Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption
Autor(a) principal: | |
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Data de Publicação: | 2022 |
Outros Autores: | , , , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.3390/membranes12030269 http://hdl.handle.net/11449/230485 |
Resumo: | Isobavachalcone (IBC) is a natural prenylated chalcone with a broad spectrum of pharmacological properties. In this work, we newly synthesized and investigated the antibacterial activity of IBC against Gram-positive, Gram-negative and mycobacterial species. IBC was active against Grampositive bacteria, mainly against Methicillin-Susceptible Staphylococcus aureus (MSSA) and MethicillinResistant Staphylococcus aureus (MRSA), with minimum inhibitory concentration (MIC) values of 1.56 and 3.12 µg/mL, respectively. On the other hand, IBC was not able to act against Gram-negative species (MIC > 400 µg/mL). IBC displayed activity against mycobacterial species (MIC = 64 µg/mL), including Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium kansasii. IBC was able to inhibit more than 50% of MSSA and MRSA biofilm formation at 0.78 µg/mL. Its antibiofilm activity was similar to vancomycin, which was active at 0.74 µg/mL. In order to study the mechanism of the action by fluorescence microscopy, the propidium iodide (PI) and SYTO9 fluorophores indicated that IBC disrupted the membrane of Bacillus subtilis. Toxicity assays using human keratinocytes (HaCaT cell line) showed that IBC did not have the capacity to reduce the cell viability. These results suggested that IBC is a promising antibacterial agent with an elucidated mode of action and potential applications as an antibacterial drug and a medical device coating. |
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Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane DisruptionAntibacterialBiofilmChalconeMembraneNatural productIsobavachalcone (IBC) is a natural prenylated chalcone with a broad spectrum of pharmacological properties. In this work, we newly synthesized and investigated the antibacterial activity of IBC against Gram-positive, Gram-negative and mycobacterial species. IBC was active against Grampositive bacteria, mainly against Methicillin-Susceptible Staphylococcus aureus (MSSA) and MethicillinResistant Staphylococcus aureus (MRSA), with minimum inhibitory concentration (MIC) values of 1.56 and 3.12 µg/mL, respectively. On the other hand, IBC was not able to act against Gram-negative species (MIC > 400 µg/mL). IBC displayed activity against mycobacterial species (MIC = 64 µg/mL), including Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium kansasii. IBC was able to inhibit more than 50% of MSSA and MRSA biofilm formation at 0.78 µg/mL. Its antibiofilm activity was similar to vancomycin, which was active at 0.74 µg/mL. In order to study the mechanism of the action by fluorescence microscopy, the propidium iodide (PI) and SYTO9 fluorophores indicated that IBC disrupted the membrane of Bacillus subtilis. Toxicity assays using human keratinocytes (HaCaT cell line) showed that IBC did not have the capacity to reduce the cell viability. These results suggested that IBC is a promising antibacterial agent with an elucidated mode of action and potential applications as an antibacterial drug and a medical device coating.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Department of Chemistry and Environmental Sciences Institute of Biosciences Humanities and Exact Sciences São Paulo State University (Unesp), SPDepartment of Microbiology Institute of Biomedical Sciences Federal University of Uberlândia (UFU), MGDepartment of Biochemistry and Microbiology Institute of Biosciences São Paulo State University (Unesp), SPDepartment of Preventive and Restorative Dentistry School of Dentistry São Paulo State University (Unesp), SPDepartment of Chemistry and Environmental Sciences Institute of Biosciences Humanities and Exact Sciences São Paulo State University (Unesp), SPDepartment of Biochemistry and Microbiology Institute of Biosciences São Paulo State University (Unesp), SPDepartment of Preventive and Restorative Dentistry School of Dentistry São Paulo State University (Unesp), SPFAPESP: 2014/18330-0FAPESP: 2018/15083-2CNPq: 306251/20167CNPq: 309957/2019-2CNPq: 429322/2018-6CNPq: 471129/2013-5Universidade Estadual Paulista (UNESP)Universidade Federal de Uberlândia (UFU)de Assis, Leticia Ribeiro [UNESP]Theodoro, Reinaldo Dos Santos [UNESP]Costa, Maria Beatriz Silva [UNESP]Nascentes, Julyanna Andrade Silva [UNESP]da Rocha, Miguel Divino [UNESP]Bessa, Meliza Arantes de SouzaMenezes, Ralciane de PaulaDilarri, Guilherme [UNESP]Hypolito, Giovane Böerner [UNESP]Dos Santos, Vanessa Rodrigues [UNESP]Duque, Cristiane [UNESP]Ferreira, Henrique [UNESP]Martins, Carlos Henrique GomesRegasini, Luis Octavio [UNESP]2022-04-29T08:40:15Z2022-04-29T08:40:15Z2022-03-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.3390/membranes12030269Membranes, v. 12, n. 3, 2022.2077-0375http://hdl.handle.net/11449/23048510.3390/membranes120302692-s2.0-85125567508Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengMembranesinfo:eu-repo/semantics/openAccess2022-04-29T08:40:15Zoai:repositorio.unesp.br:11449/230485Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T18:17:34.816293Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption |
