Table 1.
Efficacy of Lead Agents across Model Systems
Agent | FRT G542X TECC Gt (mS/cm2) (Mean ± SE) | FRT UGAC Dual-Luciferase Firefly/Renilla (Mean ± SD) | FRT G542X HRP RLU (Mean ± SE) | HBE G542X/ΔF508 HBE Ussing Chamber Isc (μA/cm2) (Mean ± SE) |
---|---|---|---|---|
Colchicine | 0.21 ± 0.0*† | 1.28 ± 0.0.008 | 36000 ± 1554* | 1.2 ± 0.2† |
Cyclohexamide | 0.13 ± 0.06‡§ | 1.81 ± 0.01 | 38171 ± 1618* | 3.4 ± 0.07§ |
Oxibendazole | 0.16 ± 0.005*|| | 1.34 ± 0.01 | 28150 ± 908.6¶ | 1.36 ± 0.04|| |
Pyronaridine tetraphosphate | 0.13 ± 0.08# | 1.1 ± 0.005 | 1091 ± 98.8 | 6.2 ± 0.3‡ |
Prednicarbate | 0.14 ± 0.02¶ | 0.89 ± 0.0034 | 10515 ± 870.2 | 4.9 ± 1.2# |
Escin | 0.20 ± 0.001* | 2.04 ± 0.02 | 57402 ± 2836* | 7.1 ± 0.3* |
Potassium paraamino benzoic acid | 0.14 ± 0‡|| | 1.44 ± 0.02 | 10811 ± 701.1 | 6.6 ± 1.2‡|| |
Doxorubicin | 0.11 ± 0.01 | 1.99 ± 0.007 | 26269 ± 1426¶ | 2.38 ± 0.14 |
Definition of abbreviations: FRT = Fischer rat thyroid; HBE = human bronchial epithelial; HRP = horseradish peroxidase; Isc = short circuit current; RLU = relative light units; TECC = transepithelial chloride conductance.
Assays included TECC (Gt; mean values ± SE; mS/cm2), dual-luciferase (Firefly/Renilla ratio; mean ± SD), and HRP-detected protein expression (RLU; mean ± SE), each using FRT cells; and Ussing chamber analysis using primary HBE cells (Isc; mean ± SE; μA/cm2). Unless indicated, these compounds were treated at 10 μM. Concentration = 10 μM unless otherwise indicated.
P < 0.0001.
1 μM.
P < 0.01.
3 μM.
30 μM.
P < 0.001.
P < 0.05.