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Description: Daunorubicin (RP13057) can inhibit DNA and RNA synthesis, with a Ki of 0.02 for DNA synthesis μ M.
Related categories
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Research Fields>>Cancer
Natural Products>>Quinones
Target point
Topoisomerase II
The average IC50 value of daunorubicin (Dnr) in Molt-4 cells studied in vitro is 0.04 μ M. Daunorubicin belongs to anthracycline, a group of cytotoxic chemotherapy agents. The cytotoxic effect of anthracycline is caused by DNA insertion and the ability to interfere with DNA transcription and replication by inhibiting topoisomerase II and producing reactive oxygen species [2]. The concentration range of daunorubicin inhibiting DNA and RNA synthesis in HeLa cells is 0.2 to 2 μ M. For daunorubicin (Dnr) in human pancreatic cell line L3.6, the IC50 value is 0.4 μ M [3].
In vivo studies showed a significant increase in urinary protein excretion, serum creatinine, and blood urea nitrogen (BUN) levels in the daunorubicin group (3mg/kg, iv) compared to the control group. Compared with the control group, the application of daunorubicin (DNR) resulted in a significant increase in the level of malondialdehyde (MDA) in renal tissue [4].
Cell experiments use MTT assay to evaluate the chemical sensitivity to daunorubicin. In short, the 96 well plate is set with an initial density of 2 × 105 cells/mL were incubated in the absence and presence of 9 different concentrations at 37 ° C in an atmosphere of 5% CO2 for 72 hours. The range of daunorubicin (Dnr) or Dox is 1.90 to 0.007 μ M. In triplicate. After warming, add 10 to each well μ LMTT solution (5mg/mL tetrazolium salt) and incubate the plate at 37 ℃ for another 4 hours. By adding 100 to a 10mM HCl solution μ Dissolve methyl crystals in L10% SDS and incubate overnight at 37 ℃. The absorbance was measured at 540nm using a 96 well enzyme-linked immunosorbent assay (ELISA) reader and a reference at 650nm. The chemical sensitivity is expressed as IC 50, which is the concentration of drug that causes 50% cell survival compared to control cells without drug growth. Calculate using Microsoft Excel [2].
Animal experimental rats [4] used 8-week-old male Sprague-Dawley rats. Before starting the experiment, isolate the animals and allow them to adapt for another 2 weeks. On day 0, each animal received a single intravenous injection of daunorubicin (iv) at a dose of 3mg/kg. Daunorubicin was administered in three equal injections at 48 hour intervals, lasting for one week, to achieve a cumulative dose of 9mg/kg, which fully demonstrates the occurrence of cardiotoxicity and nephrotoxicity. Inject 0.9% NaCl of corresponding volume into age-matched rats and use it as a control (group control; n=