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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Evaluation of the effects in cellular membrane models of antitrypanosomal poly-thymolformaldehyde (PTF) using Langmuir monolayers

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Author(s):
Parolin, Giovana A. [1] ; Goncalves, Giulia E. G. [1] ; Costa-Silva, Thais A. [2] ; Tempone, Andre G. [3] ; Caseli, Luciano [1] ; Lago, Joao Henrique G. [2] ; Peres, Laura O. [1]
Total Authors: 7
Affiliation:
[1] Univ Fed Sao Paulo, Chem Dept, Lab Hybrid Mat, Diadema, SP - Brazil
[2] Fed Univ ABC, Ctr Nat & Human Sci, Lab Chem Biol, Santo Andre, SP - Brazil
[3] Adolfo Lutz Inst, Ctr Parasitol & Mycol, Sao Paulo, SP - Brazil
Total Affiliations: 3
Document type: Journal article
Source: BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES; v. 1863, n. 2 FEB 1 2021.
Web of Science Citations: 0
Abstract

The polymerization of bioactive compounds may be interesting because the supramolecular structures formed can boost biological action on microorganism membranes. In the present work, poly-thymolformaldehyde (PTF) activity, prepared by condensation of thymol and formaldehyde, was evaluated against trypomastigote forms of Trypanosoma cruzi and related with the physicochemical changes provided by the incorporation of the compound in protozoan cell membrane models. PTF exhibited an EC50 value of 23.4 mu g/mL and no toxicity against mammalian cells (CC50 > 200 mu g/mL). To understand the molecular action of PTF as an antiprotozoal candidate, this compound was incorporated in Langmuir monolayers of dipalmitoylphosphatidylglycerol (DPPG) as a model for parasite cell membranes. PTF shifted DPPG surface pressure-area isotherms to higher areas, indicating its incorporation in the lipid films. Additionally, it changed the thermodynamic, compressional, structural, and morphological properties of the floating monolayers, decreasing the collapse pressure, reducing the surface elasticity, and segregating molecules at the interface, forming domains with different reflectivities. Infrared spectroscopy showed that the lipid films with PTF presented an increased rate of gauche/all-trans conformers for the methylene groups from the acyl chains, indicating molecular disorder. Therefore, these results show that PTF alters the physicochemical properties of DPPG monolayers as a model for protozoa cell membranes, which can enhance the comprehension of the parasitic action of PTF against T. cruzi. (AU)

FAPESP's process: 18/22214-6 - Towards a convergence of technologies: from sensing and biosensing to information visualization and machine learning for data analysis in clinical diagnosis
Grantee:Osvaldo Novais de Oliveira Junior
Support Opportunities: Research Projects - Thematic Grants
FAPESP's process: 14/50869-6 - INCT 2014: on Organic Electronics
Grantee:Roberto Mendonça Faria
Support Opportunities: Research Projects - Thematic Grants
FAPESP's process: 18/07885-1 - Biomolecules from plant species of remnant areas of the Atlantic Forest and Cerrado to treat neglected tropical diseases - chemical and pharmacological aspects
Grantee:João Henrique Ghilardi Lago
Support Opportunities: BIOTA-FAPESP Program - Regular Research Grants
FAPESP's process: 18/18180-9 - 2018 MRS Fall Meetings & Exhibits
Grantee:Laura Oliveira Péres Philadelphi
Support Opportunities: Research Grants - Meeting - Abroad
FAPESP's process: 18/10279-6 - Selection and Optimization of New Drug Candidates for Leishmaniasis and Chagas Disease
Grantee:André Gustavo Tempone Cardoso
Support Opportunities: Regular Research Grants
FAPESP's process: 19/03239-0 - Nanostructured interfaces for the investigation of bioactive substances in cell membrane models and for the construction of optoelectronic devices
Grantee:Luciano Caseli
Support Opportunities: Regular Research Grants