15-Desmethyl FK-506 and 15,31-desmethyl FK-506 from human liver microsomes: isolation, identification (by fast atom bombardment mass spectrometry and NMR), and evaluation of in vitro immunosuppressive activity.

Lhöest, G J;Verbeeck, R K;Maton, Nicole;Latinne, Dominique;Laurent, André
(1994) Clinical Chemistry : international journal of molecular diagnostics and laboratory medicine — Vol. 40, n° 5, p. 740-744 (1994)

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  • Lhöest, G J
    Author
  • Verbeeck, R K
    Author
  • Maton, NicoleUCLouvain
    Author
  • Latinne, DominiqueUCLouvain
    Author
  • Laurent, AndréUCLouvain
    Author
Abstract
15-Desmethyl FK-506 and 15,31-desmethyl FK-506 metabolites extracted from incubated human liver microsomes were separated by normal and reversed-phase HPLC. The metabolites were identified by fast atom bombardment/mass spectrometry and nuclear magnetic resonance spectroscopy. The in vitro 50% inhibitory concentration, tested against bidirectional mixed lymphocyte reactions, was 325 mg/L for 15,31-desmethyl FK-506 and 4 mg/L for 15-desmethyl FK-506, indicating that these products of FK-506 demethylation retain in vitro immunosuppressive activity.
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Lhöest, G. J., Verbeeck, R. K., Maton, N., Latinne, D., & Laurent, A. (1994). 15-Desmethyl FK-506 and 15,31-desmethyl FK-506 from human liver microsomes: isolation, identification (by fast atom bombardment mass spectrometry and NMR), and evaluation of in vitro immunosuppressive activity. Clinical Chemistry : international journal of molecular diagnostics and laboratory medicine, 40(5), 740-744. https://hdl.handle.net/2078.5/129431 (Original work published 1994)