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    Antitrypanosomal activity of epi-polygodial from Drimys brasiliensis and its effects in cellular membrane models at the air-water interface

    Year: 2019

    Journal: Bioorganic Chem., Volume 84, MAR, page 186–191

    Authors: Guimaraes Goncalves, Giulia Elisa; Morais, Thiago Rahal; Gomes, Kaio de Souza; Costa-Silva, Thais Alves; Tempone, Andre Gustavo; Ghilardi Lago, Joao Henrique; Caseli, Luciano

    Organizations: FAPESPFundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2018/07885-1, 2015/23446-0, 2015/23403-9, 2013/14262-7]; CNPqNational Council for Scientific and Technological Development (CNPq) [400896/2016-8]; CAPESCAPES

    Keywords: Epi-polygodial; Trypsmosoma cruzi; Langmuir monolayers; Air-water interface

    Epi-polygodial, a drimane sesquiterpene was isolated from Drimys brasiliensis (Winteraceae). This compound demonstrated high parasite selectivity towards Trypanosoma cruzi trypomastigotes (IC50 = 5.01 mu M) with a selectivity index higher than 40. These results were correlated with the effects observed when this compound was incorporated in cellular membrane models of protozoans, represented by Langmuir monolayers of dipalmitoylphosphoethanolamine (DPPE). Surface pressure-area isotherms showed that epi-polygodial expands DPPE monolayers at higher areas and condenses them at lower areas, which was attributed to the preferential interaction with the polar heads of the lipid. This mechanism of action could be corroborated with Polarization-Modulation Reflection-Absorption Spectroscopy and Brewster Angle Microscopy. These results pointed to the fact that the interaction of epi-polygodial with DPPE monolayers at the air-water interface affects the physical chemical properties of the mixed film, which may be important to comprehend the interaction of this drug with cellular membranes at the molecular level.
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