| Full text | |
| Author(s): |
Londero, Vinicius S.
;
Rosa, Matheus E.
;
Baitello, Joao B.
;
Costa-Silva, Thais A.
;
Cruz, Lucas Monteiro S.
;
Tempone, Andre G.
;
Caseli, Luciano
;
Lago, Joao Henrique G.
Total Authors: 8
|
| Document type: | Journal article |
| Source: | BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES; v. 1865, n. 7, p. 9-pg., 2023-10-01. |
| Abstract | |
As part of our ongoing studies involving the discovery of new natural prototypes with antiprotozoal activity against Trypanosoma cruzi from Brazilian plant species, the chromatographic fractionation of hexane extract from leaves of Nectandra barbellata afforded one new pseudo-disesquiterpenoid, barbellatanic acid. The structure of this compound was elucidated by NMR and HR-ESIMS data analysis. Barbellatanic acid displayed a trypanocidal effect with IC50 of 13.2 mu M to trypomastigotes and no toxicity against NCTC cells (CC50 > 200 mu M), resulting in an SI value higher than 15.1. The investigation of the lethal mechanism of barbellatanic acid in trypomastigotes, using both fluorescence microscopy and spectrofluorimetric analysis, revealed a time-dependent permeation of the plasma membrane. Based on these results, this compound was incorporated in cellular membrane models built with lipid Langmuir monolayers. The interaction of barbellatanic acid with the models was inferred by tensiometric, rheological, spectroscopical, and morphological techniques, which showed that this compound altered the thermodynamic, viscoelastic, structural, and morphological properties of the film. Taking together, these results could be employed when this prodrug interacts with lipidic interfaces, such as protozoa membranes or liposomes for drug delivery systems. (AU) | |
| FAPESP's process: | 22/03736-7 - 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 |
| 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: | 21/02789-7 - Search for bioactive metabolites with antiparasitic action in plant species from Atlantic Forest and Cerrado regions - a chemical, phenotypical, and metabolomic approach |
| Grantee: | João Henrique Ghilardi Lago |
| Support Opportunities: | BIOTA-FAPESP Program - Regular Research Grants |
| FAPESP's process: | 21/15084-1 - Interaction of natural acetogenins with biological activity in membrane models at the air-water interface |
| Grantee: | Matheus Elias Rosa |
| Support Opportunities: | Scholarships in Brazil - Doctorate (Direct) |
| FAPESP's process: | 17/17044-1 - Biomolecules from Nectandra barbellata Coe-Teixeira (Lauraceae): use of a sustainable alternative method for extraction, molecular characterization and evaluation of antiparasitic potential |
| Grantee: | Vinicius Silva Londero |
| Support Opportunities: | Scholarships in Brazil - Doctorate |