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

Lhoest, Georges;Hertsens, R.;Verbeeck, Roger-K.;Maton, Nicole;Latinne, Dominique;et.al.
(2001) Journal of Mass Spectrometry — Vol. 36, n° 8, p. 889-901 (2001)

Files

26226.pdf
  • Restricted Access
  • Adobe PDF
  • 761.49 KB
Request a copy

Details

Authors
  • Lhoest, GeorgesUCLouvain
    Author
  • Hertsens, R.UCLouvain
    Author
  • Verbeeck, Roger-K.orcid-logoUCLouvain
    Author
  • Maton, NicoleUCLouvain
    Author
  • Wallemacq, PierreUCLouvain
    Author
  • Dehoux, Jean-PaulUCLouvain
    Author
  • Latinne, DominiqueUCLouvain
    Author
Show more
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.
Affiliations

Citations

  • APA
  • Chicago
  • FWB

Lhoest, G., Hertsens, R., Verbeeck, R.-K., Maton, N., Wallemacq, P., Dehoux, J.-P., & Latinne, D. (2001). 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. Journal of Mass Spectrometry, 36(8), 889-901. https://doi.org/10.1002/jms.190 (Original work published 2001)