RESUMO
Background: The antimicrobial properties and molecular interaction analysis of curcumin and its derivatives against three different strains of Streptococcus pneumoniae (Penicillin-susceptible, Penicillin-intermediate and Penicillin-resistant) are studied. Results: These properties were analyzed based on the measurement of the inhibition zone, minimum inhibitory concentration (MIC), and rate of kill revealed that curcumin monoglucoside, curcumin diglucoside and curcumin possessed strong antimicrobial properties even on the Penicillin-resistant strains. Additionally, the molecular docking simulation analyses against Penicillin Binding Protein of S. pneumoniae also confirm that these compounds docked at the active site of the enzyme. Further, the molecular dynamics simulation validates the conformational stability of the docked ligand-protein complexes in the dynamic environment. Conclusion: curcumin monoglucoside, curcumin diglucoside and curcumin can be prescribed for treatment against Penicillin-resistant S. pneumoniae.
Assuntos
Streptococcus pneumoniae/efeitos dos fármacos , Curcumina/química , Anti-Infecciosos/farmacologia , Resistência às Penicilinas , Testes de Sensibilidade Microbiana , Simulação de Acoplamento MolecularRESUMO
Antimicrobial therapy is a key component of modern medical practice and a cornerstone for the development of complex clinical interventions in critically ill patients. Unfortunately, the increasing problem of antimicrobial resistance is now recognized as a major public health threat jeopardizing the care of thousands of patients worldwide. Gram-positive pathogens exhibit an immense genetic repertoire to adapt and develop resistance to virtually all antimicrobials clinically available. As more molecules become available to treat resistant gram-positive infections, resistance emerges as an evolutionary response. Thus, antimicrobial resistance has to be envisaged as an evolving phenomenon that demands constant surveillance and continuous efforts to identify emerging mechanisms of resistance to optimize the use of antibiotics and create strategies to circumvent this problem. Here, we will provide a broad perspective on the clinical aspects of antibiotic resistance in relevant gram-positive pathogens with emphasis on the mechanistic strategies used by these organisms to avoid being killed by commonly used antimicrobial agents.