Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1016/j.msec.2020.110943 http://hdl.handle.net/11449/201686 |
Resumo: | 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. |
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Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranesArtepillin CGreen propolisGUVsModel membranesOropharyngeal carcinoma cellsArtepillin 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.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)São Paulo State University (UNESP) School of Sciences Humanities and LanguagesSão Paulo State University (UNESP) School of Technology and Applied SciencesSão Paulo State University (UNESP) School of Sciences Humanities and LanguagesSão Paulo State University (UNESP) School of Technology and Applied SciencesFAPESP: 2013/14262-7FAPESP: 2016/13280-0CNPq: 403713/2016-1Universidade Estadual Paulista (Unesp)Kobal, Mirella B. [UNESP]Pazin, Wallance M. [UNESP]Bistaffa, Maria J. [UNESP]Constantino, Carlos J.L. [UNESP]Toledo, Karina A. [UNESP]Aoki, Pedro H.B. [UNESP]2020-12-12T02:39:06Z2020-12-12T02:39:06Z2020-07-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1016/j.msec.2020.110943Materials Science and Engineering C, v. 112.1873-01910928-4931http://hdl.handle.net/11449/20168610.1016/j.msec.2020.1109432-s2.0-85083279560Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengMaterials Science and Engineering Cinfo:eu-repo/semantics/openAccess2024-06-19T12:44:51Zoai:repositorio.unesp.br:11449/201686Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T23:08:31.476346Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes |
title |
Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes |
spellingShingle |
Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes Kobal, Mirella B. [UNESP] Artepillin C Green propolis GUVs Model membranes Oropharyngeal carcinoma cells |
title_short |
Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes |
title_full |
Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes |
title_fullStr |
Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes |
title_full_unstemmed |
Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes |
title_sort |
Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes |
author |
Kobal, Mirella B. [UNESP] |
author_facet |
Kobal, Mirella B. [UNESP] Pazin, Wallance M. [UNESP] Bistaffa, Maria J. [UNESP] Constantino, Carlos J.L. [UNESP] Toledo, Karina A. [UNESP] Aoki, Pedro H.B. [UNESP] |
author_role |
author |
author2 |
Pazin, Wallance M. [UNESP] Bistaffa, Maria J. [UNESP] Constantino, Carlos J.L. [UNESP] Toledo, Karina A. [UNESP] Aoki, Pedro H.B. [UNESP] |
author2_role |
author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) |
dc.contributor.author.fl_str_mv |
Kobal, Mirella B. [UNESP] Pazin, Wallance M. [UNESP] Bistaffa, Maria J. [UNESP] Constantino, Carlos J.L. [UNESP] Toledo, Karina A. [UNESP] Aoki, Pedro H.B. [UNESP] |
dc.subject.por.fl_str_mv |
Artepillin C Green propolis GUVs Model membranes Oropharyngeal carcinoma cells |
topic |
Artepillin C Green propolis GUVs Model membranes Oropharyngeal carcinoma cells |
description |
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. |
publishDate |
2020 |
dc.date.none.fl_str_mv |
2020-12-12T02:39:06Z 2020-12-12T02:39:06Z 2020-07-01 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.1016/j.msec.2020.110943 Materials Science and Engineering C, v. 112. 1873-0191 0928-4931 http://hdl.handle.net/11449/201686 10.1016/j.msec.2020.110943 2-s2.0-85083279560 |
url |
http://dx.doi.org/10.1016/j.msec.2020.110943 http://hdl.handle.net/11449/201686 |
identifier_str_mv |
Materials Science and Engineering C, v. 112. 1873-0191 0928-4931 10.1016/j.msec.2020.110943 2-s2.0-85083279560 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Materials Science and Engineering C |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808129494146351104 |