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2022
Assis, Leticia Ribeiro; Theodoro, Reinaldo Dos Santos; Costa, Maria Beatriz Silva; Nascentes, Julyanna Andrade Silva; Rocha, Miguel Divino; Bessa, Meliza Arantes Souza; Menezes, Ralciane Paula; Dilarri, Guilherme; Hypolito, Giovane Böerner; Santos, Vanessa Rodrigues Dos; Duque, Cristiane; Ferreira, Henrique; Martins, Carlos Henrique Gomes; Regasini, Luis Octavio
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption Journal Article
In: Membranes, vol. 12, iss. 3, pp. 269, 2022, ISSN: 20770375.
Abstract | Links | BibTeX | Tags: Antibacterial, Biofilm, Chalcone, Membrane, Natural product
@article{nokey,
title = {Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption},
author = {Leticia Ribeiro Assis and Reinaldo Dos Santos Theodoro and Maria Beatriz Silva Costa and Julyanna Andrade Silva Nascentes and Miguel Divino Rocha and Meliza Arantes Souza Bessa and Ralciane Paula Menezes and Guilherme Dilarri and Giovane Böerner Hypolito and Vanessa Rodrigues Dos Santos and Cristiane Duque and Henrique Ferreira and Carlos Henrique Gomes Martins and Luis Octavio Regasini},
url = {https://www.mdpi.com/2077-0375/12/3/269/htm https://www.mdpi.com/2077-0375/12/3/269},
doi = {10.3390/MEMBRANES12030269/S1},
issn = {20770375},
year = {2022},
date = {2022-01-01},
journal = {Membranes},
volume = {12},
issue = {3},
pages = {269},
publisher = {MDPI},
abstract = {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.},
keywords = {Antibacterial, Biofilm, Chalcone, Membrane, Natural product},
pubstate = {published},
tppubtype = {article}
}
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.
Assis, Leticia Ribeiro; Theodoro, Reinaldo Dos Santos; Costa, Maria Beatriz Silva; Nascentes, Julyanna Andrade Silva; Rocha, Miguel Divino; Bessa, Meliza Arantes Souza; Menezes, Ralciane Paula; Dilarri, Guilherme; Hypolito, Giovane Böerner; Santos, Vanessa Rodrigues Dos; Duque, Cristiane; Ferreira, Henrique; Martins, Carlos Henrique Gomes; Regasini, Luis Octavio
Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption Journal Article
In: Membranes, vol. 12, iss. 3, pp. 269, 2022, ISSN: 20770375.
Abstract | Links | BibTeX | Tags: Antibacterial, Biofilm, Chalcone, Membrane, Natural product
@article{nokey,
title = {Antibacterial Activity of Isobavachalcone (IBC) Is Associated with Membrane Disruption},
author = {Leticia Ribeiro Assis and Reinaldo Dos Santos Theodoro and Maria Beatriz Silva Costa and Julyanna Andrade Silva Nascentes and Miguel Divino Rocha and Meliza Arantes Souza Bessa and Ralciane Paula Menezes and Guilherme Dilarri and Giovane Böerner Hypolito and Vanessa Rodrigues Dos Santos and Cristiane Duque and Henrique Ferreira and Carlos Henrique Gomes Martins and Luis Octavio Regasini},
url = {https://www.mdpi.com/2077-0375/12/3/269/htm https://www.mdpi.com/2077-0375/12/3/269},
doi = {10.3390/MEMBRANES12030269/S1},
issn = {20770375},
year = {2022},
date = {2022-01-01},
journal = {Membranes},
volume = {12},
issue = {3},
pages = {269},
publisher = {MDPI},
abstract = {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.},
keywords = {Antibacterial, Biofilm, Chalcone, Membrane, Natural product},
pubstate = {published},
tppubtype = {article}
}
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.
2020
Morão, Luana G.; Lorenzoni, André S. G.; Chakraborty, Parichita; Ayusso, Gabriela M.; Cavalca, Lucia B.; Santos, Mariana B.; Marques, Beatriz C.; Dilarri, Guilherme; Zamuner, Caio; Regasini, Luis O.; Ferreira, Henrique; Scheffers, Dirk Jan
Investigating the Modes of Action of the Antimicrobial Chalcones BC1 and T9A Journal Article
In: Molecules 2020, Vol. 25, Page 4596, vol. 25, iss. 20, pp. 4596, 2020, ISSN: 1420-3049.
