9041-93-4 Usage
Description
Bleomycin sulfate is a complex of 11 glycopeptide antitumor antibiotics, originally isolated from Streptomyces verticillus in 1972. It coordinates with metals to produce reactive oxygen species, causing oxidative damage to DNA and RNA, and induces double-strand DNA damage. The main component of bleomycin used clinically is Bleomycin A2.
Uses
Used in Anticancer Applications:
Bleomycin sulfate is used as an antineoplastic agent for the treatment of a range of tumors. It acts by intercalation of DNA and RNA, and in the presence of oxygen and metal ions, notably copper and iron, forms a pseudo-enzyme that induces DNA cleavage.
Used in Research:
Bleomycin sulfate is used to induce lung fibrosis in animal disease models for research purposes.
Used in DNA and RNA Cleavage:
Bleomycin sulfate binds to DNA, inhibiting DNA synthesis and causing scission of DNA. It requires binding to oxygen and a metal ion, such as copper or iron, to cleave DNA. It is also able to cleave RNA, but at a less efficient and more selective degree.
Used in Apoptosis Induction and Regulation:
Bleomycin sulfate is reported to induce and regulate apoptosis in a variety of cells.
Used in Tumor Angiogenesis Inhibition:
Bleomycin sulfate is used to inhibit tumor angiogenesis.
Biochem/physiol Actions
Bleomycin sulfate binds to DNA, causes ssDNA scission at specific base sequences and inhibits DNA synthesis. This inhibitory action requires bleomycin to bind oxygen and a metal ion. It can also cleave RNA, to a lesser degree but more selectively. It acts as an inducer and regulator of apoptosis and inhibits tumor angiogenesis.
Clinical Use
Bleomycin is used IV in the palliative treatment of squamous cell head and neck cancers, testicular and other genital carcinomas, and Hodgkin's and non-Hodgkin's lymphoma.
Side effects
It is excreted via the kidneys, and serum concentrations of active drug are increased in patients with renal disease. The elimination half-life can rise from 2 to 4 hours to more than 20 hours in renal failure, resulting in significant toxicity, especially pulmonary toxicity.
Veterinary Drugs and Treatments
Bleomycin has occasionally been used as adjunctive treatment of
lymphomas, squamous cell carcinomas, teratomas, and nonfunctional
thyroid tumors in both dogs and cats. Recent work has demonstrated
that bleomycin may be promising for intralesional treatment
for a variety of localized tumors with or without concomitant
electropermeabilization.
References
1) Petering?et al.?(1990),?The role of redox-active metals in the mechanism of action of bleomycin; Chem. Biol. Interact.,?73?133
2) Huttenhofer?et al. (1992),?Cleavage of tRNA by Fe(II)-bleomycin; J. Biol. Chem.,?267?24471
3) Lee?et al.?(2017)?ASF1a Promotes Non-homologous End Joining Repair by facilitating Phosphorylation of MDC1 by ATM at Double-Strand Breaks;?Mol. Cell?68?61
4)?Xie?et al.?(2016), Upregulation of RGS2: a new mechanism for pirfenidone amelioration of pulmonary fibrosis; Respir. Res.,?17?103
5) Inomata?et al. (2014) Pirfenidone inhibits fibrocyte accumulation in the lungs in bleomycin-induced murine pulmonary fibrosis; Respir. Res.,?15?16
6) Tanaka?et al. (2008)?Increased glutathione level is not involved in enhanced bleomycin sensitivity in cisplatin-resistant 2780CP cells; Anticancer Res.,?28?2663
Check Digit Verification of cas no
The CAS Registry Mumber 9041-93-4 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 9,0,4 and 1 respectively; the second part has 2 digits, 9 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 9041-93:
(6*9)+(5*0)+(4*4)+(3*1)+(2*9)+(1*3)=94
94 % 10 = 4
So 9041-93-4 is a valid CAS Registry Number.
InChI:InChI=1/C52H77N13O19S3/c1-7-11-54-18-32-56-13-9-26(62-32)45(75)65-35(41(27-16-55-22-60-27)82-51-43(39(72)37(70)29(19-66)81-51)83-50-40(73)42(84-52(53)79)38(71)30(20-67)80-50)48(78)61-24(3)36(69)23(2)44(74)64-34(25(4)68)47(77)58-14-10-33-63-28(21-85-33)49-59-17-31(86-49)46(76)57-12-8-15-87(5)6/h9,13,16-17,21-25,29-30,34-43,50-51,54,66-73H,7-8,10-12,14-15,18-20H2,1-6H3,(H7-,53,55,57,58,60,61,64,65,74,75,76,77,78,79)/p+1/t23-,24+,25?,29+,30+,34?,35+,36-,37+,38-,39+,40-,41+,42+,43-,50-,51+/m0/s1
9041-93-4Relevant articles and documents
THERAPEUTIC FOR HEPATIC CANCER
-
, (2011/02/18)
A novel pharmaceutical composition for treating or preventing hepatocellular carcinoma and a method of treatment are provided. A pharmaceutical composition for treating or preventing liver cancer is obtained by combining a chemotherapeutic agent with an anti-glypican 3 antibody. Also disclosed is a pharmaceutical composition for treating or preventing liver cancer which comprises as an active ingredient an anti-glypican 3 antibody for use in combination with a chemotherapeutic agent, or which comprises as an active ingredient a chemotherapeutic agent for use in combination with an anti-glypican 3 antibody. Using the chemotherapeutic agent and the anti-glypican 3 antibody in combination yields better therapeutic effects than using the chemotherapeutic agent alone, and mitigates side effects that arise from liver cancer treatment with the chemotherapeutic agent.
Medicines for treating tumoral pathologies containing the ro5-4864 compound and an apoptosis-inducing agent
-
, (2008/06/13)
The invention concerns the use of Ro5-4864, and compounds derived therefrom, for preparing medicines for treating tumoral pathologies. The invention also concerns said compounds combined with an apoptosis-inducing agent, as combination products for simultaneous, separate or prolonged use, in cancer therapy.
Compositions containing piperine
-
, (2008/06/13)
A pharmaceutical composition having increased bioavailability characterized by piperine of the formula and a drug for treating a disease or condition of the human cardiovascular system, central nervous system, gastrointestinal tract, respiratory tract, endocrine system, genito urinary tract or haemopoietic system.
