| Autor: |
Ozanique PR; Department of Chemistry and Environmental Sciences, Institute of Biosciences, Humanities and Exact Sciences, São Paulo State University (Unesp), São José do Rio Preto 15054-000, SP, Brazil., Helena AL; Department of Chemistry and Environmental Sciences, Institute of Biosciences, Humanities and Exact Sciences, São Paulo State University (Unesp), São José do Rio Preto 15054-000, SP, Brazil., Menezes RP; Department Microbiology, Institute of Biomedical Sciences, Federal University of Uberlândia (UFU), Umuarama 38405-320, MG, Brazil., Gonçalves DS; Department Microbiology, Institute of Biomedical Sciences, Federal University of Uberlândia (UFU), Umuarama 38405-320, MG, Brazil., Santiago MB; Department Microbiology, Institute of Biomedical Sciences, Federal University of Uberlândia (UFU), Umuarama 38405-320, MG, Brazil., Dilarri G; Department of Biochemistry and Microbiology, Institute of Biosciences, São Paulo State University (Unesp), Rio Claro 13506-900, SP, Brazil., Sardi JCO; Dental Research Division, Guarulhos University, Guarulhos 07023-070, SP, Brazil., Ferreira H; Department of Biochemistry and Microbiology, Institute of Biosciences, São Paulo State University (Unesp), Rio Claro 13506-900, SP, Brazil., Martins CHG; Department Microbiology, Institute of Biomedical Sciences, Federal University of Uberlândia (UFU), Umuarama 38405-320, MG, Brazil., Regasini LO; Department of Chemistry and Environmental Sciences, Institute of Biosciences, Humanities and Exact Sciences, São Paulo State University (Unesp), São José do Rio Preto 15054-000, SP, Brazil. |
| Abstrakt: |
Drug-resistant bacteria constitute a big barrier against current pharmacotherapy. Efforts are urgent to discover antibacterial drugs with novel chemical and biological features. Our work aimed at the synthesis, evaluation of antibacterial effects, and toxicity of licochalcone C (LCC), a naturally occurring chalcone. The synthetic route included six steps, affording a 10% overall yield. LCC showed effects against Gram-positive bacteria (MIC = 6.2-50.0 µg/mL), Mycobacterium species (MIC = 36.2-125 µg/mL), and Helicobacter pylori (MIC = 25 µg/mL). LCC inhibited the biofilm formation of MSSA and MRSA, demonstrating MBIC 50 values of 6.25 μg/mL for both strains. The investigations by fluorescence microscopy, using PI and SYTO9 as fluorophores, indicated that LCC was able to disrupt the S. aureus membrane, similarly to nisin. Systemic toxicity assays using Galleria mellonella larvae showed that LCC was not lethal at 100 µg/mL after 80 h treatment. These data suggest new uses for LCC as a compound with potential applications in antibacterial drug discovery and medical device coating. |
