TY - JOUR AU - Leba, L.-J. AU - Popovici, J. AU - Estevez, Y. AU - Pelleau, S. AU - Legrand, E. AU - Musset, L. AU - Duplais, C. PY - 2017// TI - Antiplasmodial activities of dyes against Plasmodium falciparum asexual and sexual stages: Contrasted uptakes of triarylmethanes Brilliant green, Green S (E142), and Patent Blue V (E131) by erythrocytes T2 - International Journal for Parasitology: Drugs and Drug Resistance JO - International Journal for Parasitology: Drugs and Drug Resistance SP - 314 EP - 320 VL - 7 IS - 3 KW - Antimalarial dyes KW - Brilliant green KW - Drug uptake KW - Food dyes KW - Transmission blocking KW - Triarylmethanes N2 - The search for safe antimalarial compounds acting against asexual symptom-responsible stages and sexual transmission-responsible forms of Plasmodium species is one of the major challenges in malaria elimination programs. So far, among current drugs approved for human use, only primaquine has transmission-blocking activity. The discovery of small molecules targeting different Plasmodium falciparum life stages remains a priority in antimalarial drug research. In this context, several independent studies have recently reported antiplasmodial and transmission-blocking activities of commonly used stains, dyes and fluorescent probes against P. falciparum including chloroquine-resistant isolates. Herein we have studied the antimalarial activities of dyes with different scaffold and we report that the triarylmethane dye (TRAM) Brilliant green inhibits the growth of asexual stages (IC50 ≤ 2 μM) and has exflagellation-blocking activity (IC50 ≤ 800 nM) against P. falciparum reference strains (3D7, 7G8) and chloroquine-resistant clinical isolate (Q206). In a second step we have investigated the antiplasmodial activities of two polysulfonated triarylmethane food dyes. Green S (E142) is weakly active against P. falciparum asexual stage (IC50 ≃ 17 μM) whereas Patent Blue V (E131) is inactive in both antimalarial assays. By applying liquid chromatography techniques for the culture supernatant analysis after cell washings and lysis, we report the detection of Brilliant green in erythrocytes, the selective uptake of Green S (E142) by infected erythrocytes, whereas Patent Blue V (E131) could not be detected within non-infected and 3D7-infected erythrocytes. Overall, our results suggest that two polysulfonated food dyes might display different affinity with transporters or channels on infected RBC membrane. © 2017 The Authors UR - https://www.scopus.com/inward/record.uri?eid=2-s2.0-85028713282&doi=10.1016%2fj.ijpddr.2017.07.002&partnerID=40&md5=9d02a984bb6b24fd30a592ffba582854 L1 - http://php.ecofog.gf/refbase/files/leba/2017/765_Leba_etal2017.pdf UR - http://dx.doi.org/10.1016/j.ijpddr.2017.07.002 N1 - Export Date: 18 September 2017 ID - Leba_etal2017 ER -