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1.
Int J Mol Sci ; 22(11)2021 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-34067346

RESUMO

Prenylated flavonoids are an important class of naturally occurring flavonoids with important biological activity, but their low abundance in nature limits their application in medicines. Here, we showed the hemisynthesis and the determination of various biological activities of seven prenylated flavonoids, named 7-13, with an emphasis on antimicrobial ones. Compounds 9, 11, and 12 showed inhibitory activity against human pathogenic fungi. Compounds 11, 12 (flavanones) and 13 (isoflavone) were the most active against clinical isolated Staphylococcus aureus MRSA, showing that structural requirements as prenylation at position C-6 or C-8 and OH at positions C-5, 7, and 4' are key to the antibacterial activity. The combination of 11 or 12 with commercial antibiotics synergistically enhanced the antibacterial activity of vancomycin, ciprofloxacin, and methicillin in a factor of 10 to 100 times against drug-resistant bacteria. Compound 11 combined with ciprofloxacin was able to decrease the levels of ROS generated by ciprofloxacin. According to docking results of S enantiomer of 11 with ATP-binding cassette transporter showed the most favorable binding energy; however, more studies are needed to support this result.


Assuntos
Antibacterianos/farmacologia , Flavonoides/farmacologia , Prenilação/fisiologia , Transportadores de Cassetes de Ligação de ATP/metabolismo , Animais , Linhagem Celular , Linhagem Celular Tumoral , Simulação por Computador , Flavanonas/farmacologia , Fungos/efeitos dos fármacos , Humanos , Isoflavonas/farmacologia , Camundongos , Testes de Sensibilidade Microbiana/métodos , Espécies Reativas de Oxigênio/metabolismo , Staphylococcus aureus/efeitos dos fármacos
2.
One Health ; 12: 100219, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33553565

RESUMO

Aquaculture is seen as an essential requirement for improving food security and nutrition. Fish such as salmonids are a primary source of protein and essential nutrients. Aquaculture provide income for communities across the world and have a smaller carbon footprint than terrestrial animal-production systems. However, fish diseases are a constant threat, and the use of antibiotics is a source of concern due to its adverse impacts on the environment and human health. Chilean salmon farming has made several efforts to reduce the use of antibiotics for the eradication of piscirickettsiosis, a disease caused by the gram-negative bacteria Piscirickettsia salmonis. Excessive amounts of antibiotics continue to be used in Chilean aquaculture, playing an important role in the emerging public health crisis of antimicrobial resistance. Without doubt, P. salmonis is becoming increasingly resistant to important frontline antimicrobial classes, with severe implications for the future treatment of infectious human and animal diseases. Antimicrobial-resistant bacteria as well as antibiotic residues from salmon production are spreading in the environment, and thus both salmon food commodities and wild organisms can become a source of resistant bacteria that can be transmitted to humans as foodborne contaminants. This urgent threat needs to be addressed by implementing national strategies in compliance with international standards that include both prudent antimicrobial use in marine salmon farms and the investment towards a One Health approach, which combines human, animal and environmental health.

3.
Methods Mol Biol ; 1602: 239-250, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28508224

RESUMO

The piscine Orthomyxovirus called Infectious Salmon Anemia Virus (ISAV) is one of the most important emerging pathogens affecting the salmon industry worldwide. The first reverse genetics system for ISAV, which allows the generation of recombinant ISA virus (rISAV), is an important tool for the characterization and study of this fish virus. The plasmid-based reverse genetics system for ISAV includes the use of a novel fish promoter, the Atlantic salmon internal transcribed spacer region 1 (ITS-1). The salmon, viral and mammalian genetic elements included in pSS-URG vectors allow the expression of the eight viral RNA segments. In addition to four cytomegalovirus (CMV)-based vectors that express the four proteins of the ISAV ribonucleoprotein complex, the eight pSS-URG vectors allowed the generation of infectious rISAV in salmon cells.


Assuntos
DNA Complementar , Isavirus/genética , RNA Viral , Replicação Viral , Animais , Linhagem Celular , Clonagem Molecular , Expressão Gênica , Ordem dos Genes , Genoma Viral , Plasmídeos/genética , Genética Reversa , Transfecção
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