Biological and physio-chemical properties of some N-acyl-daunorubicin derivatives

Toxicity of liposomal N-acyl daunorubicins to L929 cells in culture

“…This difference appeared to be due to Nsubstitution, as found by Aszalos et al (1979) with another cell line, since the toxicity of the analogues was related to the lengths of the N-acyl chain, and could not be accounted for by differences in incorporation or retention by liposomes. Furthermore, the toxicity of liposomal N-acyl daunorubicins to L929 cells was highly dependent on lipid concentration, confirming that their action was mediated by the liposomes, though the mechanisms involved were not investigated.…”

“…Furthermore, the toxicity of liposomal N-acyl daunorubicins to L929 cells was highly dependent on lipid concentration, confirming that their action was mediated by the liposomes, though the mechanisms involved were not investigated. The mode of action of N-acyl daunorubicins is not entirely clear, and may differ from that of the unmodified compound (Aszalos et al, 1979). Free daunorubicin can interact with the DNA double helix and block transcription (Ward et al, 1965) but N-acyl daunorubicins do not interact specifically with DNA (Aszalos et al, 1979;Di Marco & Arcamone, 1975).…”

“…The mode of action of N-acyl daunorubicins is not entirely clear, and may differ from that of the unmodified compound (Aszalos et al, 1979). Free daunorubicin can interact with the DNA double helix and block transcription (Ward et al, 1965) but N-acyl daunorubicins do not interact specifically with DNA (Aszalos et al, 1979;Di Marco & Arcamone, 1975). Daunorubicin can also act by inhibiting respiration (Murphree et al, 1976) and by generating superoxide radicals (Bozzi et al, 1981) and these mechanisms of cytotoxicity would predominate in the case of analogues unable to bind to DNA.…”