Dactinomycin


Dactinomycin. Dactinomycin [50-76-0] (actinomycin D, actinomycin Cl, Cosmegen), is the only actinomycin in clinical use.  [c.157]

Total synthesis of dactinomycin has been accompHshed, and at least thirty natural actinomycins and many synthetic and semisynthetic actinomycins have been tested (220,221,228). At one time cactinomycin [8052-16-2] (actinomycin C), a mixture of actinomycins D, C2, and C3, was sold as an antineoplastic.  [c.157]

Common Name Distamycin A  [c.1387]

Yon must consider these factors when decidingon sampling interval. There is no ideal interval for all iTiolecii les however, intervals ofO.5 1.0 ps are often used.  [c.80]

The recognition of specific nucleic acid sequences is important in the regulation of many biological processes. The antibiotic distamycin binds to the minor groove of the DNA double helix with a strong preference for A-T rich regions. The sequence specificity presumably results from hydrogen bonding between the amide NH groups of distamycin and 0-2 of thymine and N-3 of adenine. The stepwise peptide synthesis of distamycin (M. Bialer, 1978 L. Grehn, 1983, 1986 J.W. Lown, 1985) can be modified by attachment of EDTA-type chelands at the terminal amide and insertion of oligoethylene glycol type chelands in the centre of the oligomer chain (J.H. Griffin, 1987). The binding of the central amide groups to DNA in the hypothetical  [c.343]

Bleomycin and cyclosporine are the two economically most important streptomycete peptide antibiotics used as antitumor agents and immunomodulators, although dactinomycin is important medically for several tumors (see Chemotherapeutics, anticancer Immunotherapeutic agents).  [c.157]

Dactinomycin, an antineoplastic dmg, was discovered in 1943 and is made in rather pure form by StreptomjcesparvuUus. Dactinomycin has some bacteriostatic antibacterial and antifungal activity, but high toxicity limits its use to antineoplastic therapy. It may be used alone or with other antineoplastics, with or without surgery and synergistic x-ray therapy. Dose limiting bone marrow toxicity may result in low white cell and platelet count. Intestinal mucosal damage also occurs. Reviews of more detailed chemotherapeutic information are available (217—222).  [c.157]

Dactinomycin forms bright red, rhomboid prisms from absolute ethanol. Dactinomycin USP is a yellow lyophylized powder. It is soluble in water at 10°C, slightly soluble in water at 37°C, and soluble in ethanol Dactinomycin USP must be protected from light and should be preserved in air-tight containers and stored below 40°C. Great care must be taken in handling this extremely toxic dmg to avoid breathing the powder or getting dry powder or solutions on the skin. Dactinomycin is mutagenic, carcinogenic, and teratogenic. The LD q in mice, when given intravenously, is about 0.7 mg/kg body weight. Other properties, fermentation, and purification methods (223—226), and studies on biosynthesis by multien2yme complexes can be found in the hterature (227).  [c.157]

Fig. 12. Stmcture of dactinomycin (actinomycin D) where MeVal = N-methylvaline and Sar = sarcosine. Fig. 12. Stmcture of dactinomycin (actinomycin D) where MeVal = N-methylvaline and Sar = sarcosine.
Dactinomycin is useful against several tumors especially Wilms tumor of the kidney and rhabdomyosarcoma. Wilms tumor normally requires a combination of surgery, x-ray irradiation, and dactinomycin plus vincristine [57-22-7] or other antitumor agents. Resistance of the multidmg  [c.157]

Dactinomycin intercalates into double stranded DNA inhibiting DNA-dependent RNA polymerase. Dactinomycin also can cause single strand breaks in DNA. Inhibition of DNA synthesis only takes place at higher concentrations of dmg. A molecular model for dactin omycin -DN A interaction has been proposed based in part on x-ray crystallography of a complex containing two molecules of deoxyguanosine and one of dactinomycin (230). Conformations of dactinomycin—oligonucleotide complexes are being studied by nmr (231,232).  [c.157]

To 17 C of a culture obtained by submerged fermentation as mentioned above, siliceous earth is added and the batch is filtered. The mixture of mycelium and the siliceous earth are agi-tatedforl hour with 2.5 Cof butanol. This treatment is repeated twice. Thebutanolic extracts are combined, washed with water, evaporated to dry ness (about 10 g) and boiled with acetone (80 ml). The residue (5.41 g of yellowish powder) is distamycin.  [c.1387]


See pages that mention the term Dactinomycin : [c.344]    [c.344]    [c.277]    [c.277]    [c.277]    [c.277]    [c.277]    [c.337]    [c.852]    [c.1053]    [c.1070]    [c.485]    [c.485]    [c.485]    [c.147]    [c.147]    [c.147]    [c.147]    [c.157]    [c.157]    [c.160]    [c.439]    [c.508]    [c.504]    [c.298]    [c.426]    [c.956]    [c.1387]    [c.1388]    [c.1606]    [c.1607]    [c.1687]    [c.1693]    [c.1693]    [c.1714]   
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Pharmaceutical manufacturing encyclopedia Edition 2  -> Dactinomycin