Antitumor effect of new conjugates of anthracycline antibiotic carminomycin bound to chitosan

作者：Todorova Nedyalka^*; Ilarionova Maya; Todorov Dimiter

来源：Macedonian Journal of Chemistry and Chemical Engineering, 2007, 26(2): 147-150.

• carminomycin
• pharmacokinetics
• HL-60 cells
• leukemia P388
• leukemia L1210
• chitosan
• anthracycline antibiotics

The antileukemic activities of two conjugates of the anthracycline antibiotic carminomycin - CX(1) and CX(2), were investigated. The direct cytotoxic efficacies of the two conjugates and free carminomycin (C), were measured by an MTT-assay which provides excellent reproducibility and statistical significance. The treatment of HL-60 cells with the three compounds for 48 and 96 hours showed considerable sensitivity to the free carminimycin, as well as to its conjugates CX(1) and CX(2). The ascetic form of leukemia P388 and leukemia L1210 (transplantation dose of 1.10(6) tumor cells) in hybrid mice BDF(1) was used as leukemic models. All compounds investigated showed a maximal cytotoxic response and strong concentration dependence. By comparing the cytotoxic profile of carminomycin to those of CX(1) and CX(2), it can be assumed that a slower release of the active drug carminomycin have occurred. The criterion T/C showed a considerable antileukemic effect from 1.0 to 18.0 mg/kg. In conclusion, the conjugates CX(1) and CX(2) represent biologically active compounds with a putative depot-effect of slow release of the active intercalating agent carminomycin.

• 出版日期2007
• 单位北京化工大学