Abstract | Links | BibTeX | Tags: <i>Bacillus subtilis</i>, <i>Xanthomonas citri</i>, Asiatic citrus canker, Chalcone
@article{nokey,
title = {Investigating the Modes of Action of the Antimicrobial Chalcones BC1 and T9A},
author = {Luana G. Morão and André S. G. Lorenzoni and Parichita Chakraborty and Gabriela M. Ayusso and Lucia B. Cavalca and Mariana B. Santos and Beatriz C. Marques and Guilherme Dilarri and Caio Zamuner and Luis O. Regasini and Henrique Ferreira and Dirk Jan Scheffers},
url = {https://www.mdpi.com/1420-3049/25/20/4596/htm https://www.mdpi.com/1420-3049/25/20/4596},
doi = {10.3390/MOLECULES25204596},
issn = {1420-3049},
year = {2020},
date = {2020-01-01},
journal = {Molecules 2020, Vol. 25, Page 4596},
volume = {25},
issue = {20},
pages = {4596},
publisher = {Multidisciplinary Digital Publishing Institute},
abstract = {Xanthomonas citri subsp. citri (X. citri) is an important phytopathogen and causes Asiatic Citrus Canker (ACC). To control ACC, copper sprays are commonly used. As copper is an environmentally damaging heavy metal, new antimicrobials are needed to combat citrus canker. Here, we explored the antimicrobial activity of chalcones, specifically the methoxychalcone BC1 and the hydroxychalcone T9A, against X. citri and the model organism Bacillus subtilis. BC1 and T9A prevented growth of X. citri and B. subtilis in concentrations varying from 20 µg/mL to 40 µg/mL. BC1 and T9A decreased incorporation of radiolabeled precursors of DNA, RNA, protein, and peptidoglycan in X. citri and B. subtilis. Both compounds mildly affected respiratory activity in X. citri, but T9A strongly decreased respiratory activity in B. subtilis. In line with that finding, intracellular ATP decreased strongly in B. subtilis upon T9A treatment, whereas BC1 increased intracellular ATP. In X. citri, both compounds resulted in a decrease in intracellular ATP. Cell division seems not to be affected in X. citri, and, although in B. subtilis the formation of FtsZ-rings is affected, a FtsZ GTPase activity assay suggests that this is an indirect effect. The chalcones studied here represent a sustainable alternative to copper for the control of ACC, and further studies are ongoing to elucidate their precise modes of action.},
keywords = {<i>Bacillus subtilis</i>, <i>Xanthomonas citri</i>, Asiatic citrus canker, Chalcone},
pubstate = {published},
tppubtype = {article}
}
Xanthomonas citri subsp. citri (X. citri) is an important phytopathogen and causes Asiatic Citrus Canker (ACC). To control ACC, copper sprays are commonly used. As copper is an environmentally damaging heavy metal, new antimicrobials are needed to combat citrus canker. Here, we explored the antimicrobial activity of chalcones, specifically the methoxychalcone BC1 and the hydroxychalcone T9A, against X. citri and the model organism Bacillus subtilis. BC1 and T9A prevented growth of X. citri and B. subtilis in concentrations varying from 20 µg/mL to 40 µg/mL. BC1 and T9A decreased incorporation of radiolabeled precursors of DNA, RNA, protein, and peptidoglycan in X. citri and B. subtilis. Both compounds mildly affected respiratory activity in X. citri, but T9A strongly decreased respiratory activity in B. subtilis. In line with that finding, intracellular ATP decreased strongly in B. subtilis upon T9A treatment, whereas BC1 increased intracellular ATP. In X. citri, both compounds resulted in a decrease in intracellular ATP. Cell division seems not to be affected in X. citri, and, although in B. subtilis the formation of FtsZ-rings is affected, a FtsZ GTPase activity assay suggests that this is an indirect effect. The chalcones studied here represent a sustainable alternative to copper for the control of ACC, and further studies are ongoing to elucidate their precise modes of action.
