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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-...
Autores principales: | , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2021
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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. |
format | Online Article Text |
id | pubmed-8199546 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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