Studies on the effects of anthracyclines on mitochondrial respiration in vitro.
Aclacinomycin, 4'-epi-doxorubicin and 4'-epi-tetrahydropyranyl-adriamycin, three novel anthraquinone derivatives under investigation for their antitumour activity, showed an inhibitory effect on the in vitro respiration of mitochondria from rat hearts. The inhibition proved to be concentration-dependent in the range 0.05 to 1.40 mM and both the NADH-oxidase and the succinate oxidase systems were affected to different extents. Among the compounds tested, 4'-epi-tetrahydropyranyl-adriamycin appeared to be the least powerful effector, requiring a significantly higher concentration for 50% inhibition of oxidation than doxorubicin and the other analogues examined.
D015250:Aclarubicin / Q000031:analogs & derivatives*; D000818:Animals; D004317:Doxorubicin / Q000031:analogs & derivatives* / Q000494:pharmacology*; D015251:Epirubicin; D066298:In Vitro Techniques; D008297:Male; D008929:Mitochondria, Heart / Q000187:drug effects* / Q000378:metabolism; D009279:Naphthacenes / Q000494:pharmacology; D010085:Oxidative Phosphorylation; D010101:Oxygen Consumption; D051381:Rats; D011919:Rats, Inbred Strains
D009279:Naphthacenes; C011157:aclacinomycins; D015251:Epirubicin; D015250:Aclarubicin; D004317:Doxorubicin; C027260:pirarubicin