Roxithromycin potentiates the effects of chloroquine and mefloquine on multidrug-resistant Plasmodium falciparum in vitro
(2007) In Experimental Parasitology 115(4). p.387-392- Abstract
- Chloroquine (CQ) and mefloquine (MQ) are no longer potent antimalarial drugs due to the emergence of resistant Plasmodium falciparum. Combination therapy has become the standard for many regimes in overcoming drug resistance. Roxithromycin (ROM), a known p-glycoprotein inhibitor, is reported to have antimalarial activity and it is hoped it will potentiate the effects of both CQ/MQ and reverse CQ/MQ-resistance. We assayed the effects of CQ and MQ individually and in combination with ROM on synchronized P. falciparum (Dd2 strain) cultures. The IC(50) values of CQ and MQ were 60.0+/-5.0 and 16.0+/-3.0 ng/ml; these were decreased substantially when combined with ROM. Isobolograms indicate that CQ-ROM combinations were relatively more... (More)
- Chloroquine (CQ) and mefloquine (MQ) are no longer potent antimalarial drugs due to the emergence of resistant Plasmodium falciparum. Combination therapy has become the standard for many regimes in overcoming drug resistance. Roxithromycin (ROM), a known p-glycoprotein inhibitor, is reported to have antimalarial activity and it is hoped it will potentiate the effects of both CQ/MQ and reverse CQ/MQ-resistance. We assayed the effects of CQ and MQ individually and in combination with ROM on synchronized P. falciparum (Dd2 strain) cultures. The IC(50) values of CQ and MQ were 60.0+/-5.0 and 16.0+/-3.0 ng/ml; these were decreased substantially when combined with ROM. Isobolograms indicate that CQ-ROM combinations were relatively more synergistic (mean FICI 0.70) than MQ-ROM (mean FICI 0.85) with their synergistic effect at par with CQ-verapamil (VRP) (mean FICI 0.64) and MQ-VRP (mean FICI 0.60) combinations. We conclude that ROM potentiates the CQ/MQ response on multidrug-resistant P. falciparum. (Less)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/1140034
- author
- Tan Grahn, Hooi Min LU ; Khairul, M F M ; Low, J H ; Che Nasriyyah, C H ; A'shikin, A Noor ; Norazmi, M N ; Ravichandran, M and Raju, S S
- organization
- publishing date
- 2007
- type
- Contribution to journal
- publication status
- published
- subject
- in
- Experimental Parasitology
- volume
- 115
- issue
- 4
- pages
- 387 - 392
- publisher
- Elsevier
- external identifiers
-
- pmid:17118354
- scopus:33846621061
- pmid:17118354
- ISSN
- 0014-4894
- DOI
- 10.1016/j.exppara.2006.10.004
- language
- English
- LU publication?
- yes
- id
- 1461fde5-f11f-4446-9e78-929852c6cba1 (old id 1140034)
- alternative location
- http://www.ncbi.nlm.nih.gov/pubmed/17118354
- date added to LUP
- 2016-04-01 11:33:29
- date last changed
- 2022-01-26 07:03:38
@article{1461fde5-f11f-4446-9e78-929852c6cba1, abstract = {{Chloroquine (CQ) and mefloquine (MQ) are no longer potent antimalarial drugs due to the emergence of resistant Plasmodium falciparum. Combination therapy has become the standard for many regimes in overcoming drug resistance. Roxithromycin (ROM), a known p-glycoprotein inhibitor, is reported to have antimalarial activity and it is hoped it will potentiate the effects of both CQ/MQ and reverse CQ/MQ-resistance. We assayed the effects of CQ and MQ individually and in combination with ROM on synchronized P. falciparum (Dd2 strain) cultures. The IC(50) values of CQ and MQ were 60.0+/-5.0 and 16.0+/-3.0 ng/ml; these were decreased substantially when combined with ROM. Isobolograms indicate that CQ-ROM combinations were relatively more synergistic (mean FICI 0.70) than MQ-ROM (mean FICI 0.85) with their synergistic effect at par with CQ-verapamil (VRP) (mean FICI 0.64) and MQ-VRP (mean FICI 0.60) combinations. We conclude that ROM potentiates the CQ/MQ response on multidrug-resistant P. falciparum.}}, author = {{Tan Grahn, Hooi Min and Khairul, M F M and Low, J H and Che Nasriyyah, C H and A'shikin, A Noor and Norazmi, M N and Ravichandran, M and Raju, S S}}, issn = {{0014-4894}}, language = {{eng}}, number = {{4}}, pages = {{387--392}}, publisher = {{Elsevier}}, series = {{Experimental Parasitology}}, title = {{Roxithromycin potentiates the effects of chloroquine and mefloquine on multidrug-resistant Plasmodium falciparum in vitro}}, url = {{http://dx.doi.org/10.1016/j.exppara.2006.10.004}}, doi = {{10.1016/j.exppara.2006.10.004}}, volume = {{115}}, year = {{2007}}, }