The Isolation, Structural Characterization, and Immunosuppressive Activity of Cyclosporin G (NVa2-Cyclosporine) Metabolites
- 1 July 1991
- journal article
- research article
- Published by Wolters Kluwer Health in Therapeutic Drug Monitoring
- Vol. 13 (4) , 281-288
- https://doi.org/10.1097/00007691-199107000-00001
Abstract
Seven cyclosporin G metabolites were isolated by high-performance liquid chromatography from the urine of normal subjects receiving the drug. The structure and purity of the metabolites were assessed by fast atom bombardment/mass spectroscopy, by proton nuclear magnetic resonance (NMR), and by 13C-NMR. The structural modifications of the cyclosporin G metabolites consisted primarily of hydroxylation and demethylation, as is the case for cyclosporin A metabolites. The immunosuppressive activities of the metabolites were tested in three separate in vitro systems: a primary and secondary mixed lymphocyte system, as well as a mitogen stimulated system. In general, the metabolites have immunosuppressive activity of less than 10% of cyclosporin G. The significance of these findings in relation to the therapeutic monitoring of cyclosporin G is discussed.Keywords
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