georg Thieme Verlag KG Stuttgart · New York

Catechol Conjugates Are In Vivo Metabolites of Salicis cortex

Authors

Susanne Knuth

¹University of Regensburg, Institute of Pharmacy, Department of Pharmaceutical Biology, Regensburg, Germany
Rania M. Abdelsalam

²Cairo University, Faculty of Pharmacy, Department of Pharmacology, Cairo, Egypt
Mohamed T. Khayyal

²Cairo University, Faculty of Pharmacy, Department of Pharmacology, Cairo, Egypt
Frank Schweda

³University of Regensburg, Institute of Physiology, Regensburg, Germany
Jörg Heilmann

¹University of Regensburg, Institute of Pharmacy, Department of Pharmaceutical Biology, Regensburg, Germany
Martin Georg Kees

⁴Charité University Hospital, Campus Benjamin Franklin, Department of Anesthesiology and Intensive Care, Berlin, Germany

⁵Freie Universität Berlin, Institute of Pharmacy, Department of Clinical Pharmacy and Biochemistry, Berlin, Germany
Georg Mair

⁶Intensive Care Unit, Bezirksklinikum Regensburg, Regensburg, Germany
Frieder Kees

⁷University of Regensburg, Institute of Pharmacy, Department of Pharmacology and Toxicology, Regensburg, Germany
Guido Jürgenliemk

¹University of Regensburg, Institute of Pharmacy, Department of Pharmaceutical Biology, Regensburg, Germany

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 c_max (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

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References

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