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Chemical Compound Review

Ledakrin     3-dimethylammoniopropyl-(1- nitroacridin-9...

Synonyms: Ledacrine, DwLIP-GCGRrx, Nitracrine HCl, CCRIS 9297, C-283, ...
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Disease relevance of Nitracrine

  • Behavior of some biochemical components of blood of patients with ovarian carcinoma during Ledakrin treatment [1].
  • DNA from the liver nuclei unable to synthesize RNA due to Ledakrin treatment, retained the template activity against E. coli RNA polymerase [2].
  • Mutagenic activity of Ledakrin in microbial testing as well as its inductive effect on the release of free phages in lysogenic bacteria were compared with its transforming ability in human cell system [3].
  • Results of combined treatment withlung tissue resection and simultaneous administration of Ledakrin in bronchial carcinoma [4].
  • In Ehrlich ascites tumour cell nuclei ledakrin (1-nitro-9/3'-dimethylpropyloamine/acridine-2 HCl) induces condensation and margination of chromatin, compaction and segregation of nucleolar components and conglomeration of chromatin granule clusters [5].
 

High impact information on Nitracrine

 

Biological context of Nitracrine

  • Stimulation of DNA-repair synthesis is gradually shut off during prolonged incubation of the cells with Ledakrin or during postincubation of the cells in a drug-free medium [10].
  • The first cross-links were introduced in B. subtilis cell genomes at minimal bactericidal concentrations of Ledakrin of mitomycin C [11].
  • DNA damage in HeLa s3 cells by an antitumor drug Ledakrin and other antitumor 1-nitro-9-aminoacridines [10].
  • Ledakrin, as compared to mitomycin C, was a very effective cross-linking agent, inducing one covalent cross-link per approx. 20 X 10(3) (B. subtilis), 56 X 10(3) (HeLa) or 80 X 10(3) (Eat) DNA base pairs [11].
  • These studies were aimed at characterizing the capability of an antitumor DNA-damaging drug, Ledakrin, and its analogs to inhibit DNA replication in HeLa S3 cells [12].
 

Anatomical context of Nitracrine

 

Associations of Nitracrine with other chemical compounds

  • Some of Ledakrin -induced DNA breaks are probably generated by endonucleolytic cleavage in the course of repair processes as indicated by experiments with Novobiocin, an antibiotic preventing the incision step of DNA repair [10].
  • Unlike [ethyl-14C]quinacrine, compared in vitro, covalent macromolecules binding with Ledakrin in vitro, and most probably in vivo, can be equated to NADPH-dependent activation(s) by oxidoreductase systems and the presence of DNA alone was not satisfactory in itself to attain Ledakrin binding [16].
 

Gene context of Nitracrine

  • An antitumour DNA cross-linking drug, ledakrin, and other antitumour 1-nitro-9-aminoacridines applied to HeLa S3 cells caused a preferential accumulation of cells in S phase, as found by the flow cytometry technique [9].
  • The phases G1 and S are prolonged while M is unchanged after 6h incubation with ledakrin [17].
  • Analysis of the cell cycle in the root meristem of Allium cepa under the influence of ledakrin [17].
  • Ledakrin induced a biphasic action, after a phase of increase of PD, SCC and sodium flux the transport of sodium ions decreased gradually [14].
 

Analytical, diagnostic and therapeutic context of Nitracrine

  • The ledakrin transformation products were separated and analyzed by HPLC with diode array detection [6].
  • Localization of DNA in nuclei of the cells labelled with 3H-thymidine and subsequently treated with ledakrin is studied using high-resolution autoradiography [5].

