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Fig. 1 | Malaria Journal

Fig. 1

From: Proguanil and cycloguanil are organic cation transporter and multidrug and toxin extrusion substrates

Fig. 1

Inhibition of OCT1 and OCT2 by anti-malarials. The inhibition of OCT1 (a) and OCT2 (b) by eleven anti-malarials (AQ, ART, ATO, CQ, DHA, LUM, MQ, PQ, PG, PM, and QN) at a concentration of 50 μM (except for ATO, LUM: 25 μM, and QN: 100 μM) was studied using 10 μM ASP as a substrate during 10 min incubation at 37 °C. Percentage of ASP uptake was expressed relative to solvent controls, which were fixed at 100%. Anti-malarials showing an inhibitory potential > 67% (grey bars) were selected for IC50 determination. Concentration-dependent inhibition of OCT2-mediated ASP (10 μM) uptake during 10 min incubation at 37 °C resulted in IC50 values of 11 μM (95% CI 6–22 µM), 13 μM (95% CI 10–17 µM), 1.6 μM (95% CI 1.0–2.5 µM), and 3.4 μM (95% CI 1.1–11 µM) for AQ (c), PG (d), PM (e), and QN (f), respectively. *p < 0.05, ***p < 0.001

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