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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

✍ Scribed by G. Lhoëst; R. Hertsens; R. K. Verbeeck; N. Maton; P. Wallemacq; J. P. Dehoux; D. Latinne

Publisher: John Wiley and Sons
Year: 2001
Tongue: English
Weight: 305 KB
Volume: 36
Category: Article
ISSN: 1076-5174
DOI: 10.1002/jms.190

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✦ Synopsis

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 C~16~–C~27~ 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. Copyright © 2001 John Wiley & Sons, Ltd.

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