|
|||||
|
|
Inhibition of malaria parasite growth by quinomycin A and its derivatives through DNA-intercalating activity |
|
| Authors: | Hiroki Hayase Nobumoto Watanabe Chung Liang Lim Toshihiko Nogawa Keisuke Komatsuya Kiyoshi Kita |
| Institution: | 1. Antibiotics Laboratory, RIKEN, Wako, Japan;2. Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, Wako, Japan;3. Industrial Biotechnology Research Laboratory, School of Biological Sciences, Universiti Sains Malaysia, Penang, Malaysia;4. Chemical Biology Research Group, RIKEN Center for Sustainable Resource Science, Wako, Japan;5. Department of Biomedical Chemistry, Graduate School of Medicine, The University of Tokyo, Tokyo, Japan |
| Abstract: | Quinomycin A and its derivatives were identified as potent antimalarial (Plasmodium falciparum) agents in a screen of the RIKEN NPDepo chemical library. IC50 values of quinomycin A and UK-63,598 were approximately 100 times lower than that of the antimalarial drug chloroquine. This activity was mitigated by the addition of plasmid DNA, suggesting that these compounds act against parasites by intercalating into their DNA. |
| Keywords: | antimalarial agents quinomycin A DNA intercalation |