References

  1. Behavior of some biochemical components of blood of patients with ovarian carcinoma during Ledakrin treatment. Dobryszcka, W. Materia medica Polona. Polish journal of medicine and pharmacy. (1976) [Pubmed]
  2. Inhibition of RNA polymerase B activity in normal and regenerating rat liver after administration of 9-aminoacridine. Krawczyk, Z. Acta Biochim. Pol. (1982) [Pubmed]
  3. Comparative study of mutagenic, inductive and transforming activities of ledakrin. Gajcy, H., Chłopkiewicz, B., Koziorowska, J. Polish journal of pharmacology and pharmacy. (1979) [Pubmed]
  4. Results of combined treatment withlung tissue resection and simultaneous administration of Ledakrin in bronchial carcinoma. Rogalski, E., Domagala, J., Kolodziej, J. Materia medica Polona. Polish journal of medicine and pharmacy. (1976) [Pubmed]
  5. High-resolution autoradiographic study on the presence of chromatin structures within interchromatin granule conglomerations. Gruca, S., Krzyzowska-Gruca, S., Zborek, A. Acta Histochem. (1981) [Pubmed]
  6. Products of metabolic activation of the antitumor drug ledakrin (nitracrine) in vitro. Gorlewska, K., Mazerska, Z., Sowiński, P., Konopa, J. Chem. Res. Toxicol. (2001) [Pubmed]
  7. Distribution of interchromatin granules in nuclear matrices obtained from nuclei exhibiting different degree of chromatin condensation. Krzyzowska-Gruca, S., Zborek, A., Gruca, S. Cell Tissue Res. (1983) [Pubmed]
  8. In vitro DNA crosslinking by Ledakrin, an antitumor derivative of 1-nitro-9-aminoacridine. Bartoszek, A., Dackiewicz, P., Składanowski, A., Konopa, J. Chem. Biol. Interact. (1997) [Pubmed]
  9. Effects of ledakrin on DNA and cell cycle in HeLa S3 cells. Woynarowski, J.M., Konopa, J. Drugs under experimental and clinical research. (1986) [Pubmed]
  10. DNA damage in HeLa s3 cells by an antitumor drug Ledakrin and other antitumor 1-nitro-9-aminoacridines. Woynarowski, J.M., Bartoszek, A., Konopa, J. Chem. Biol. Interact. (1984) [Pubmed]
  11. The mode of action of cytotoxic and antitumor 1-nitroacridines. III. In vivo interstrand cross-linking of DNA of mammalian or bacterial cells by 1-nitroacridines. Konopa, J., Pawlak, J.W., Pawlak, K. Chem. Biol. Interact. (1983) [Pubmed]
  12. The mechanism of inhibition of DNA replication in HeLa S3 cells by the antitumor drug Ledakrin and other antitumor 1-nitro-9-aminoacridines. Woynarowski, J.M., Bartoszek, A. Biochim. Biophys. Acta (1985) [Pubmed]
  13. Sodium transport across isolated epithelial structures in vitro--Ledakrin in the liposomes as a moderator of the bioelectric activity of frog skin. Rakowski, W., Knapowski, J. Acta physiologica Polonica. (1983) [Pubmed]
  14. Early effect of ledakrin -- a nitro-derivative of acridine -- on cell membrane. Popowicz, P., Podsiadło, H., Knapowski, J. Acta physiologica Polonica. (1980) [Pubmed]
  15. Blood serum peptidases in patients with ovarian carcinoma treated with Ledakrin. Warwas, M., Narczeuska, B., Dobryszycka, W. Arch. Immunol. Ther. Exp. (Warsz.) (1977) [Pubmed]
  16. The mode of action of cytotoxic and antitumor 1-nitroacridines. II. In vivo enzyme-mediated covalent binding of a 1-nitroacridine derivative, Ledakrin or Nitracrine, with dna and other macromolecules of mammalian or bacterial cells. Pawlak, J.W., Pawlak, K., Konopa, J. Chem. Biol. Interact. (1983) [Pubmed]
  17. Analysis of the cell cycle in the root meristem of Allium cepa under the influence of ledakrin. Antosiewicz, D. Folia Histochem. Cytobiol. (1990) [Pubmed]
 
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