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• W2007925264 abstract "Abstract This study was designed to test the hypothesis that there exists a correlation between the ability of lipophilic drugs to mediate the reversal of multidrug-resistance (MDR) by interacting with the membrane phospholipids and the metabolic level in tissues. The permeation properties of five MDR-modulators were studied by quantifying their ability to induce the leakage of Sulphan blue through unilamellar liposomes, over the temperature range 27–42°C. The dye leakage induced by a non-ionic detergent (Triton X-100), two calcium blockers (diltiazem and verapamil) and two antiparasitic agents (thioacridine derivative and mepacrine) was temperature-dependent. The permeation process was a co-operative one (1.1 &lt; Hill coefficient &lt; 7.5) and the permeation doses inducing 50% dye leakage (PD50) were 1.5–14.9 mM. The permeation ability of the MDR-modulators (log(1/PD50)) decreased significantly as the net electric charge (z) increased. The passive dye leakage (ΔG &lt; 0) was found to be an endothermic process (ΔH &gt; 0), favoured by an increase in the membrane disorder (ΔS &gt; 0). The apparent enthalpy factor (ΔH50) associated with 50% dye leakage increased with the net electric charge of the compound, and this energetically non-favoured event was entirely offset by the concomitant increase in the entropy factor (ΔS50). The apparent permeation enthalpy (ΔH50) and entropy (ΔS50) showed the lowest values for Triton X-100 (ΔH50 = 7.1 ± 0.53 kJ mol−1, ΔS50=76.9 ± 1.86 J mol−1 K−1), and the highest values for mepacrine (ΔH50 = 79.5±3.80 kJ mol−1, ΔS50 = 306.7 ± 5.97 J mol−1 K−1). When the temperature was increased from 27 to 42°C, the apparent Gibbs free energy (ΔG50) of the dye leakage induced by Triton X-100 decreased by less than 10% of the initial value, and that induced by mepacrine decreased by nearly 40%. The results provide evidence that in tissues with high metabolic levels and therefore high temperatures, MDR-reversal is likely to be enhanced via favourable drug-membrane interactions controlled by the electric charge of the modulators." @default.
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• W2007925264 date "2000-10-01" @default.
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• W2007925264 title "Thermal Dependence of Multidrug-resistant-modulator Efficiency: a Study in Anionic Liposomes" @default.
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• W2007925264 doi "https://doi.org/10.1211/0022357001777298" @default.
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