<p>Extract-based libraries represent an underexplored resource for discovering compounds with potential for new drug development. This study aimed to screen 114 extracts from the Brazilian Atlantic Forest plants to identify new antibacterial agents. The antibacterial activity against pathogenic bacteria was measured using the microdilution method. Bio-guided fractionation of active extracts was performed using silica gel columns, and phytochemical profiling was conducted via GC–MS and HPLC-RF. Notably, the hexane fraction derived from the dichloromethane-methanol crude extract of <i>Eugenia astringens</i> Cambess., Myrtaceae, leaves demonstrated significant activity by inhibiting the growth of <i>Staphylococcus aureus</i> ATCC 29213 and methicillin-resistant <i>S. aureus</i> (MRSA) USA 300, with a synergistic interaction observed when combined with ofloxacin. Time-kill assays revealed that the hexane extract of <i>E. astringens</i> exhibited bactericidal action against <i>S. aureus</i> ATCC 29213 and <i>S. intermedius</i> ATCC 29663. A relationship between cytotoxicity and antibacterial activity was established in the hexane extract of <i>E. astringens</i>, indicating that this fraction is more selective against bacteria than Vero cells. The phytochemical analysis identified α-guaiene and italicene as the major components of the fraction of the hexane extract of <i>E. astringens</i>, suggesting their involvement in the antibacterial activity of the species. In conclusion, developing extract-based libraries that integrate extraction, fractionation, isolation, identification, and pharmacological evaluation remains a powerful strategy for identifying new plant species with bioactive compounds, contributing to the discovery of novel therapeutic agents.</p> Graphical Abstract <p></p>

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Screening of Plant Extracts from the Brazilian Atlantic Forest Reveals a Fraction Rich in Sesquiterpenes from Eugenia astringens as a Potential Antibacterial

  • Alisson Andrade Almeida,
  • Ana Paula Agrizzi,
  • Jeany Paschoalino Mendes,
  • Laís Azevedo Rodrigues,
  • João Pedro Vianna Braga,
  • Arley Rey Páez,
  • Rodinei Augusti,
  • Júlio Onésio F. Melo,
  • Mauro R. Silva,
  • Andréa de Oliveira Barros Ribon,
  • João Paulo Viana Leite

摘要

Extract-based libraries represent an underexplored resource for discovering compounds with potential for new drug development. This study aimed to screen 114 extracts from the Brazilian Atlantic Forest plants to identify new antibacterial agents. The antibacterial activity against pathogenic bacteria was measured using the microdilution method. Bio-guided fractionation of active extracts was performed using silica gel columns, and phytochemical profiling was conducted via GC–MS and HPLC-RF. Notably, the hexane fraction derived from the dichloromethane-methanol crude extract of Eugenia astringens Cambess., Myrtaceae, leaves demonstrated significant activity by inhibiting the growth of Staphylococcus aureus ATCC 29213 and methicillin-resistant S. aureus (MRSA) USA 300, with a synergistic interaction observed when combined with ofloxacin. Time-kill assays revealed that the hexane extract of E. astringens exhibited bactericidal action against S. aureus ATCC 29213 and S. intermedius ATCC 29663. A relationship between cytotoxicity and antibacterial activity was established in the hexane extract of E. astringens, indicating that this fraction is more selective against bacteria than Vero cells. The phytochemical analysis identified α-guaiene and italicene as the major components of the fraction of the hexane extract of E. astringens, suggesting their involvement in the antibacterial activity of the species. In conclusion, developing extract-based libraries that integrate extraction, fractionation, isolation, identification, and pharmacological evaluation remains a powerful strategy for identifying new plant species with bioactive compounds, contributing to the discovery of novel therapeutic agents.

Graphical Abstract