title: The use of deuterium-labeled cortisol for in vivo evaluation of renal 11beta-HSD activity in man: urinary excretion of cortisol, cortisone and their A-ring reduced metabolites.
abstract: This study describes a new approach using stable isotope methodology in evaluating 11beta-HSD activities in vivo based on urinary excretion of cortisol, cortisone, and their A-ring reduced metabolites. The method involved the measurement of deuterium-labeled cortisol and its deuterium-labeled metabolites by GC/MS simultaneously with endogenous cortisol, cortisone, and their A-ring reduced metabolites after oral administration of deuterium-labeled cortisol to normal human subjects. This stable isotope approach offered unique advantages in assessing the appropriateness of measuring unconjugated and total (unconjugated + conjugated) cortisol, cortisone, and their A-ring reduced metabolites in urine as indices of renal 11beta-HSD2 activity in man. Our results strongly support that the measurement of urinary unconjugated cortisol and cortisone is a significant advance in assessing 11beta-HSD2 activity.
authors.affiliation: Department of Medicinal Chemistry and Clinical Pharmacy, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Hachioji, Tokyo, Japan. kasuyay@ps.toyaku.ac.jp
authors.forename: Y
authors.initials: Y
authors.lastname: Kasuya
authors.forename: H
authors.initials: H
authors.lastname: Shibasaki
authors.forename: T
authors.initials: T
authors.lastname: Furuta
mesh_terms: D042842:11-beta-Hydroxysteroid Dehydrogenases; D000328:Adult; D003348:Cortisone / Q000378:metabolism / Q000652:urine; D003903:Deuterium / Q000008:administration & dosage / Q000378:metabolism; D006801:Humans; D006854:Hydrocortisone / Q000008:administration & dosage / Q000378:metabolism; D006913:Hydroxysteroid Dehydrogenases / Q000378:metabolism*; D007668:Kidney / Q000201:enzymology* / Q000378:metabolism; D008297:Male; D013058:Mass Spectrometry; D013760:Tetrahydrocortisol / Q000378:metabolism / Q000652:urine; D013761:Tetrahydrocortisone / Q000378:metabolism / Q000652:urine; D013997:Time Factors
chemical_list: D013761:Tetrahydrocortisone; D013760:Tetrahydrocortisol; D003903:Deuterium; D006913:Hydroxysteroid Dehydrogenases; D042842:11-beta-Hydroxysteroid Dehydrogenases; D003348:Cortisone; D006854:Hydrocortisone