Binding of Nitrofuran Derivatives to Nucleic Acids and Protein

Abstract

1) The in vitro reduction of ¹⁴C-2-(2-furyl)-3-(5-nitro-2-furyl) acrylamide (AF-2) and ¹⁴C-nitrofurazone by xanthine oxidase-hypoxanthine resulted in the formation of their active metabolites capable of binding to desoxyribonucleic acid (DNA), ribonucleic acid (RNA) and protein. 2) The distribution and excretion of radioactivity in various tissues, gastrointestinal contents, feces and urine were examined after oral administration of ¹⁴C-AF-2 to rats. 3) The in vivo binding of ¹⁴C-AF-2 and ¹⁴C-nitrofurazone to liver protein, DNA and ribosomal RNA, and to kidney protein was demonstrated in rats given orally these drugs.