| Author | Pina, Jeferson Rodrigo Souza | |
| Author | Silva, João Victor Silva | |
| Author | Carvalho, Josiwander Miranda | |
| Author | Bitencourt, Heriberto Rodrigues | |
| Author | Watanabe, Luciano Almeida | |
| Author | Fernandes, Juan Matheus Pereira | |
| Author | Souza, Guilherme Eduardo de | |
| Author | Aguiar, Anna Caroline Campos | |
| Author | Guido, Rafael Victorio Carvalho | |
| Author | Souza, Fernando Almeida | |
| Author | Calabrese, Kátia da Silva | |
| Author | Marinho, Patrícia Santana Barbosa | |
| Author | Marinho, Andrey Moacir do Rosario | |
| Access date | 2021-07-16T13:52:56Z | |
| Available date | 2021-07-16T13:52:56Z | |
| Document date | 2021 | |
| Citation | PINA, Jeferson Rodrigo Souza et al. Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum. Molecules, v. 26, 3339, 11 p, 2021. | pt_BR |
| ISSN | 1420-3049 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/48256 | |
| Language | eng | pt_BR |
| Publisher | MDPI | pt_BR |
| Rights | open access | |
| Subject in Portuguese | Antimicrobiano | pt_BR |
| Subject in Portuguese | Antiprotozoário | pt_BR |
| Subject in Portuguese | Poliketídeos | pt_BR |
| Subject in Portuguese | Xanthone | pt_BR |
| Subject in Portuguese | Ácido Graxo Sintase Tipo II | pt_BR |
| Title | Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum | pt_BR |
| Type | Article | |
| DOI | 10.3390/molecules26113339 | |
| Abstract | 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 (IC50 value of 5 ± 1 µM) and the intracellular
amastigote forms of T. cruzi (IC50 value of 9 ± 2 µM), as well as against P. falciparum (IC50 value of
3.4 ± 0.4 µM). Ravenelin showed low cytotoxic effects on both HepG2 (CC50 > 50 µM) and peritoneal
macrophage (CC50 = 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. | pt_BR |
| Affilliation | Universidade Federal do Pará. Programa de Pós-Graduação em Química. Belém, PA, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Pará. Programa de Pós-Graduação em Química. Belém, PA, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Pará. Programa de Pós-Graduação em Química. Belém, PA, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Pará. Programa de Pós-Graduação em Química. Belém, PA, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade de São Paulo. Instituto de Física de São Carlos. São Carlos, SP, Brasil. | pt_BR |
| Affilliation | Universidade de São Paulo. Instituto de Física de São Carlos. São Carlos, SP, Brasil. | pt_BR |
| Affilliation | Universidade de São Paulo. Instituto de Física de São Carlos. São Carlos, SP, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil / Universidade do Estado do Maranhão. Programa de Pós-Graduação em Ciências Animal. São Luis, MA, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Imunomodulação e Protozoologia. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Pará. Programa de Pós-Graduação em Química. Belém, PA, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Pará. Programa de Pós-Graduação em Química. Belém, PA, Brasil. | pt_BR |
| Subject | Antimicrobial | pt_BR |
| Subject | Antiprotozoan | pt_BR |
| Subject | Polyketides | pt_BR |
| Subject | Fungi | pt_BR |
| Subject | Xanthone | pt_BR |
| DeCS | Ácido Graxo Sintase Tipo II | pt_BR |
