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Roxithromycin potentiates the effects of chloroquine and mefloquine on multidrug-resistant Plasmodium falciparum in vitro

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 (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)
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author
organization
publishing date
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
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
2013-05-14 15:06:44
date last changed
2017-01-01 04:19:59
@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},
  volume       = {115},
  year         = {2007},
}