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. Author manuscript; available in PMC: 2015 Jan 3.
Published in final edited form as: Chembiochem. 2013 Nov 29;15(1):157–169. doi: 10.1002/cbic.201300565

Figure 2. Inhibition of P-gp-mediated Calcein-AM transport by various derivatives.

Figure 2

Figure 2

HeLa cells transduced with wild-type P-gp BacMam virus were evaluated for transport function using calcein-AM (0.5 μM) as described in Experimental Section. A) The reversal of calcein-AM transport was carried out in the presence of solvent DMSO (control, solid line), or in the presence of various synthesized derivatives at 5 μM. The reversal by monomer (5) (dashed line), dimer (9) (complex line), linear trimer (13) (long dashed line), and cyclic trimer (QZ59S-SSS, 17) (dotted line) are compared with tariquidar (1 μM), which is a known inhibitor of P-gp (tinted filled trace). B) BacMam P-gp transduced HeLa cells were assayed for calcein-AM transport in the presence of increasing concentrations of monomer (5) (filled squares), dimer (9) (filled triangles), linear trimer (13) (filled inverted triangles) and cyclic trimer (QZ59S-SSS, 17) (filled circles). The transport in the absence of these compounds was taken as 100%. The results are represented as an average of two independent experiments. The IC50 value for the dimer (9) was 20 μM and that for both linear trimer (13) and cyclic trimer (17) was 1.5 μM.