Strong binding of ditrisarubicin B to DNA.
- 1 January 1988
- journal article
- research article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 41 (5) , 655-659
- https://doi.org/10.7164/antibiotics.41.655
Abstract
DNA binding characteristics of ditrisarubicin B were studied by the fluorescence titration technique. Ditrisarubicin B bound to calf thymus DNA with an affinity higher than any we have ever seen among anthracyclines. The apparent association constant (Kapp) of ditrisarubicin B was 2.36 .times. 108 M-1, which is 22.7 times larger than that of doxorubicin. The apparent number of binding sites (napp) of ditrisarubicin B per nucleotide of DNA was 0.164, and this value is identical with that of doxorubicin. Betaclamycin A, which has a trisaccharide chain at C-7 but no carbohydrate at C-10 in the aglycone, interacted with DNA to give a Kapp of 5.92 .times. 106 M-1 and napp of 0.178. These results suggest to us that the high affinity of ditrisarubicin B for DNA is caused by the existence of a glycosidic chain at C-10.This publication has 2 references indexed in Scilit:
- Structure-activity relationships of anthracyclines relative to cytotoxicity and effects on macromolecular synthesis in L1210 leukemia cells.The Journal of Antibiotics, 1981
- The interaction of adriamycin and adriamycin analogues with nucleic acids in the B and A conformationsBiochimica et Biophysica Acta (BBA) - Nucleic Acids and Protein Synthesis, 1979