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Potentiation of Antibiotic Activity by a Meldrum’s Acid Arylamino Methylene Derivative against Multidrug-Resistant Bacterial Strains

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Abstract

This study aimed to evaluate the intrinsic antibacterial activity and antibiotic-enhancing effect of an arylamino methylene derivative (MAD) in association with fluoroquinolones. The antibacterial activity against multiresistant Pseudomonas aeruginosa, Staphylococcus aureus and Escherichia coli was analyzed by determining the minimum inhibitory concentration (MIC) using the broth micro dilution method. A reduction in the MIC of the fluoroquinolones against strains treated simultaneously with the MAD was interpreted as an enhanced antibiotic activity. While the MAD exhibited no clinically effective action (MIC ≥ 1.024 µg/mL), it was found to significantly potentiate the activity of norfloxacin, ofloxacin and lomefloxacin against all the strains, which may be related to structural similarities between the MAD and quinolones. Our findings suggest that Meldrum’s acid arylamino derivatives may represent promising molecules in the elaboration of new drugs to reverse resistance to fluoroquinolones.

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References

  1. Rodrigues TS, Santos AMR, Lima PC, Moura MEB, Goiano PDOL, Fontinele DRS (2018) Bacterial resistance to antibiotics in the intensive therapy unit: integrative review. REPIS 4:1–17. https://doi.org/10.26694/repis.v4i0.7350

    Article  Google Scholar 

  2. Loureiro RJ, Roque F, Rodrigues AT, Herdeiro MT, Ramalheira E (2016) Use of antibiotics and bacterial resistances: brief notes on its evolution. Rev Port Saúde Pública 34:77–84. https://doi.org/10.1016/j.rpsp.2015.11.003

    Article  Google Scholar 

  3. Blair JMA, Webber MA, Baylay AJ, Ogbolu DO, Piddock LJV (2015) Molecular mechanisms of antibiotic resistance. Nat Rev Microbiol 13:42–51. https://doi.org/10.1038/nrmicro3380

    Article  CAS  PubMed  Google Scholar 

  4. Sampaio GMM, Teixeira AMR, Coutinho HDM, Junior DMS, Freire PTC, Bento RRF, Silva LE (2014) Synthesis and antibacterial activity of a new derivative of the Meldrun acid: 2,2-dimethyl-5-(4h–1,2,4- triazol-4-ylaminomethylene)-1,3-dioxane-4,6-dione (C9H10N4O4). EXCLI J 13:1022–1028

    PubMed  PubMed Central  Google Scholar 

  5. Coutinho HDM, Matias EFF, Santos KKA, Santos FAV, Morais-Braga MFB, Souza TM, Andrade JC, Souza CES, Siqueira-Júnior JP, Costa JGM (2011) Modulation of the norfloxacin resistance in Staphylococcus aureus by Croton campestris A. and Ocimum gratissimum L. Biomedica 31:608–612

    Article  Google Scholar 

  6. Bezerra CF, Camilo CJ, Silva MKN, Freitas TS, Ribeiro-Filho J, Coutinho HDM (2017) Vanillin selectively modulates the action of antibiotics against resistant bacteria. Microb Pathog 113:265–268. https://doi.org/10.1016/j.micpath.2017.10.052

    Article  CAS  PubMed  Google Scholar 

  7. Coutinho HDM, Costa JGM, Lima EO, Falcão-Silva VS, Siqueira-Júnior JP (2008) Enhancement of the antibiotic activity against a multiresistant Escherichia coli by Mentha arvensis L. and chlorpromazine. Chemotherapy 54:328. https://doi.org/10.1159/000151267

    Article  CAS  PubMed  Google Scholar 

  8. Houghton PJ, Howes MJ, Lee CC, Steventon G (2007) Uses and abuses of in vitro tests in ethnopharmacology: visualizing an elephant. J Ethnopharmacol 110:391–400. https://doi.org/10.1016/j.jep.2007.01.032

    Article  CAS  PubMed  Google Scholar 

  9. Santos CBR, Lobato CC, Sousa MAC, Macêdo WJC, Carvalho JCT (2014) Molecular modeling: origin, fundamental concepts and applications using structure-activity relationship and quantitative structure-activity relationship. Rev Theor Sci 2:91–115. https://doi.org/10.1166/rits.2014.1016

    Article  Google Scholar 

  10. Wong CA, Galvis V, Tello A, Villareal D, Rey JJ (2012) In vitro antibiotic susceptibility to fluoroquinolones. Arch Soc Esp Oftalmol 87:72–78. https://doi.org/10.1016/j.oftal.2011.06.023

    Article  CAS  PubMed  Google Scholar 

  11. Janković N, Muškinja J, Ratković Z, Bugarčić Z, Ranković B, Kosanić M, Stefanović S (2016) Solvent-free synthesis of novel vanillidene derivatives of Meldrum's acid: biological evaluation, DNA and BSA binding study. RSC Adv 6:39452–39459. https://doi.org/10.1039/C6RA07711K

    Article  Google Scholar 

  12. Silva JMB, Hollenbach CB (2010) Fluoroquinolones x bacterial resistance on veterinary medicine. Arq Inst Biol 77:363–369

    Article  Google Scholar 

  13. Liu H, Ren ZL, Wang W, Gong JX, Chu MJ, Ma QW, Wang JC, Lv XL (2018) Novel coumarin-pyrazole carboxamide derivatives as potential topoisomerase II inhibitors: design, synthesis and antibacterial activity. Eur J Med Chem 157:81–87. https://doi.org/10.1016/j.ejmech.2018.07.059

    Article  CAS  PubMed  Google Scholar 

  14. Guimarães DO, Momesso LS, Pupo MT (2010) Antibióticos: importância terapêutica e perspectivas para a descoberta e desenvolvimento de novos agentes. Quim Nova 33:667–679. https://doi.org/10.1590/S0100-40422010000300035

    Article  Google Scholar 

  15. Souza RB, Magnani M, Oliveira TCRM (2010) Mechanisms of quinolone resistance in Salmonella spp. Cienc Agrar 31:413–427

    Article  Google Scholar 

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Funding

This study was financed in part by the National Council of Scientific and Technological Development—CNPq. Process (150456/2018-2 and 406685/2018-5)

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Correspondence to Henrique D. M. Coutinho.

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da Silva, M.M.C., de Araújo-Neto, J.B., de Araújo, A.C.J. et al. Potentiation of Antibiotic Activity by a Meldrum’s Acid Arylamino Methylene Derivative against Multidrug-Resistant Bacterial Strains. Indian J Microbiol 61, 100–103 (2021). https://doi.org/10.1007/s12088-020-00910-6

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  • DOI: https://doi.org/10.1007/s12088-020-00910-6

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