International Journal of Pharmacy and Chemistry

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Evaluation of Amlodipine Inhibition and Antimicrobial Effects

Received: 19 February 2019    Accepted: 25 March 2019    Published: 15 April 2019
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Abstract

Antibiotic resistant pathogens is the an urgent challenge of the medicine field. To counter these pathogens, the antibiotic assisting drugs is an ideal choice. Assisting drugs can improve the efficiency of the treatment without further induce of antibiotic resistance. Amlodipine (AML) is one of the most common generic cardiovascular drug for lowering blood pressure. In previous studies, amlodipine was suggested to have some antibiotic properties. The MIC is not very low for amlodipine against these pathogens. However, the findings imply amlodipine potential to be repurposed as assisting drug and its inhibition of β-lactamase. To further discover and verify its potential of antimicrobial drug, amlodipine was tested for β-lactamase inhibition, and its synergistic effects were investigated against methicillin-resistant Staphylococcus aureus (MRSA). The compound was found to inhibit β-lactamase mixture (3 distinct species) in broad spectrum. Cephalosporins requires high concentration (>=64 ug/ml) to inhibit MRSA; combine both amlodipine and cephalosporins, the MIC only requires 8ug/ml (4 ug/ml amlodipine + 4 ug/ml Cefuroxime) in total, with FIC lower than 0.1 for strong synergistic effect. Both enzyme assay and bacterial tests indicate amlodipine as an ideal assisting drug for antibiotics; one of the mechanism is β-lactamase inhibition.

DOI 10.11648/j.ijpc.20190501.12
Published in International Journal of Pharmacy and Chemistry (Volume 5, Issue 1, January 2019)
Page(s) 12-14
Creative Commons

This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.

Copyright

Copyright © The Author(s), 2024. Published by Science Publishing Group

Keywords

Amlodipine, β-lactamase, MRSA, Synergic

References
[1] Kumar K, Ganguly K, Mazumdar K, Dutta N, Dastidar S, Chakrabarty A. Amlodipine: a cardiovascular drug with powerful antimicrobial property. Acta Microbiol Pol. 2003; 52(3): p. 285-92.
[2] Gupta P, Chanda R, Rai N, Kataria V, Kumar N. Antihypertensive, amlodipine besilate inhibits growth and biofilm of human fungal pathogen candida. Assay Drug Dev Technol. 2016 Jan; 14(5): p. online.
[3] Owen AJ, Reid CM. Cardio classics revisited focus on the role of amlodipine. Integr Blood Press Control. 2012 Jan; 2012(5): p. 1-7.
[4] Partha P, Nahid A. Oral therapy with amlodipine and lacidipine, 1,4-dihydropyridine derivatives showing activity against experimental Visceral leishmaniasis. Antimicrob Agents Chemother. 2008 Jan; 52(1): p. 374-7.
[5] Li Y, Pan C, Zhao Z, Zhao Z, Chen H, Lu W. Effects of a combination of amlodipine and imipenem on 42 clinical isolates of Acinetobacter baumannii obtained from a teaching hospital in Guangzhou, China. BMC Infect Dis. 2013 Nov; 13: p. 548.
[6] Hu C, Li Y, Zhao Z, Wei S, Zhao Z, Chen H, et al. in vitro synergistic effect of amlodipine and imipenem on the expression of the AdeABC efflux pump in multidrug-resistant Acinetobacter baumannii. PLoS One. 2018 June; 13(6): p. e0198061.
[7] Delaney J', Schneider-Lindner V, Brassard P, Suissa S. Mortality after infection with methicillin-resistant Staphylococcus aureus (MRSA) diagnosed in the community. BMC Medicine. 2008 Jan; 6: p. 2.
[8] Kavanagh KT, Abusalem S, Calderon E. the incidence of MRSA infections in the United States: is a more comprehensive tracking system needed? Antimicrob Resist Infect Control. 2017 April; 6: p. 34.
[9] Arêde P, Ministro J, Oliveira DC. Redefining the role of the β-lactamase locus in methicillin-resistant Staphylococcus aureus: β-lactamase regulators disrupt the MecI-mediated strong repression on mecA and optimize the phenotypic expression of resistance in strains with constitutive mecA. Antimicrob Agents Chemother. 2013 July; 57(7): p. 3037-45.
[10] Leticia I. L, Jed F. F, Shahriar M. Molecular basis and phenotype of methicillin resistance in Staphylococcus aureus and insights into new β-lactams that meet the challenge. Antimicrob Agents Chemother. 2009 Oct; 53(10): p. 4051-63.
[11] Fuda CCS, Fisher JF, Mobashery S. Β-lactam resistance in Staphylococcus aureus: the adaptive resistance of a plastic genome. Cell Mol Life Sci. 2015 Nov; 62(22): p. 2617-33.
[12] O'Callaghan, Cynthia H. et al. Novel Method for Detection of B-Lactamases by Using a Chromogenic Cephalosporin Substrate. Antimicrob Agents Chemother. 1972 April; 1(4): p. 283-88.
[13] Chin N, Neu N, Neu H. Synergy of sulbactam and ampicillin against methicillin-resistant staphylococci. Drugs Exp Clin Res. 1986; 12(12): p. 939-42.
Author Information
  • Case Western Reserve University, Cleveland, United States

