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Binding to DNA and cytotoxic evaluation of ascididemin, the major alkaloid from the Mediterranean ascidian Cystodytes dellechiajei
Bonnard, I.; Bontemps, N.; Lahmy, S.; Banaigs, B.; Combaut, G.; Francisco, C.; Colson, P.; Houssier, C.; Waring, M.J.; Bailly, C. (1995). Binding to DNA and cytotoxic evaluation of ascididemin, the major alkaloid from the Mediterranean ascidian Cystodytes dellechiajei. Anti-Cancer Drug Design 10(4): 333-346
In: Anti-Cancer Drug Design. Oxford University Press: Oxford. ISSN 0266-9536
Peer reviewed article  
Beschikbaar in  Auteurs 
Trefwoorden
    Cystodytes dellechiajei (Della Valle, 1877) [WoRMS]
    Marien/Kust
Author keywords
    ASCIDIDEMIN; CYSTODYTES DELLECHIAJEI; CYTOTOXICITY; DNA BINDING
Auteurs  Top 
  • Bonnard, I.
  • Bontemps, N.
  • Lahmy, S.
  • Banaigs, B.
  • Combaut, G.
  • Francisco, C.
  • Colson, P.
  • Houssier, C.
  • Waring, M.J.
  • Bailly, C.
Abstract
    The isolation of ascididemin from the Mediterranean ascidian Cystodytes dellechiajei is described. This alkaloid consists of a planar pentacyclic chromophore which was investigated for its DNA-binding and cytotoxic properties. Spectroscopic measurements provided evidence that the drug intercalates into DNA. DNase I footprinting assays indicated that the binding of ascididemin to CC-rich sequences is favoured over binding to AT-rich and mixed sequences. Chemical probes were used to detect ligand-induced structural changes in DNA. The alkaloid induces a hyperreactivity of the DNA towards potassium permanganate, but not towards diethylpyrocarbonate, just as is the case with ethidium bromide;; it has little effect on the catalytic activities of topoisomerases I and II. Ascididemin exhibits marked cytotoxicity towards human leukaemic cells in vitro and appears to be practically equally toxic for drug-sensitive and multidrug-resistant cell lines. The results suggest that DNA, but not topoisomerases, may represent the critical cellular target at which this marine alkaloid exhibits its potent cytotoxic properties in vitro.
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