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- Title
Antiprotozoal and Antibacterial Activity of Ravenelin, a Xanthone Isolated from the Endophytic Fungus Exserohilum rostratum.
- Authors
Pina, Jeferson Rodrigo Souza; Silva-Silva, João Victor; Carvalho, Josiwander Miranda; Bitencourt, Heriberto Rodrigues; Watanabe, Luciano Almeida; Fernandes, Juan Matheus Pereira; Souza, Guilherme Eduardo de; Aguiar, Anna Caroline Campos; Guido, Rafael Victorio Carvalho; Almeida-Souza, Fernando; Calabrese, Kátia da Silva; Marinho, Patrícia Santana Barbosa; Marinho, Andrey Moacir do Rosario
- 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.
- Subjects
ENDOPHYTIC fungi; PLASMODIUM falciparum; PERITONEAL macrophages; XANTHONE; HIGH performance liquid chromatography; GRAM-positive bacteria; ANTIPARASITIC agents
- Publication
Molecules, 2021, Vol 26, Issue 11, p3339
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules26113339