IIBYT   23944
INSTITUTO DE INVESTIGACIONES BIOLOGICAS Y TECNOLOGICAS
Unidad Ejecutora - UE
congresos y reuniones científicas
Título:
EFFECT OF THUJONE AND DIHYDROCARVONE ON PHOSPHOLIPID MONOLAYER
Autor/es:
MARIA E MARIANI; MARIELA SANCHEZ-BORZONE; DANIEL A. GARCIA
Lugar:
Santiago del Estero
Reunión:
Congreso; XLIV REUNION ANUAL DE LA SOCIEDAD ARGENTINA DE BIOFISICA (SAB).; 2015
Institución organizadora:
Sociedad Argentina de Biofisica
Resumen:
ResumenDihydropyrimidines (DHPMs) derivatives have a signficant role in medicinal chemistry for various pharmacological activities, such as anticancer, antibacterial, antifungal, antihypertensive, antitubercular, antimalarial, antiviral, and anti-inflammatory activities. The high hydrophobicity of DHPMs suggests that many of these effects could involve their interaction with biological membranes modulating the supramolecular organization of the substrate summarized in the concept of ?interfacial quality?. The purpose of the present study was to determine the ability of two DHPM analogs, -1 and -6, which demonstrated larvicide and repellent activity against Anopheles arabiensis, to interact with artificial model membranes. The effects on the microviscosity of dpPC liposomes and on the properties of dpPC monomolecular films were studied. In this context, both compounds were able to modify the membrane microviscosity measure by fluorescence anisotropy of DPH and TMA-DPH. The DHPMs decreased the membrane fluidity at different depths and at different membrane phase states, as revealed by both fluorescent probes. This effect was more noticeable with TMA-DPH indicating that the presence of DHPMs between lipid molecules would induce an enhancement of the intermolecular interaction, increasing the molecular order throughout the bilayer thickness. The compression isotherms (π/A isotherms) performed in the presence of DHPMs in the subphase, indicated that both compounds were able to modify the interfacial characteristics of dpPC, causing the expansion of the monolayer. The compressibility modulus clearly showed that DHPMs induced the disappearance of dpPC phase transition between LE and LC states and the reduction of the elasticity of condensed phases (LC). Moreover, both compounds showed ability to penetrate in lipid monolayers with a πcutoff= 37 mN/m, indicating that both compounds are able to penetrate natural membranes and modify their properties.