A Novel 11β-Hydroxysteroid Dehydrogenase Inhibitor Contained in Saiboku-To, a Herbal Remedy for Steroid-dependent Bronchial Asthma
- 12 April 1994
- journal article
- Published by Oxford University Press (OUP) in Journal of Pharmacy and Pharmacology
- Vol. 46 (4), 305-309
- https://doi.org/10.1111/j.2042-7158.1994.tb03799.x
Abstract
To identify the inhibitor of prednisolone metabolism contained in Saiboku-To, we conducted in-vitro experiments of 11β-hydroxysteroid dehydrogenase (11β-HSD), using rat liver homogenate and Cortisol as a typical substrate. We studied the effects often herbal constituents on 11β-HSD. Five herbal extracts showed inhibitory activity with Glycyrrhiza glabra > Perillae frutescens< Zizyphus vulgaris > Magnolia officinalis > Scutellaria baicalensis. This suggests that unknown 11β-HSD inhibitors are contained in four herbs other than G. glabra which contains a known inhibitor, glycyrrhizin (and glycyrrhetinic acid). Seven chemical constituents which have been identified as the major urinary products of Saiboku-To in healthy and asthmatic subjects were studied; magnolol derived from M. officinalis showed the most potent inhibition of the enzyme (IC50, 1·8 × 10−4 m). Although this activity was less than that of glycyrrhizin, the inhibition mechanism (non-competitive) was different from a known competitive mechanism. These results suggest that magnolol might contribute to the inhibitory effects of Saiboku-To on prednisolone metabolism through inhibition of 11β-HSD.Keywords
Funding Information
- Ministry of Education in Japan (03857345)
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