Partition of Amphiphilic Molecules to Lipid Bilayers by ITC: LowAffinity Solutes

SAMELO J; MORA M.J.; GRANERO G.E.; MORENO J

ACS Omega

ACS Publications-American Chemical Society

Año: 2017 vol. 2 p. 6863 - 6863

2470-1343

protocol is developed to allow the accurate characterizationof partition to lipid bilayers for solutes with low affinity, using isothermaltitration calorimetry. The methodology proposed is suitable for studies usingcomplex membranes, such as intact biomembranes or whole cells. In themethod developed, the association is characterized at increasing soluteconcentrations. This allows the characterization of solute partition intounperturbed membranes, as well as effects induced by high soluteconcentrations. Most druglike molecules are expected to interact with lowto-moderateaffinity with relevant cell membranes. This is due to both theneed for a relatively high aqueous solubility of the drug and the poor bindingproperties of the cell membranes. The methodology is applied to characterizethe interaction of antibiotic Rifampicin with 1-palmitoyl-2-oleoyl-sn-glycero3-phosphocholineand with lipid bilayers representative of bacterialmembranes.