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Interaction of anthracycline antibiotics with biopolymers: Comparative studies of DNA binding and antimicrobial activity of rhodomycin‐type anthracycline antibiotics
Author(s) -
Stutter E.,
Walter Axel,
Fleck Werner F.
Publication year - 1986
Publication title -
journal of basic microbiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.58
H-Index - 54
eISSN - 1521-4028
pISSN - 0233-111X
DOI - 10.1002/jobm.3620261010
Subject(s) - bacillus subtilis , ionic strength , antimicrobial , chemistry , antibiotics , anthracycline , homogeneous , titration , equilibrium constant , stereochemistry , combinatorial chemistry , thermodynamics , biochemistry , organic chemistry , biology , bacteria , aqueous solution , genetics , physics , cancer , breast cancer
The binding of the anthracyclines β‐rhodomycin‐I and β‐rhodomycin‐II to calf thymus DNA was investigated by both equilibrium and kinetic methods taking into account ligand dimerization (ionic strength I = 0.2 M, pH 6.0). The analysis was based upon a cooperative single‐step binding mechanism with overlapping of potential binding sites on a linear homogeneous lattice. Equilibrium binding parameters were estimated from spectrophotometric titration experiments by means of a nonlinear fitting program. The results were compared with those obtained previously for the related antibiotic iremycin and were complemented by kinetic parameters determined from temperature‐jump experiments at high binding ratio. The binding constants and the mean attachment times of the drugs were found to increase in the serial order iremycin, β‐rhodomycin‐I and β‐rhodomycin‐II, which is in line with their increasing antimicrobial activity on Bacillus subtilis ATCC 6633.