Bleomycin

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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 4.56, 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.

Name Bleomycin Sulfate 
Blenoxane
CAS# 9041-93-4 (bleomycin sulfate)
CAS#  11056-06-7 (bleomycin)
NSC# 125066 (bleomycins)
Category Peptide antibiotic, DNA strand scission agent.
Binding Mode Intercalation
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.
   

 

  1. Bleomycin, epidoxorubicin, cyclophosphamide, vincristine and prednisone (BACOP) in patients with follicular non-Hodgkin's lymphoma
  2. In vivo antioxidant treatment protects against bleomycin-induced lung damage in rats.
  3. Induction of arginase I and II in bleomycin induced fibrosis of mouse lung.  
  4.  Role of Repeated Lung Injury and Genetic Background in Bleomycin-induced Fibrosis
  5. etoposide and either bleomycin or ifosfamide in the treatment of disseminated germ cell tumors
  6. Antileukinate, a Hexapeptide Inhibitor of CXC-Chemokine Receptor, Suppresses Bleomycin-induced Acute Lung Injury in Mice
  7. High-dose-rate brachytherapy with local injection of bleomycin for N0 oral tongue cancer--possibilities of the control of tumor implant by inserting applicators and the decrease in tumor dose
  8. Combining histology and biochemical measurements of connective tissue components in small samples of lung: application to bleomycin-induced fibrosis in the mouse
  9. The solution structure of the Ga(III)- bleomycin A2 complex resolved by NMR and molecular modeling; interaction with d(CCAGGCCTGG)

 

 

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