  • Hengyang Normal University, Hengyang, China

  • Nanjing University of Chinese Medicine, Nanjing, China

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    Ziyue Yi, Zhu Pei, Ma Xiaoyan. (2019). Evaluation of Amlodipine Inhibition and Antimicrobial Effects. International Journal of Pharmacy and Chemistry, 5(1), 12-14. https://doi.org/10.11648/j.ijpc.20190501.12

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    ACS Style

    Ziyue Yi; Zhu Pei; Ma Xiaoyan. Evaluation of Amlodipine Inhibition and Antimicrobial Effects. Int. J. Pharm. Chem. 2019, 5(1), 12-14. doi: 10.11648/j.ijpc.20190501.12

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    AMA Style

    Ziyue Yi, Zhu Pei, Ma Xiaoyan. Evaluation of Amlodipine Inhibition and Antimicrobial Effects. Int J Pharm Chem. 2019;5(1):12-14. doi: 10.11648/j.ijpc.20190501.12

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  • @article{10.11648/j.ijpc.20190501.12,
      author = {Ziyue Yi and Zhu Pei and Ma Xiaoyan},
      title = {Evaluation of Amlodipine Inhibition and Antimicrobial Effects},
      journal = {International Journal of Pharmacy and Chemistry},
      volume = {5},
      number = {1},
      pages = {12-14},
      doi = {10.11648/j.ijpc.20190501.12},
      url = {https://doi.org/10.11648/j.ijpc.20190501.12},
      eprint = {https://download.sciencepg.com/pdf/10.11648.j.ijpc.20190501.12},
      abstract = {Antibiotic resistant pathogens is the an urgent challenge of the medicine field. To counter these pathogens, the antibiotic assisting drugs is an ideal choice. Assisting drugs can improve the efficiency of the treatment without further induce of antibiotic resistance. Amlodipine (AML) is one of the most common generic cardiovascular drug for lowering blood pressure. In previous studies, amlodipine was suggested to have some antibiotic properties. The MIC is not very low for amlodipine against these pathogens. However, the findings imply amlodipine potential to be repurposed as assisting drug and its inhibition of β-lactamase. To further discover and verify its potential of antimicrobial drug, amlodipine was tested for β-lactamase inhibition, and its synergistic effects were investigated against methicillin-resistant Staphylococcus aureus (MRSA). The compound was found to inhibit β-lactamase mixture (3 distinct species) in broad spectrum. Cephalosporins requires high concentration (>=64 ug/ml) to inhibit MRSA; combine both amlodipine and cephalosporins, the MIC only requires 8ug/ml (4 ug/ml amlodipine + 4 ug/ml Cefuroxime) in total, with FIC lower than 0.1 for strong synergistic effect. Both enzyme assay and bacterial tests indicate amlodipine as an ideal assisting drug for antibiotics; one of the mechanism is β-lactamase inhibition.},
     year = {2019}
    }
    

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  • TY  - JOUR
    T1  - Evaluation of Amlodipine Inhibition and Antimicrobial Effects
    AU  - Ziyue Yi
    AU  - Zhu Pei
    AU  - Ma Xiaoyan
    Y1  - 2019/04/15
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    DO  - 10.11648/j.ijpc.20190501.12
    T2  - International Journal of Pharmacy and Chemistry
    JF  - International Journal of Pharmacy and Chemistry
    JO  - International Journal of Pharmacy and Chemistry
    SP  - 12
    EP  - 14
    PB  - Science Publishing Group
    SN  - 2575-5749
    UR  - https://doi.org/10.11648/j.ijpc.20190501.12
    AB  - Antibiotic resistant pathogens is the an urgent challenge of the medicine field. To counter these pathogens, the antibiotic assisting drugs is an ideal choice. Assisting drugs can improve the efficiency of the treatment without further induce of antibiotic resistance. Amlodipine (AML) is one of the most common generic cardiovascular drug for lowering blood pressure. In previous studies, amlodipine was suggested to have some antibiotic properties. The MIC is not very low for amlodipine against these pathogens. However, the findings imply amlodipine potential to be repurposed as assisting drug and its inhibition of β-lactamase. To further discover and verify its potential of antimicrobial drug, amlodipine was tested for β-lactamase inhibition, and its synergistic effects were investigated against methicillin-resistant Staphylococcus aureus (MRSA). The compound was found to inhibit β-lactamase mixture (3 distinct species) in broad spectrum. Cephalosporins requires high concentration (>=64 ug/ml) to inhibit MRSA; combine both amlodipine and cephalosporins, the MIC only requires 8ug/ml (4 ug/ml amlodipine + 4 ug/ml Cefuroxime) in total, with FIC lower than 0.1 for strong synergistic effect. Both enzyme assay and bacterial tests indicate amlodipine as an ideal assisting drug for antibiotics; one of the mechanism is β-lactamase inhibition.
    VL  - 5
    IS  - 1
    ER  - 

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