title: Covalent binding of the antitumor agent N2-methyl-9-hydroxy-ellipticinium acetate (NSC 264137) on RNA and poly A in vitro.
abstract: The antineoplastic compound N2-methyl-9-hydroxyellipticinium (9-OH-NME) is able to bind to different biological molecules after an oxidative activation by horseradish peroxidase and hydrogen peroxide. In this study, the efficient covalent binding in vitro of 9-OH-NME onto RNA and poly A is described. The phenomenon is analyzed by different HPLC methods and the yield of binding is determined using [3H]9-OH-NME. For an initial ratio drug per nucleotide of 0.07, the rb obtained (ratio of drug bound per nucleotide) of 0.026 for RNA and 0.044 for poly A, which represent respectively a yield of 40% and 60% for the drug fixation onto these macromolecules. These facts demonstrate the high electrophilicity of para-quinone-imine derivatives in ellipticinium series.
mesh_terms: D000470:Alkaloids; D000478:Alkylation; D000970:Antineoplastic Agents; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D004611:Ellipticines; D006735:Horseradish Peroxidase; D011061:Poly A; D012331:RNA, Fungal; D012441:Saccharomyces cerevisiae; D014316:Tritium
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; D004611:Ellipticines; D012331:RNA, Fungal; D014316:Tritium; C027767:elliptinium; D011061:Poly A; D006735:Horseradish Peroxidase