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A CD study of interactions of ellipticine derivatives with DNA
Author(s) -
Monnot Monique,
Mauffret Olivier,
Simon Valérie,
Lescot Elie,
Psaume Bernard,
Saucier Jean-Marie,
Belehradek Jean,
Fermandjian Serge
Publication year - 1990
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(90)81053-q
Subject(s) - intercalation (chemistry) , chemistry , dna , circular dichroism , stereochemistry , base pair , molecule , crystallography , in vitro , biophysics , biochemistry , organic chemistry , biology
UV‐absorption and circular dichroism (CD) experiments showed that ellipticine derivatives may interact with DNA according to 3 possible binding modes depending on their structure and concentration. The first mode concerned intercalation of 1‐methyl‐9‐hydroxyellipticine (1‐Me‐HE) with its long axis perpendicular to the long axis of base pairs. The same drug was able to bind to external sites (second mode) once the intercalation sites were saturated at high concentration. The third mode illustrated by 1,2‐dimethyl‐9‐hydroxyisoellipticinium (1‐Me‐isoNMHE), concerned self‐stacked molecules interacting at the surface of DNA. Biological significance of these different binding modes was then discussed in connection with in vitro cytotoxic activity of compounds.