Uptake of a fluorescently tagged chloroquine analogue is reduced in CQ-resistant compared to CQ-sensitive Plasmodium falciparum parasites.

Antimalarials / metabolism Biological Transport Chloroquine / analogs & derivatives Drug Resistance Fluorescent Dyes / metabolism Plasmodium falciparum / drug effects
Antimalarial drugs Chloroquine resistant Chloroquine sensitive Live cell imaging LynxTag-CQGREEN Malaria

Journal

Malaria journal
ISSN: 1475-2875
Titre abrégé: Malar J
Pays: England
ID NLM: 101139802

Informations de publication

Date de publication:
07 Oct 2019
Historique:
received: 14 06 2019
accepted: 28 09 2019
entrez: 9 10 2019
pubmed: 9 10 2019
medline: 29 1 2020
Statut: epublish

Résumé

Chloroquine (CQ) was the drug of choice for decades in the treatment of falciparum malaria until resistance emerged. CQ is suggested to accumulate in the parasite's digestive vacuole (DV), where it unfolds its anti-malarial properties. Discrepancies of CQ accumulation in CQ-sensitive (CQS) and CQ-resistant (CQR) strains are thought to play a significant role in drug susceptibility. Analysis of CQ transport and intracellular localization using a fluorescently tagged CQ analogue could provide much needed information to distinguish susceptible from resistant parasite strains. The fluorescently tagged CQ analogue LynxTag-CQ™ IC In CQS strains, twofold higher IC Although fluorescence of CQ

Sections du résumé

BACKGROUND BACKGROUND
Chloroquine (CQ) was the drug of choice for decades in the treatment of falciparum malaria until resistance emerged. CQ is suggested to accumulate in the parasite's digestive vacuole (DV), where it unfolds its anti-malarial properties. Discrepancies of CQ accumulation in CQ-sensitive (CQS) and CQ-resistant (CQR) strains are thought to play a significant role in drug susceptibility. Analysis of CQ transport and intracellular localization using a fluorescently tagged CQ analogue could provide much needed information to distinguish susceptible from resistant parasite strains. The fluorescently tagged CQ analogue LynxTag-CQ™
METHODS METHODS
IC
RESULTS RESULTS
In CQS strains, twofold higher IC
CONCLUSION CONCLUSIONS
Although fluorescence of CQ

Identifiants

DOI: 10.1186/s12936-019-2980-y PMID: 31590674 PMC: PMC6781371
pubmed: 31590674
doi: 10.1186/s12936-019-2980-y
pii: 10.1186/s12936-019-2980-y
pmc: PMC6781371
doi:

Substances chimiques

Antimalarials 0
Fluorescent Dyes 0
Chloroquine 886U3H6UFF

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

342

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Auteurs

Sarah J Reiling (SJ)

Institute of Parasitology, McGill University, Ste. Anne de Bellevue, Montreal, QC, H9X-3V9, Canada.

Petra Rohrbach (P)

Institute of Parasitology, McGill University, Ste. Anne de Bellevue, Montreal, QC, H9X-3V9, Canada. petra.rohrbach@mcgill.ca.
ORCID: 0000-0002-7887-984X

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiparasitaires › Antiprotozoaires › Antipaludiques › Uptake of a fluorescently tagged chloroquine...
questionsmedicales.fr › Métabolisme › Transport biologique › Uptake of a fluorescently tagged chloroquine...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Quinoléines › Aminoquinoléines › Chloroquine › Uptake of a fluorescently tagged chloroquine...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Résistance aux substances › Uptake of a fluorescently tagged chloroquine...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Indicateurs et réactifs › Luminescents › Colorants fluorescents › Uptake of a fluorescently tagged chloroquine...
questionsmedicales.fr › Eucaryotes › Alveolata › Apicomplexa › Haemosporida › Plasmodium › Plasmodium falciparum › Uptake of a fluorescently tagged chloroquine...