Studies on interaction of 1,2,3,4- tetrahydropyrimido[1,2-]benzimidazole-2-оn with model lipid membranes
Abstract
The molecular mechanisms of interaction of the compound for pharmacological correction of insulin-resistance - 1,2,3,4-tetrahydropyrimido[1,2-α]benzimidazole-2-on (ТHPBI) with phosphatidylcholine liposomes (PC) have been investigated by fluorescent spectroscopy method. The partition coefficient of ТHPBI into the lipid phase Кр = 1810±300. The binding parameters were obtained using the Langmuir model: Ка=0,071мкМ-1, the number of binding sites n = 11.2, maximal change of absorption of ТHPBI upon binding to the liposomes Аmax=0,29±0,011. The partition model is appeared to be more adequate to describe THPBI binding and insertion into PC. ТHPBI was found to exert no influence on the transversal distribution of pyrene monomers in a membrane and polarity of the hydrophobic region of the bilayer, but affect the packing density of lipid molecules. The fluorescence quenching of probes JC-1 and АNS by ТHPBI resulted was suggested to result from the increased polarity of the probe microenvironment.
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