Uptake and subcellular localization of daunorubicin and adriamycin in cultured fibroblasts

Modification of uptake and subcellular distribution of doxorubicin by N-acylhydrazone residues as visualised by intrinsic fluorescence

“…4 / E, F). This is in line with the previously reported uptake and subcellular distribution of 1 in other cells, e.g., rat embryo fibroblasts and human myeloid leukaemia cells [9,10]. For the menthylterminated hydrazone 3 we found a subcellular localisation similar to that of 1, albeit proceeding more slowly.…”

“…The cells were incubated with 5 µM of 1-3 for 3 h and the residual fluorescence intensity in the supernatant following incubation was measured after a centrifugation step. The percental cellular drug uptake relative to reference solutions was calculated and plotted as shown in Figure 3 [9]. All test compounds accumulated strongly in the 518A2 and the HL-60 cells which corresponds well with their previously reported high cytotoxicity against these cell lines [7].…”

“…Typically, the cells were grown in DMEM (750 µL) in 4-well plates (Nunc) on glass coverslips and incubated with the test compounds 1, 2 or 3 (10 µM) for periods ranging from 2 h to 16 h. The medium was removed, 5 the cells were washed twice with phosphate buffered saline (PBS) and mounted vital in PBS. The Hoechst dye 33342 was optionally added (5 µg mL -1 ) to stain the nuclei and the cells were imaged using a ZEISS Axioplan fluorescence microscope [9,10].…”

In vivo effects of several anthracyclines on DNA integrity

“…In conclusion, if in vitro the binding of the analogs of daunorubicin studied here does not induce singlestrand breaks in the double-helical DNA, it is not the same in rive after treatment of mice bearing an Ehrlich ascites tumor by the same anthracycline derivatives: a Corrected values taking into account the lysosomal contamination [20] Mice were inoculated i.p. with 1 mg drug/mouse and sacrificed after 60 min.…”

Comparative uptake of adriamycin and daunorubicin in sensitive and resistant friend leukemia cells measured by flow cytometry

“…Presented at the VIII Conference on Analytical Cytology and Cytometry, Wentworth-by-the-Sea, New Hampshire, May 19-25, 1981. uptake (4,14,20,24,29) and the mechanism by which this uptake could be altered in vitro and in vivo are not known (13,15,22). The possibility of changes in the dynamic structural organization of the cell surface occurring during the development of cell resistance cannot be excluded.…”