Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes
| Autor: | Pedro H. B. Aoki, Wallance Moreira Pazin, Karina Alves Toledo, Maria Julia Bistaffa, Mirella B. Kobal, Carlos J. L. Constantino |
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| Přispěvatelé: | Universidade Estadual Paulista (Unesp) |
| Rok vydání: | 2020 |
| Předmět: |
Cell Membrane Permeability
Materials science Cell Survival Antineoplastic Agents Bioengineering 02 engineering and technology 010402 general chemistry 01 natural sciences Flow cytometry Biomaterials Hydrophobic effect Cell Line Tumor medicine Humans Cytotoxic T cell Viability assay Cytotoxicity Unilamellar Liposomes Artepillin C Oropharyngeal carcinoma cells Microscopy Confocal Phenylpropionates medicine.diagnostic_test Vesicle Cell Membrane GUVs Hydrogen-Ion Concentration 021001 nanoscience & nanotechnology 0104 chemical sciences Membrane Mechanics of Materials Biophysics Model membranes Efflux 0210 nano-technology Green propolis Hydrophobic and Hydrophilic Interactions |
| Zdroj: | Scopus Repositório Institucional da UNESP Universidade Estadual Paulista (UNESP) instacron:UNESP |
| ISSN: | 0928-4931 |
| Popis: | Made available in DSpace on 2020-12-12T02:39:06Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-07-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Artepillin C is the main compound present in propolis from Baccharis dracunculifolia, whose antitumor activity has been the focus of many studies. Herein, we shall investigate the Artepillin C mechanisms of action against cells derived from the oropharyngeal carcinoma (HEp-2). Cytotoxicity tests revealed that the concentrations of Artepillin C required to reduce cell viability by 50% (CC50) are dependent on the incubation time, decreasing from 40.7 × 10−5 mol/L to 15.7 × 10−5 mol/L and 9.05 × 10−5 mol/L considering 12, 24 and 48 h, respectively. Hydrophobic interactions on neutral species of Artepillin C induce aggregation over the HEp-2 plasma membrane, given the acid conditions of the cellular culture. Indeed, Langmuir monolayers mimicking cellular membranes of tumor cells revealed Artepillin C affinity to interact with 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) containing 20 mol% of 1,2-dipalmitoyl-sn-glychero-3-phosphoserine (DPPS), leading aggregation on giant unilamellar vesicles (GUVs) at pH 3.2. Moreover, leakage experiments on GUVs have shown that the presence of DPPS enhances the efflux of the fluorescent probe signaling the membrane permeabilization, which is the origin of the necrotic pathway triggered in HEp-2 cells, as observed by flow cytometry assays. São Paulo State University (UNESP) School of Sciences Humanities and Languages São Paulo State University (UNESP) School of Technology and Applied Sciences São Paulo State University (UNESP) School of Sciences Humanities and Languages São Paulo State University (UNESP) School of Technology and Applied Sciences FAPESP: 2013/14262-7 FAPESP: 2016/13280-0 CNPq: 403713/2016-1 |
| Databáze: | OpenAIRE |
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