Mutactimycin,a new anthracycline antibiotic,consists of 5 components: mutac-timycin A,B,C,D and 7-deoxymutactimycinone A. Mutactimycin components differ from each other in suppressing proliferation and inducing differ...Mutactimycin,a new anthracycline antibiotic,consists of 5 components: mutac-timycin A,B,C,D and 7-deoxymutactimycinone A. Mutactimycin components differ from each other in suppressing proliferation and inducing differentiation of human erythroleukemia K-562 cells. Determined by benzidine staining, the percentage of K-562 cells with hemoglobin expression was86% by mutactimycin C. The peak percentage of benzidine positive cells appeared on day 5 or 6.The differentiated cells were partially reversed after drug removal.The induced cells lost the clonogenicity in soft-agar. The kinetics of differentiation induced by mutactimycin C, in comparison with other known anthracycline antibiotics,was similar to that by doxorubicin, epirubicin anddaunorubicin. Mutactimycin C was more active than aclarubicin A. The structure-activity relationship for mutactimycin components suggested that the substituting groups on C_3, C_11, and the saccharide on C_7 might be important for their activities.展开更多
文摘Mutactimycin,a new anthracycline antibiotic,consists of 5 components: mutac-timycin A,B,C,D and 7-deoxymutactimycinone A. Mutactimycin components differ from each other in suppressing proliferation and inducing differentiation of human erythroleukemia K-562 cells. Determined by benzidine staining, the percentage of K-562 cells with hemoglobin expression was86% by mutactimycin C. The peak percentage of benzidine positive cells appeared on day 5 or 6.The differentiated cells were partially reversed after drug removal.The induced cells lost the clonogenicity in soft-agar. The kinetics of differentiation induced by mutactimycin C, in comparison with other known anthracycline antibiotics,was similar to that by doxorubicin, epirubicin anddaunorubicin. Mutactimycin C was more active than aclarubicin A. The structure-activity relationship for mutactimycin components suggested that the substituting groups on C_3, C_11, and the saccharide on C_7 might be important for their activities.
