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Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum

The natural compound ravenelin was isolated from the biomass extracts of Exserohilum rostratum fungus, and its antimicrobial, antiplasmodial, and trypanocidal activities were evaluated. Ravenelin was isolated by column chromatography and HPLC and identified by NMR and MS. The susceptibility of Gram-...

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Autores principales: Pina, Jeferson Rodrigo Souza, Silva-Silva, João Victor, Carvalho, Josiwander Miranda, Bitencourt, Heriberto Rodrigues, Watanabe, Luciano Almeida, Fernandes, Juan Matheus Pereira, de Souza, Guilherme Eduardo, Aguiar, Anna Caroline Campos, Guido, Rafael Victorio Carvalho, Almeida-Souza, Fernando, Calabrese, Kátia da Silva, Marinho, Patrícia Santana Barbosa, Marinho, Andrey Moacir do Rosario
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8199546/
https://www.ncbi.nlm.nih.gov/pubmed/34199336
http://dx.doi.org/10.3390/molecules26113339
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author Pina, Jeferson Rodrigo Souza
Silva-Silva, João Victor
Carvalho, Josiwander Miranda
Bitencourt, Heriberto Rodrigues
Watanabe, Luciano Almeida
Fernandes, Juan Matheus Pereira
de Souza, Guilherme Eduardo
Aguiar, Anna Caroline Campos
Guido, Rafael Victorio Carvalho
Almeida-Souza, Fernando
Calabrese, Kátia da Silva
Marinho, Patrícia Santana Barbosa
Marinho, Andrey Moacir do Rosario
author_facet Pina, Jeferson Rodrigo Souza
Silva-Silva, João Victor
Carvalho, Josiwander Miranda
Bitencourt, Heriberto Rodrigues
Watanabe, Luciano Almeida
Fernandes, Juan Matheus Pereira
de Souza, Guilherme Eduardo
Aguiar, Anna Caroline Campos
Guido, Rafael Victorio Carvalho
Almeida-Souza, Fernando
Calabrese, Kátia da Silva
Marinho, Patrícia Santana Barbosa
Marinho, Andrey Moacir do Rosario
author_sort Pina, Jeferson Rodrigo Souza
collection PubMed
description The natural compound ravenelin was isolated from the biomass extracts of Exserohilum rostratum fungus, and its antimicrobial, antiplasmodial, and trypanocidal activities were evaluated. Ravenelin was isolated by column chromatography and HPLC and identified by NMR and MS. The susceptibility of Gram-positive and Gram-negative bacteria strains to ravenelin was determined by microbroth dilution assay. Cytotoxicity was evaluated in hepatocarcinoma cells (HepG2) and BALB/c peritoneal macrophages by using MTT. SYBR Green I-based assay was used in the asexual stages of Plasmodium falciparum. Trypanocidal activity was tested against the epimastigote and intracellular amastigote forms of Trypanosoma cruzi. Ravenelin was active against Gram-positive bacteria strains, with emphasis on Bacillus subtilis (MIC value of 7.5 µM). Ravenelin’s antiparasitic activities were assessed against both the epimastigote (IC(50) value of 5 ± 1 µM) and the intracellular amastigote forms of T. cruzi (IC(50) value of 9 ± 2 µM), as well as against P. falciparum (IC(50) value of 3.4 ± 0.4 µM). Ravenelin showed low cytotoxic effects on both HepG2 (CC(50) > 50 µM) and peritoneal macrophage (CC(50) = 185 ± 1 µM) cells with attractive selectivity for the parasites (SI values > 15). These findings indicate that ravenelin is a natural compound with both antibacterial and antiparasitic activities, and considerable selectivity indexes. Therefore, ravenelin is an attractive candidate for hit-to-lead development.
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spelling pubmed-81995462021-06-14 Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum Pina, Jeferson Rodrigo Souza Silva-Silva, João Victor Carvalho, Josiwander Miranda Bitencourt, Heriberto Rodrigues Watanabe, Luciano Almeida Fernandes, Juan Matheus Pereira de Souza, Guilherme Eduardo Aguiar, Anna Caroline Campos Guido, Rafael Victorio Carvalho Almeida-Souza, Fernando Calabrese, Kátia da Silva Marinho, Patrícia Santana Barbosa Marinho, Andrey Moacir do Rosario Molecules Article The natural compound ravenelin was isolated from the biomass extracts of Exserohilum rostratum fungus, and its antimicrobial, antiplasmodial, and trypanocidal activities were evaluated. Ravenelin was isolated by column chromatography and HPLC and identified by NMR and MS. The susceptibility of Gram-positive and Gram-negative bacteria strains to ravenelin was determined by microbroth dilution assay. Cytotoxicity was evaluated in hepatocarcinoma cells (HepG2) and BALB/c peritoneal macrophages by using MTT. SYBR Green I-based assay was used in the asexual stages of Plasmodium falciparum. Trypanocidal activity was tested against the epimastigote and intracellular amastigote forms of Trypanosoma cruzi. Ravenelin was active against Gram-positive bacteria strains, with emphasis on Bacillus subtilis (MIC value of 7.5 µM). Ravenelin’s antiparasitic activities were assessed against both the epimastigote (IC(50) value of 5 ± 1 µM) and the intracellular amastigote forms of T. cruzi (IC(50) value of 9 ± 2 µM), as well as against P. falciparum (IC(50) value of 3.4 ± 0.4 µM). Ravenelin showed low cytotoxic effects on both HepG2 (CC(50) > 50 µM) and peritoneal macrophage (CC(50) = 185 ± 1 µM) cells with attractive selectivity for the parasites (SI values > 15). These findings indicate that ravenelin is a natural compound with both antibacterial and antiparasitic activities, and considerable selectivity indexes. Therefore, ravenelin is an attractive candidate for hit-to-lead development. MDPI 2021-06-02 /pmc/articles/PMC8199546/ /pubmed/34199336 http://dx.doi.org/10.3390/molecules26113339 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Pina, Jeferson Rodrigo Souza
Silva-Silva, João Victor
Carvalho, Josiwander Miranda
Bitencourt, Heriberto Rodrigues
Watanabe, Luciano Almeida
Fernandes, Juan Matheus Pereira
de Souza, Guilherme Eduardo
Aguiar, Anna Caroline Campos
Guido, Rafael Victorio Carvalho
Almeida-Souza, Fernando
Calabrese, Kátia da Silva
Marinho, Patrícia Santana Barbosa
Marinho, Andrey Moacir do Rosario
Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum
title Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum
title_full Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum
title_fullStr Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum
title_full_unstemmed Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum
title_short Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum
title_sort antiprotozoal and antibacterial activity of ravenelin, a xanthone isolated from the endophytic fungus exserohilum rostratum
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8199546/
https://www.ncbi.nlm.nih.gov/pubmed/34199336
http://dx.doi.org/10.3390/molecules26113339
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