Synthesis of deuterium-labelled elliptinium and its use in metabolic studies.
The 9-hydroxy-2-(U-2H3) methylellipticinium acetate (elliptinium) was synthesized with an isotopic purity of at least 96%. The structure was confirmed by proton nuclear magnetic resonance and direct probe fast atom bombardment mass spectrometry. A mixture of elliptinium and its deuterated analogue was administered intravenously to rats. In urine, after analysis by liquid chromatography/mass spectrometry (LC/MS), unchanged drug and N-acetylcysteinylelliptinium were found. In bile, after ion-pair extraction and LC/MS, the glutathionylelliptinium was found in addition to the parent drug and the N-acetylcysteine adduct.
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Pharmacologie Clinique (UA147 CNRS, U140 INSERM), Pavillon de Recherche, Institut Gustave-Roussy, Villejuif, France.
D000470:Alkaloids / Q000138:chemical synthesis*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism; D001646:Bile / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D002853:Chromatography, Liquid; D003903:Deuterium; D004611:Ellipticines / Q000138:chemical synthesis* / Q000378:metabolism; D007553:Isotope Labeling; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D051381:Rats; D011919:Rats, Inbred Strains
D000470:Alkaloids; D000970:Antineoplastic Agents; D004611:Ellipticines; C027767:elliptinium; D003903:Deuterium