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Fig. 3 | Malaria Journal

Fig. 3

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

Fig. 3

PG and CG uptake by MATE1 and MATE2-K. Uptake of 100 µM PG for 5 min for MATE1 (430 ± 110 pmol/mg/min) and MATE2-K (360 ± 90 pmol/mg/min) compared to the control (300 ± 40 pmol/mg/min) in HEK293 transduced cells (a). Following co-transduction of eYFP and OCT1, after measuring uptake of 1 μM PG during 1 min incubation, PG was taken up for 850 ± 60% as compared to eYFP control cells. MATE1 was not capable of reducing OCT1-mediated PG uptake by exporting this anti-malarial, however, MATE2-K reduced PG uptake to 470 ± 80% of control, which is a relative decrease of 44% in uptake (b). Uptake of 100 µM CG for 5 min was significantly higher for MATE1 (40 ± 9 pmol/mg/min) and MATE2-K (56 ± 15 pmol/mg/min) compared to the control (11.8 ± 0.9 pmol/mg/min) (c). *p < 0.05, **p < 0.01, ***p < 0.001

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