Please use this identifier to cite or link to this item: https://doi.org/10.3390/molecules23102635
Title: Near infrared fluorophore-tagged chloroquine in plasmodium falciparum diagnostic imaging
Authors: Chan, L.Y
Teo, J.D.W
Tan, K.S.-W 
Sou, K
Kwan, W.L
Lee, C.-L.K
Keywords: antimalarial agent
chloroquine
cyclobutane derivative
fluorescent dye
phenol derivative
squaraine
blood
chemical structure
chemistry
confocal microscopy
drug effect
drug resistance
human
IC50
molecular imaging
parasitology
Plasmodium falciparum
Antimalarials
Blood
Chloroquine
Cyclobutanes
Drug Resistance
Fluorescent Dyes
Humans
Inhibitory Concentration 50
Microscopy, Confocal
Molecular Imaging
Molecular Structure
Phenols
Plasmodium falciparum
Issue Date: 2018
Publisher: MDPI AG
Citation: Chan, L.Y, Teo, J.D.W, Tan, K.S.-W, Sou, K, Kwan, W.L, Lee, C.-L.K (2018). Near infrared fluorophore-tagged chloroquine in plasmodium falciparum diagnostic imaging. Molecules 23 (10) : 2635. ScholarBank@NUS Repository. https://doi.org/10.3390/molecules23102635
Rights: Attribution 4.0 International
Abstract: Chloroquine was among the first of several effective drug treatments against malaria until the onset of chloroquine resistance. In light of diminished clinical efficacy of chloroquine as an antimalarial therapeutic, there is potential in efforts to adapt chloroquine for other clinical applications, such as in combination therapies and in diagnostics. In this context, we designed and synthesized a novel asymmetrical squaraine dye coupled with chloroquine (SQR1-CQ). In this study, SQR1-CQ was used to label live Plasmodium falciparum (P. falciparum) parasite cultures of varying sensitivities towards chloroquine. SQR1-CQ positively stained ring, mature trophozoite and schizont stages of both chloroquine-sensitive and chloroquine-resistant P. falciparum strains. In addition, SQR1-CQ exhibited significantly higher fluorescence, when compared to the commercial chloroquine-BODIPY (borondipyrromethene) conjugate CQ-BODIPY. We also achieved successful SQR1-CQ labelling of P. falciparum directly on thin blood smear preparations. Drug efficacy experiments measuring half-maximal inhibitory concentration (IC50) showed lower concentration of effective inhibition against resistant strain K1 by SQR1-CQ compared to conventional chloroquine. Taken together, the versatile and highly fluorescent labelling capability of SQR1-CQ and promising preliminary IC50 findings makes it a great candidate for further development as diagnostic tool with drug efficacy against chloroquine-resistant P. falciparum. © 2018 by the Authors.
Source Title: Molecules
URI: https://scholarbank.nus.edu.sg/handle/10635/179016
ISSN: 14203049
DOI: 10.3390/molecules23102635
Rights: Attribution 4.0 International
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