Crossregulation between the insertion of Hexadecylphosphocholine (miltefosine) into lipid membranes and their rheology and lateral structure

YENISLEIDY DE LAS MERCEDES ZULUETA DIAZ; MARIA LAURA FANANI

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2017 vol. 1859 p. 1891 - 1891

0005-2736

exadecylphosphocholine (HePC, miltefosine) is an alkylphospholipid used clinically for the topical treatment of cancer and against leishmaniasis. The mechanism of action of HePC, not yet elucidated, involves its insertion into the plasma membrane, affecting lipid homeostasis. It has also been proposed that HePC directly affects lipid raft stability and function in cell membranes. The present work deals with two main questions in the understanding of the action of HePC: the bases for membrane selectivity and as a membrane perturbator agent. We explored the interaction of HePC with lipid monolayers and bilayer vesicles, combining monolayer penetration experiments, Brewster angle microscopy and differential scanning calorimetry. Several membrane compositions were tested to explore different rheological conditions, phase states and lateral structures. Additionally, the kinetics between the soluble and the membrane form of HePC was explored. Our results showed an increase in elasticity ind