Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption

Autor: Leticia Ribeiro de Assis, Reinaldo dos Santos Theodoro, Maria Beatriz Silva Costa, Julyanna Andrade Silva Nascentes, Miguel Divino da Rocha, Meliza Arantes de Souza Bessa, Ralciane de Paula Menezes, Guilherme Dilarri, Giovane Böerner Hypolito, Vanessa Rodrigues dos Santos, Cristiane Duque, Henrique Ferreira, Carlos Henrique Gomes Martins, Luis Octavio Regasini
Přispěvatelé: Universidade Estadual Paulista (UNESP), Universidade Federal de Uberlândia (UFU)
Rok vydání: 2021
Předmět:
Zdroj: Membranes; Volume 12; Issue 3; Pages: 269
Scopus
Repositório Institucional da UNESP
Universidade Estadual Paulista (UNESP)
instacron:UNESP
ISSN: 2077-0375
Popis: Made available in DSpace on 2022-04-29T08:40:15Z (GMT). No. of bitstreams: 0 Previous issue date: 2022-03-01 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) 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. Department of Chemistry and Environmental Sciences Institute of Biosciences Humanities and Exact Sciences São Paulo State University (Unesp), SP Department of Microbiology Institute of Biomedical Sciences Federal University of Uberlândia (UFU), MG Department of Biochemistry and Microbiology Institute of Biosciences São Paulo State University (Unesp), SP Department of Preventive and Restorative Dentistry School of Dentistry São Paulo State University (Unesp), SP Department of Chemistry and Environmental Sciences Institute of Biosciences Humanities and Exact Sciences São Paulo State University (Unesp), SP Department of Biochemistry and Microbiology Institute of Biosciences São Paulo State University (Unesp), SP Department of Preventive and Restorative Dentistry School of Dentistry São Paulo State University (Unesp), SP FAPESP: 2014/18330-0 FAPESP: 2018/15083-2 CNPq: 306251/20167 CNPq: 309957/2019-2 CNPq: 429322/2018-6 CNPq: 471129/2013-5
Databáze: OpenAIRE
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