Morão, Luana G.; Lorenzoni, André S. G.; Chakraborty, Parichita; Ayusso, Gabriela M.; Cavalca, Lucia B.; Santos, Mariana B.; Marques, Beatriz C.; Dilarri, Guilherme; Zamuner, Caio; Regasini, Luis O.; Ferreira, Henrique; Scheffers, Dirk Jan
Investigating the Modes of Action of the Antimicrobial Chalcones BC1 and T9A Journal Article
In: Molecules 2020, Vol. 25, Page 4596, vol. 25, iss. 20, pp. 4596, 2020, ISSN: 1420-3049.
Abstract | Links | BibTeX | Tags: <i>Bacillus subtilis</i>, <i>Xanthomonas citri</i>, Asiatic citrus canker, Chalcone
@article{nokey,
title = {Investigating the Modes of Action of the Antimicrobial Chalcones BC1 and T9A},
author = {Luana G. Morão and André S. G. Lorenzoni and Parichita Chakraborty and Gabriela M. Ayusso and Lucia B. Cavalca and Mariana B. Santos and Beatriz C. Marques and Guilherme Dilarri and Caio Zamuner and Luis O. Regasini and Henrique Ferreira and Dirk Jan Scheffers},
url = {https://www.mdpi.com/1420-3049/25/20/4596/htm https://www.mdpi.com/1420-3049/25/20/4596},
doi = {10.3390/MOLECULES25204596},
issn = {1420-3049},
year = {2020},
date = {2020-01-01},
journal = {Molecules 2020, Vol. 25, Page 4596},
volume = {25},
issue = {20},
pages = {4596},
publisher = {Multidisciplinary Digital Publishing Institute},
abstract = {Xanthomonas citri subsp. citri (X. citri) is an important phytopathogen and causes Asiatic Citrus Canker (ACC). To control ACC, copper sprays are commonly used. As copper is an environmentally damaging heavy metal, new antimicrobials are needed to combat citrus canker. Here, we explored the antimicrobial activity of chalcones, specifically the methoxychalcone BC1 and the hydroxychalcone T9A, against X. citri and the model organism Bacillus subtilis. BC1 and T9A prevented growth of X. citri and B. subtilis in concentrations varying from 20 µg/mL to 40 µg/mL. BC1 and T9A decreased incorporation of radiolabeled precursors of DNA, RNA, protein, and peptidoglycan in X. citri and B. subtilis. Both compounds mildly affected respiratory activity in X. citri, but T9A strongly decreased respiratory activity in B. subtilis. In line with that finding, intracellular ATP decreased strongly in B. subtilis upon T9A treatment, whereas BC1 increased intracellular ATP. In X. citri, both compounds resulted in a decrease in intracellular ATP. Cell division seems not to be affected in X. citri, and, although in B. subtilis the formation of FtsZ-rings is affected, a FtsZ GTPase activity assay suggests that this is an indirect effect. The chalcones studied here represent a sustainable alternative to copper for the control of ACC, and further studies are ongoing to elucidate their precise modes of action.},
keywords = {<i>Bacillus subtilis</i>, <i>Xanthomonas citri</i>, Asiatic citrus canker, Chalcone},
pubstate = {published},
tppubtype = {article}
}
Xanthomonas citri subsp. citri (X. citri) is an important phytopathogen and causes Asiatic Citrus Canker (ACC). To control ACC, copper sprays are commonly used. As copper is an environmentally damaging heavy metal, new antimicrobials are needed to combat citrus canker. Here, we explored the antimicrobial activity of chalcones, specifically the methoxychalcone BC1 and the hydroxychalcone T9A, against X. citri and the model organism Bacillus subtilis. BC1 and T9A prevented growth of X. citri and B. subtilis in concentrations varying from 20 µg/mL to 40 µg/mL. BC1 and T9A decreased incorporation of radiolabeled precursors of DNA, RNA, protein, and peptidoglycan in X. citri and B. subtilis. Both compounds mildly affected respiratory activity in X. citri, but T9A strongly decreased respiratory activity in B. subtilis. In line with that finding, intracellular ATP decreased strongly in B. subtilis upon T9A treatment, whereas BC1 increased intracellular ATP. In X. citri, both compounds resulted in a decrease in intracellular ATP. Cell division seems not to be affected in X. citri, and, although in B. subtilis the formation of FtsZ-rings is affected, a FtsZ GTPase activity assay suggests that this is an indirect effect. The chalcones studied here represent a sustainable alternative to copper for the control of ACC, and further studies are ongoing to elucidate their precise modes of action.