Daunorubicin

Daunorubicin inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 µM. The IC50 value: 0.02 µM (Ki for inhibition of DNA synthesis). in vitro: Daunorubicin inhibits both DNA and RNA syntheses in HeLa cells over a concentration range of 0.2 through 2 µM. Daunorubicin inhibits both DNA syntheses in Ehrlich ascites tumor cells over a concentration range of 4 µM. Daunorubic triggers apoptosis at concentrations of 0.5 and 1 µM in either HL-60 or U-937 human leukemic cells [1]. Daunorubicin stimulates ceramide elevation and apoptosis in P388 and U937 cells through de novo synthesis via activation of the enzyme ceramide synthase[2]. Daunorubicin dose-dependently increases the phosphatidylserine exposure and consequent procoagulant activity of human umbilical vein endothelial cells. In vivo: daunorubicin inhibited the proliferation of KG1a cells in a dose and time dependent manner (r = 0.983, P < 0.01).[1]. Fornari FA, et al. Interference by doxorubicin with DNA unwinding in MCF-7 breast tumor cells. Mol Pharmacol. 1994 Apr;45(4):649-56.[2]. Weiss RB. The anthracyclines: will we ever find a better doxorubicin? Semin Oncol. 1992 Dec;19(6):670-86. Potential mode of action/Key words. Targeting DNA & RNA, DNA & RNA synthesis inhibitor, Antitumoral, Induces Necrosis, Cytotoxic, Antibiotic