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Bleomycin is an antineoplastic antibiotic. The drug is active against gram-positive and gram-negative bacteria and fungi, but its cytotoxicity precludes its use as an anti-infective agent. The precise mechanism(s) of action of bleomycin is not fully known. Several studies in Escherichia coli and HeLa cells suggest that the drug inhibits the incorporation of thymidine into DNA. In these in vitro studies, DNA synthesis was inhibited to a greater extent than was RNA or protein synthesis. Bleomycin also appears to labilize the DNA structure, resulting in scission of both single- and double-stranded DNA. The drug has no immunosuppressive activity in mice
Bleomycin sulfate is a mixture of basic cytotoxic glycopeptide antibiotics produced by Streptomyces verticillus; bleomycin A2 and bleomycin B2 are the major components. Bleomycin sulfate occurs as a cream-colored, amorphous powder and is very soluble in water and sparingly soluble in alcohol. The potency of bleomycin is assayed microbiologically; the activity of 1 unit of bleomycin is equivalent to the activity of 1 mg of bleomycin A2 reference standard. Following reconstitution, bleomycin sulfate injection has a pH of 4.5–6, depending upon the diluent used
Currently, antibiotic therapies using bleomycin are indicated in patients with Hodgkin's lymphoma, testicular tumor and Wilms' tumor, among others. Furthermore, in the course of studying the chemically complex structure of bleomycin, researchers were able to clarify the mechanisms that made it effective, and to develop techniques for antibiotic synthesis and biosynthesis that led to the development of peplomycin, a less toxic derivative with a wide antitumor spectrum that was introduced in 1981 for the treatment of prostatic cancer.
|CAS#||9041-93-4 (bleomycin sulfate)|
|Category||Peptide antibiotic, DNA strand scission agent.|
|Site Specificity||5'-GpT-3' and 5'-GpC-3'|
|Effect on DNA||DNA unwinding angle 12o, lengthens DNA 0.31 nm per drug insertion [Povirk, 1979]. Alters PAGE migration of intrinsically bent DNA|
|Source||Blenoxane is a mixture of bleomycins, approximately 60% bleomycin A2, 30% bleomycin B2 and 10% other bleomycins. Natural product produced by Streptomyces verticillus.|
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