PMID- 8051615 OWN - NLM STAT- MEDLINE DCOM- 19940906 LR - 20190710 IS - 0022-3573 (Print) IS - 0022-3573 (Linking) VI - 46 IP - 4 DP - 1994 Apr TI - A novel 11 beta-hydroxysteroid dehydrogenase inhibitor contained in saiboku-to, a herbal remedy for steroid-dependent bronchial asthma. PG - 305-9 AB - To identify the inhibitor of prednisolone metabolism contained in Saiboku-To, we conducted in-vitro experiments of 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD), using rat liver homogenate and cortisol as a typical substrate. We studied the effects of ten herbal constituents on 11 beta-HSD. Five herbal extracts showed inhibitory activity with Glycyrrhiza glabra > Perillae frutescens > Zizyphus vulgaris > Magnolia officinalis > Scutellaria baicalensis. This suggests that unknown 11 beta-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 x 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 11 beta-HSD. FAU - Homma, M AU - Homma M AD - Department of Clinical Pharmacology, Tokyo College of Pharmacy, Japan. FAU - Oka, K AU - Oka K FAU - Niitsuma, T AU - Niitsuma T FAU - Itoh, H AU - Itoh H LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - England TA - J Pharm Pharmacol JT - The Journal of pharmacy and pharmacology JID - 0376363 RN - 0 (Antineoplastic Agents, Phytogenic) RN - 0 (Biphenyl Compounds) RN - 0 (Drugs, Chinese Herbal) RN - 0 (Glucocorticoids) RN - 0 (Immunosuppressive Agents) RN - 0 (Lignans) RN - 0 (saiboku-to) RN - 001E35HGVF (magnolol) RN - 11513CCO0N (honokiol) RN - 6FO62043WK (Glycyrrhizic Acid) RN - EC 1.1.- (Hydroxysteroid Dehydrogenases) RN - EC 1.1.1.146 (11-beta-Hydroxysteroid Dehydrogenases) RN - P540XA09DR (Glycyrrhetinic Acid) RN - V27W9254FZ (Cortisone) RN - WI4X0X7BPJ (Hydrocortisone) SB - IM MH - 11-beta-Hydroxysteroid Dehydrogenases MH - Animals MH - Antineoplastic Agents, Phytogenic/isolation & purification/pharmacology/therapeutic use MH - Asthma/*drug therapy MH - Biphenyl Compounds/isolation & purification/pharmacology/therapeutic use MH - Chromatography, High Pressure Liquid MH - Cortisone/biosynthesis MH - Dose-Response Relationship, Drug MH - Drugs, Chinese Herbal/chemistry/*pharmacology/therapeutic use MH - Glucocorticoids/analysis MH - Glycyrrhetinic Acid/analogs & derivatives/pharmacology MH - Glycyrrhizic Acid MH - Hydrocortisone/metabolism MH - Hydroxysteroid Dehydrogenases/*antagonists & inhibitors MH - Immunosuppressive Agents/chemistry/*pharmacology/therapeutic use MH - *Lignans MH - Liver/*drug effects/enzymology MH - Male MH - *Medicine, Kampo MH - Rats MH - Rats, Wistar EDAT- 1994/04/01 00:00 MHDA- 1994/04/01 00:01 CRDT- 1994/04/01 00:00 PHST- 1994/04/01 00:00 [pubmed] PHST- 1994/04/01 00:01 [medline] PHST- 1994/04/01 00:00 [entrez] AID - 10.1111/j.2042-7158.1994.tb03799.x [doi] PST - ppublish SO - J Pharm Pharmacol. 1994 Apr;46(4):305-9. doi: 10.1111/j.2042-7158.1994.tb03799.x.