Article (Scientific journals)
DNA intercalation, topoisomerase II inhibition and cytotoxic activity of the plant alkaloid cryptolepine
Bailly, Christian; Laine, W.; Baldeyrou, B. et al.
2000In Anti-Cancer Drug Design, 15 (3), p. 191-201
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Abstract :
[en] Cryptolepine and neocryptolepine are two indoloquinoline alkaloids isolated from the roots of the African plant Cryptolepis sanguinolenta. Both drugs have revealed antibacterial and antiparasitic activities and are strongly cytotoxic to tumour cells. We have recently shown that cryptolepine can intercalate into DNA and stimulates DNA cleavage by human topoisomerase II. In this study, we have investigated the mechanism of action and cytotoxicity of neocryptolepine, which differs from the parent isomer only by the orientation of the indole unit with respect to the quinoline moiety. The biochemical and physicochemical results presented here indicate that neocryptolepine also intercalates into DNA, preferentially at GC-rich sequences, but exhibits a reduced affinity for DNA compared with cryptolepine. The two alkaloids interfere with the catalytic activity of human topoisomerase II but the poisoning activity is slightly more pronounced with cryptolepine than with its isomer. The data provide a molecular basis to account for the reduced cytotoxicity of neocryptolepine compared with the parent drug.
Disciplines :
Physical, chemical, mathematical & earth Sciences: Multidisciplinary, general & others
Biochemistry, biophysics & molecular biology
Author, co-author :
Bailly, Christian
Laine, W.
Baldeyrou, B.
De Pauw-Gillet, Marie-Claire ;  Université de Liège - ULiège > Département des sciences biomédicales et précliniques > Histologie - Cytologie - Département des sciences biomédicales et précliniques
Colson, Pierre ;  Université de Liège - ULiège > Département de chimie (sciences) > Chimie physique biologique
Houssier, Claude ;  Université de Liège - ULiège > Services généraux (Faculté des sciences) > Relations académiques et scientifiques (Sciences)
Cimanga, K.
Van Miert, S.
Vlietinck, A. J.
Pieters, L.
Language :
English
Title :
DNA intercalation, topoisomerase II inhibition and cytotoxic activity of the plant alkaloid cryptolepine
Publication date :
June 2000
Journal title :
Anti-Cancer Drug Design
ISSN :
0266-9536
Publisher :
Oxford University Press, Oxford, United Kingdom
Volume :
15
Issue :
3
Pages :
191-201
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
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