Ellipticines: correlation between in vitro DNA intercalation and physiological properties?
The in vitro DNA-intercalator ellipticine and five of its derivatives have been investigated for some of their physiological effects on several Escherichia coli strains. The highly water-soluble, quaternarized derivatives of ellipticine have no bactericidal effect and do not induce the synthesis of rec A protein. Ellipticine itself, as well as the derivatives obtained by adding an amino or an hydroxyl substituent in position 9, promotes the induction of rec A protein and is cytostatic on some bacterial strains. The non-intercalating brominated derivative is a strong bactericidal agent, which apparently promotes the lysis of the bacteria. At low concentrations, it slightly induces the synthesis of rec A protein. We conclude that there is no correlation at all between the physiological properties of the ellipticines and their physico-chemical behavior in vitro.
D000470:Alkaloids / Q000494:pharmacology*; D004269:DNA, Bacterial; D004611:Ellipticines / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects* / Q000235:genetics / Q000254:growth & development / Q000378:metabolism; D007364:Intercalating Agents / Q000494:pharmacology*; D016685:Mitomycin; D008937:Mitomycins / Q000494:pharmacology; D011938:Rec A Recombinases / Q000096:biosynthesis; D013997:Time Factors
D000470:Alkaloids; D004269:DNA, Bacterial; D004611:Ellipticines; D007364:Intercalating Agents; D008937:Mitomycins; D016685:Mitomycin; D011938:Rec A Recombinases