Synthesis and Antibacterial Activity of Polyalthic Acid Analogs
Polyalthic acid (PA) is a diterpene found in copaiba oil. As a continuation of our work with PA, we synthesized PA analogs and investigated their antibacterial effects on preformed biofilms of <i>Staphylococcus epidermidis</i> and determined the minimal inhibitory concentration (MIC) of...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-07-01
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| Series: | Antibiotics |
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| Online Access: | https://www.mdpi.com/2079-6382/12/7/1202 |
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| author | Marcela Nunes Argentin Felipe de Paula Nogueira Cruz Ariana Borges Souza Elisa Marcela de Oliveira D’Aurea Jairo Kenupp Bastos Sérgio Ricardo Ambrósio Rodrigo Cassio Sola Veneziani Ilana Lopes Baratella Cunha Camargo Cassia Suemi Mizuno |
| author_facet | Marcela Nunes Argentin Felipe de Paula Nogueira Cruz Ariana Borges Souza Elisa Marcela de Oliveira D’Aurea Jairo Kenupp Bastos Sérgio Ricardo Ambrósio Rodrigo Cassio Sola Veneziani Ilana Lopes Baratella Cunha Camargo Cassia Suemi Mizuno |
| author_sort | Marcela Nunes Argentin |
| collection | DOAJ |
| description | Polyalthic acid (PA) is a diterpene found in copaiba oil. As a continuation of our work with PA, we synthesized PA analogs and investigated their antibacterial effects on preformed biofilms of <i>Staphylococcus epidermidis</i> and determined the minimal inhibitory concentration (MIC) of the best analogs against planktonic bacterial cells. There was no difference in activity between the amides <b>2a</b> and <b>2b</b> and their corresponding amines <b>3a</b> and <b>3b</b> regarding their ability to eradicate biofilm. PA analogs <b>2a</b> and <b>3a</b> were able to significantly eradicate the preformed biofilm of <i>S. epidermidis</i> and were active against all the Gram-positive bacteria tested (<i>Enterococcus faecalis</i>, <i>Enterococcus faecium</i>, <i>S. epidermidis</i>, <i>Staphylococcus aureus)</i>, with different MIC depending on the microorganism. Therefore, PA analogs <b>2a</b> and <b>3a</b> are of interest for further in vitro and in vivo testing to develop formulations for antibiotic drugs against Gram-positive bacteria. |
| first_indexed | 2024-03-11T01:21:34Z |
| format | Article |
| id | doaj.art-65555377d98942f2bc78898a82d1354a |
| institution | Directory Open Access Journal |
| issn | 2079-6382 |
| language | English |
| last_indexed | 2024-03-11T01:21:34Z |
| publishDate | 2023-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Antibiotics |
| spelling | doaj.art-65555377d98942f2bc78898a82d1354a2023-11-18T18:03:43ZengMDPI AGAntibiotics2079-63822023-07-01127120210.3390/antibiotics12071202Synthesis and Antibacterial Activity of Polyalthic Acid AnalogsMarcela Nunes Argentin0Felipe de Paula Nogueira Cruz1Ariana Borges Souza2Elisa Marcela de Oliveira D’Aurea3Jairo Kenupp Bastos4Sérgio Ricardo Ambrósio5Rodrigo Cassio Sola Veneziani6Ilana Lopes Baratella Cunha Camargo7Cassia Suemi Mizuno8Laboratory of Molecular Epidemiology and Microbiology, Department of Physics and Interdisciplinary Science, São Carlos Institute of Physics, University of São Paulo, São Carlos 13563-120, SP, BrazilLaboratory of Molecular Epidemiology and Microbiology, Department of Physics and Interdisciplinary Science, São Carlos Institute of Physics, University of São Paulo, São Carlos 13563-120, SP, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, Franca 14404-600, SP, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, Franca 14404-600, SP, BrazilSchool of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Av. do Café S/N, Ribeirão Preto 14040-930, SP, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, Franca 14404-600, SP, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, Franca 14404-600, SP, BrazilLaboratory of Molecular Epidemiology and Microbiology, Department of Physics and Interdisciplinary Science, São Carlos Institute of Physics, University of São Paulo, São Carlos 13563-120, SP, BrazilCollege of Pharmacy and Health Sciences, Western New England University, Springfield, MA 01109, USAPolyalthic acid (PA) is a diterpene found in copaiba oil. As a continuation of our work with PA, we synthesized PA analogs and investigated their antibacterial effects on preformed biofilms of <i>Staphylococcus epidermidis</i> and determined the minimal inhibitory concentration (MIC) of the best analogs against planktonic bacterial cells. There was no difference in activity between the amides <b>2a</b> and <b>2b</b> and their corresponding amines <b>3a</b> and <b>3b</b> regarding their ability to eradicate biofilm. PA analogs <b>2a</b> and <b>3a</b> were able to significantly eradicate the preformed biofilm of <i>S. epidermidis</i> and were active against all the Gram-positive bacteria tested (<i>Enterococcus faecalis</i>, <i>Enterococcus faecium</i>, <i>S. epidermidis</i>, <i>Staphylococcus aureus)</i>, with different MIC depending on the microorganism. Therefore, PA analogs <b>2a</b> and <b>3a</b> are of interest for further in vitro and in vivo testing to develop formulations for antibiotic drugs against Gram-positive bacteria.https://www.mdpi.com/2079-6382/12/7/1202polyalthic acidcopaiba oilditerpenebiofilmantimicrobialpolyalthic acid analogs |
| spellingShingle | Marcela Nunes Argentin Felipe de Paula Nogueira Cruz Ariana Borges Souza Elisa Marcela de Oliveira D’Aurea Jairo Kenupp Bastos Sérgio Ricardo Ambrósio Rodrigo Cassio Sola Veneziani Ilana Lopes Baratella Cunha Camargo Cassia Suemi Mizuno Synthesis and Antibacterial Activity of Polyalthic Acid Analogs Antibiotics polyalthic acid copaiba oil diterpene biofilm antimicrobial polyalthic acid analogs |
| title | Synthesis and Antibacterial Activity of Polyalthic Acid Analogs |
| title_full | Synthesis and Antibacterial Activity of Polyalthic Acid Analogs |
| title_fullStr | Synthesis and Antibacterial Activity of Polyalthic Acid Analogs |
| title_full_unstemmed | Synthesis and Antibacterial Activity of Polyalthic Acid Analogs |
| title_short | Synthesis and Antibacterial Activity of Polyalthic Acid Analogs |
| title_sort | synthesis and antibacterial activity of polyalthic acid analogs |
| topic | polyalthic acid copaiba oil diterpene biofilm antimicrobial polyalthic acid analogs |
| url | https://www.mdpi.com/2079-6382/12/7/1202 |
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