This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Right arrowReprints and Permissions
Right arrow Copyright Information
Right arrow Books from ASM Press
Right arrow MicrobeWorld
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Go, M.-L.
Right arrow Articles by Kirk, K.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Go, M.-L.
Right arrow Articles by Kirk, K.

 Previous Article  |  Next Article 

Antimicrobial Agents and Chemotherapy, September 2004, p. 3241-3245, Vol. 48, No. 9
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.9.3241-3245.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

Antiplasmodial Chalcones Inhibit Sorbitol-Induced Hemolysis of Plasmodium falciparum-Infected Erythrocytes

Mei-Lin Go,1* Mei Liu,1 Prapon Wilairat,2 Philip J. Rosenthal,3 Kevin J. Saliba,4 and Kiaran Kirk4

Department of Pharmacy, National University of Singapore, Republic of Singapore,1 Department of Biochemistry, Mahidol University, Bangkok, Thailand,2 Department of Medicine, University of California, San Francisco, San Francisco, California,3 School of Biochemistry and Molecular Biology, Faculty of Science, The Australian National University, Canberra, Australia4

Received 29 March 2004/ Returned for modification 4 May 2004/ Accepted 5 May 2004

A series of alkoxylated and hydroxylated chalcones previously reported to have antiplasmodial activities in vitro were investigated for their effects on the new permeation pathways induced by the malaria parasite in the host erythrocyte membrane. Of 21 compounds with good antiplasmodial activities (50% inhibitory concentrations [IC50s], ≤20 µM), 8 members were found to inhibit sorbitol-induced lysis of parasitized erythrocytes to a significant extent (≤40% of control values) at a concentration (10 µM) that was close to their antiplasmodial IC50s. Qualitative structure-activity analysis suggested that activity was governed to a greater extent by a substitution on ring B than on ring A of the chalcone template. Most of the active compounds had methoxy or dimethoxy groups on ring B. Considerable variety was permitted on ring A in terms of the electron-donating or -withdrawing property. Lipophilicity did not appear to be an important determinant for activity. Although they are not exceptionally potent as inhibitors (lowest IC50, 1.9 µM), the chalcones compare favorably with other more potent inhibitors in terms of their selective toxicities against plasmodia and their neutral character.

* Corresponding author. Mailing address: Department of Pharmacy, National University of Singapore, Science Dr. 4, Republic of Singapore. Phone: 65-68742654. Fax: 65-67791554. phagoml{at}nus.edu.sg.

Antimicrobial Agents and Chemotherapy, September 2004, p. 3241-3245, Vol. 48, No. 9
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.9.3241-3245.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Bhattacharya, A., Mishra, L. C., Bhasin, V. K. (2008). In Vitro Activity of Artemisinin in Combination with Clotrimazole or Heat-treated Amphotericin B against Plasmodium falciparum. Am J Trop Med Hyg 78: 721-728 [Abstract] [Full Text]  
  • Kang, M., Lisk, G., Hollingworth, S., Baylor, S. M., Desai, S. A. (2005). Malaria Parasites Are Rapidly Killed by Dantrolene Derivatives Specific for the Plasmodial Surface Anion Channel. Mol. Pharmacol. 68: 34-40 [Abstract] [Full Text]  


Copyright © 2009 by the American Society for Microbiology.   For an alternate route to Journals.ASM.org, visit: http://intl-journals.asm.org | More Info»