Identification and in vitro immunosuppressive activity of a SDZ-IMM-125 metabolite isolated from phenobarbital-induced rabbit liver microsomes

R. DIEDEN Department of Pharmaceutical Sciences, UCL, Pharmacokinetics and Metabolism Unit-FATC, Laboratory of Mass Spectrometry, 7246, Av. E. Mounier, B-1200 Brussels, Belgium OE Experimental Immunology Unit, UCL, Clos Chapelle aux Champs, 3056, B-1200 Brussels, Belgium

R. K. VERBEECK Department of Pharmaceutical Sciences, UCL, Pharmacokinetics and Metabolism Unit-FATC, Laboratory of Mass Spectrometry, 7246, Av. E. Mounier, B-1200 Brussels, Belgium OE Experimental Immunology Unit, UCL, Clos Chapelle aux Champs, 3056, B-1200 Brussels, Belgium

N. MATON Department of Pharmaceutical Sciences, UCL, Pharmacokinetics and Metabolism Unit-FATC, Laboratory of Mass Spectrometry, 7246, Av. E. Mounier, B-1200 Brussels, Belgium OE Experimental Immunology Unit, UCL, Clos Chapelle aux Champs, 3056, B-1200 Brussels, Belgium

D. LATINNE Department of Pharmaceutical Sciences, UCL, Pharmacokinetics and Metabolism Unit-FATC, Laboratory of Mass Spectrometry, 7246, Av. E. Mounier, B-1200 Brussels, Belgium OE Experimental Immunology Unit, UCL, Clos Chapelle aux Champs, 3056, B-1200 Brussels, Belgium

G. J. J. LHOEST* Department of Pharmaceutical Sciences, UCL, Pharmacokinetics and Metabolism Unit-FATC, Laboratory of Mass Spectrometry, 7246, Av. E. Mounier, B-1200 Brussels, Belgium OE Experimental Immunology Unit, UCL, Clos Chapelle aux Champs, 3056, B-1200 Brussels, Belgium

Abstract

1. A metabolite of D-serine-cyclosporine A has been isolated from phenobarbital induced rabbit liver microsomes using hplc. 2. This metabolite was identified by FAB, electrospray mass spectrometry as well as nmr spectroscopy and is the result of metabolism of the vinylic methyl group of the 9- carbon amino acid unique to the cyclosporins, the first amino acid of this cyclic undecapeptide. This metabolite exhibits a significantly lower immunosuppressive activity than IMM-125 and CsA.

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Identification and in vitro immunosuppressive activity of a SDZ-IMM-125 metabolite isolated from phenobarbital-induced rabbit liver microsomes

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Identification and in vitro immunosuppressive activity of a SDZ-IMM-125 metabolite isolated from phenobarbital-induced rabbit liver microsomes

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