↓ Skip to main content

Contrasting Ex Vivo Efficacies of “Reversed Chloroquine” Compounds in Chloroquine-Resistant Plasmodium falciparum and P. vivax Isolates

Overview of attention for article published in Antimicrobial Agents and Chemotherapy, July 2015
Altmetric Badge

Mentioned by

twitter
2 X users

Citations

dimensions_citation
12 Dimensions

Readers on

mendeley
37 Mendeley
You are seeing a free-to-access but limited selection of the activity Altmetric has collected about this research output. Click here to find out more.
Title
Contrasting Ex Vivo Efficacies of “Reversed Chloroquine” Compounds in Chloroquine-Resistant Plasmodium falciparum and P. vivax Isolates
Published in
Antimicrobial Agents and Chemotherapy, July 2015
DOI 10.1128/aac.01048-15
Pubmed ID
Authors

Grennady Wirjanata, Boni F. Sebayang, Ferryanto Chalfein, Prayoga, Irene Handayuni, Rintis Noviyanti, Enny Kenangalem, Jeanne Rini Poespoprodjo, Steven J. Burgess, David H. Peyton, Ric N. Price, Jutta Marfurt

Abstract

Chloroquine (CQ) has been the mainstay of malaria treatment for more than 60 years. However, the emergence and spread of CQ resistance now restricts its use to only a few malaria endemic areas. The aim of the present study was to investigate whether a novel combination of a CQ-like moiety and an imipramine-like pharmacophore can reverse CQ resistance ex vivo.Between March-October 2011 and January-September 2013, two RCQ compounds (PL69 and PL106) were tested against multidrug resistant field isolates of P. falciparum (n=41) and P. vivax (n=45) in Papua (Indonesia) using a modified ex vivo schizont maturation assay.The RCQ compounds showed high efficacy against both CQ resistant P. falciparum and P. vivax field isolates. For P. falciparum, the median IC50 values 23.2 nM for PL69 and 26.6 nM for PL106 compared to 79.4 nM for unmodified CQ (p<0.001 and p=0.036, respectively). The corresponding figures for P. vivax were 19.0 nM, 60.0 nM and 60.9 nM (p<0.001 and p=0.018, respectively). There was a significant correlation between IC50s of CQ and PL 69 (rs=0.727, p<0.001) and PL106 (rs=0.830, p<0.001) in P. vivax, but not in P. falciparum. Both RCQs were equally active against ring and trophozoite stages of P. falciparum, but in P. vivax, PL69 and PL 106 showed less potent activity against trophozoite stages (median IC50=130.2 and 172.5 nM) compared to ring stages (median IC50=17.6 and 91.3 nM).RCQ compounds have enhanced ex vivo activity against CQ resistant clinical isolates of P. falciparum and P. vivax, suggesting the potential use of reversal agents in anti-malarial drug development. Inter-species differences in RCQ compound activity may indicate differences in CQ pharmacokinetics between the two Plasmodium species.

X Demographics

X Demographics

The data shown below were collected from the profiles of 2 X users who shared this research output. Click here to find out more about how the information was compiled.
Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 37 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United Kingdom 1 3%
Unknown 36 97%

Demographic breakdown

Readers by professional status Count As %
Researcher 7 19%
Student > Bachelor 6 16%
Student > Master 4 11%
Lecturer 3 8%
Student > Ph. D. Student 2 5%
Other 8 22%
Unknown 7 19%
Readers by discipline Count As %
Medicine and Dentistry 6 16%
Immunology and Microbiology 5 14%
Pharmacology, Toxicology and Pharmaceutical Science 4 11%
Biochemistry, Genetics and Molecular Biology 3 8%
Environmental Science 2 5%
Other 6 16%
Unknown 11 30%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 19 May 2016.
All research outputs
#20,655,488
of 25,371,288 outputs
Outputs from Antimicrobial Agents and Chemotherapy
#13,974
of 15,580 outputs
Outputs of similar age
#201,811
of 276,215 outputs
Outputs of similar age from Antimicrobial Agents and Chemotherapy
#190
of 267 outputs
Altmetric has tracked 25,371,288 research outputs across all sources so far. This one is in the 10th percentile – i.e., 10% of other outputs scored the same or lower than it.
So far Altmetric has tracked 15,580 research outputs from this source. They typically receive more attention than average, with a mean Attention Score of 8.2. This one is in the 5th percentile – i.e., 5% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 276,215 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 14th percentile – i.e., 14% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 267 others from the same source and published within six weeks on either side of this one. This one is in the 19th percentile – i.e., 19% of its contemporaries scored the same or lower than it.