In vitro immunosuppressive activity of tacrolimus dihydrodiol precursors obtained by chemical oxidation and identification of a new metabolite of SDZ-RAD by electrospray and electrospray-linked scan mass spectrometry |
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Authors: | Lhoëst G Hertsens R Verbeeck R K Maton N Wallemacq P Dehoux J P Latinne D |
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Institution: | Department of Pharmaceutical Sciences, UCL, Pharmacokinetics and Drug Metabolism Unit (PMNT), Laboratory of Mass Spectrometry, 7246 Av. E. Mounier, B-1200 Brussels, Belgium. lhoest@pmnt.ucl.ac.be |
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Abstract: | Different tacrolimus epoxides and dihydrodiol epoxides arising from the chemical oxidation of the parent drug are described. Open-chain tautomeric forms involving the lactone function were identified for the tacrolimus epoxides. Moreover, the identification by electrospray and electrospray linked scan mass spectrometry of an SDZ-RAD C16-C27 O-demethyl 17, 18-19, 20-21, 22 tris-epoxide new metabolite isolated from pig liver microsomes is reported. The in vitro immunosuppressive activity, using mixed lymphocyte reactions of the two macrolide reported oxidation compounds are discussed. |
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