title |
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption |
spellingShingle |
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption de Assis, Leticia Ribeiro [UNESP] Antibacterial Biofilm Chalcone Membrane Natural product |
title_short |
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption |
title_full |
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption |
title_fullStr |
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption |
title_full_unstemmed |
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption |
title_sort |
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption |
author |
de Assis, Leticia Ribeiro [UNESP] |
author_facet |
de Assis, Leticia Ribeiro [UNESP] Theodoro, Reinaldo Dos Santos [UNESP] Costa, Maria Beatriz Silva [UNESP] Nascentes, Julyanna Andrade Silva [UNESP] da Rocha, Miguel Divino [UNESP] Bessa, Meliza Arantes de Souza Menezes, Ralciane de Paula Dilarri, Guilherme [UNESP] Hypolito, Giovane Böerner [UNESP] Dos Santos, Vanessa Rodrigues [UNESP] Duque, Cristiane [UNESP] Ferreira, Henrique [UNESP] Martins, Carlos Henrique Gomes Regasini, Luis Octavio [UNESP] |
author_role |
author |
author2 |
Theodoro, Reinaldo Dos Santos [UNESP] Costa, Maria Beatriz Silva [UNESP] Nascentes, Julyanna Andrade Silva [UNESP] da Rocha, Miguel Divino [UNESP] Bessa, Meliza Arantes de Souza Menezes, Ralciane de Paula Dilarri, Guilherme [UNESP] Hypolito, Giovane Böerner [UNESP] Dos Santos, Vanessa Rodrigues [UNESP] Duque, Cristiane [UNESP] Ferreira, Henrique [UNESP] Martins, Carlos Henrique Gomes Regasini, Luis Octavio [UNESP] |
author2_role |
author author author author author author author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (UNESP) Universidade Federal de Uberlândia (UFU) |
dc.contributor.author.fl_str_mv |
de Assis, Leticia Ribeiro [UNESP] Theodoro, Reinaldo Dos Santos [UNESP] Costa, Maria Beatriz Silva [UNESP] Nascentes, Julyanna Andrade Silva [UNESP] da Rocha, Miguel Divino [UNESP] Bessa, Meliza Arantes de Souza Menezes, Ralciane de Paula Dilarri, Guilherme [UNESP] Hypolito, Giovane Böerner [UNESP] Dos Santos, Vanessa Rodrigues [UNESP] Duque, Cristiane [UNESP] Ferreira, Henrique [UNESP] Martins, Carlos Henrique Gomes Regasini, Luis Octavio [UNESP] |
dc.subject.por.fl_str_mv |
Antibacterial Biofilm Chalcone Membrane Natural product |
topic |
Antibacterial Biofilm Chalcone Membrane Natural product |
description |
Isobavachalcone (IBC) is a natural prenylated chalcone with a broad spectrum of pharmacological properties. In this work, we newly synthesized and investigated the antibacterial activity of IBC against Gram-positive, Gram-negative and mycobacterial species. IBC was active against Grampositive bacteria, mainly against Methicillin-Susceptible Staphylococcus aureus (MSSA) and MethicillinResistant Staphylococcus aureus (MRSA), with minimum inhibitory concentration (MIC) values of 1.56 and 3.12 µg/mL, respectively. On the other hand, IBC was not able to act against Gram-negative species (MIC > 400 µg/mL). IBC displayed activity against mycobacterial species (MIC = 64 µg/mL), including Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium kansasii. IBC was able to inhibit more than 50% of MSSA and MRSA biofilm formation at 0.78 µg/mL. Its antibiofilm activity was similar to vancomycin, which was active at 0.74 µg/mL. In order to study the mechanism of the action by fluorescence microscopy, the propidium iodide (PI) and SYTO9 fluorophores indicated that IBC disrupted the membrane of Bacillus subtilis. Toxicity assays using human keratinocytes (HaCaT cell line) showed that IBC did not have the capacity to reduce the cell viability. These results suggested that IBC is a promising antibacterial agent with an elucidated mode of action and potential applications as an antibacterial drug and a medical device coating. |
publishDate |
2022 |
dc.date.none.fl_str_mv |
2022-04-29T08:40:15Z 2022-04-29T08:40:15Z 2022-03-01 |
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/10.3390/membranes12030269 Membranes, v. 12, n. 3, 2022. 2077-0375 http://hdl.handle.net/11449/230485 10.3390/membranes12030269 2-s2.0-85125567508 |
url |
http://dx.doi.org/10.3390/membranes12030269 http://hdl.handle.net/11449/230485 |
identifier_str_mv |
Membranes, v. 12, n. 3, 2022. 2077-0375 10.3390/membranes12030269 2-s2.0-85125567508 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Membranes |
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_ |
1808128917609906176 |