Carbohydrate-Based Strategies in Antimicrobial Research

A special issue of Antibiotics (ISSN 2079-6382).

Deadline for manuscript submissions: closed (30 April 2022) | Viewed by 5012

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Centro de Química Estrutural, Institute of Molecular Sciences, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Lisboa, Portugal
Interests: organic chemistry; medicinal chemistry; carbohydrate and nucleos(t)ide chemistry; bioactive molecules; enzyme inhibitors; anticancer agents; antimicrobial agents; anti-Alzheimer’s agents
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Special Issue Information

Dear Colleagues,

Among the therapeutic opportunities that carbohydrate-containing molecules and their analogs have provided, their antimicrobial potential has been a focus of intense research, encouraged by the various compounds of these classes approved as antibiotics or as antiviral or antiparasitic drugs. Moreover, the threat of antimicrobial resistance, which remains a major healthcare problem, hindering the ability of drugs to combat microorganisms that cause severe infections, necessitates the discovery and exploitation of novel agents that display alternative mechanisms of action. The relevance of glycostructures at the surfaces of pathogenic microbes for recognition and adhesion, their presence as essential constituents of bacteria and viral envelopes, as well as their role in microbial proliferation make them unique targets for the development of therapeutic approaches using carbohydrate derivatives. In this context, we welcome in this Special Issue contributions illustrating the importance of this topic in antimicrobial therapy research, highlighting recent findings.

Dr. Nuno Manuel Xavier
Guest Editor

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Keywords

  • carbohydrates
  • nucleos(t)ides
  • antibacterial agents
  • antiviral agents
  • antiparasitic agents
  • carbohydrate-protein interactions
  • lectins
  • cell-pathogen adhesion
  • drug design
  • synthesis

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Published Papers (1 paper)

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Research

30 pages, 7072 KiB  
Article
Galactose-Clicked Curcumin-Mediated Reversal of Meropenem Resistance among Klebsiella pneumoniae by Targeting Its Carbapenemases and the AcrAB-TolC Efflux System
by Shivangi Yadav, Ashish Kumar Singh, Anand K. Agrahari, Akhilesh Kumar Pandey, Munesh Kumar Gupta, Dipshikha Chakravortty, Vinod Kumar Tiwari and Pradyot Prakash
Antibiotics 2021, 10(4), 388; https://doi.org/10.3390/antibiotics10040388 - 4 Apr 2021
Cited by 8 | Viewed by 3588
Abstract
In over eighty years, despite successive antibiotics discoveries, the rapid advent of multidrug resistance among bacterial pathogens has jolted our misapprehension of success over them. Resistance is spreading faster than the discovery of new antibiotics/antimicrobials. Therefore, the search for better antimicrobials/additives becomes prudent. [...] Read more.
In over eighty years, despite successive antibiotics discoveries, the rapid advent of multidrug resistance among bacterial pathogens has jolted our misapprehension of success over them. Resistance is spreading faster than the discovery of new antibiotics/antimicrobials. Therefore, the search for better antimicrobials/additives becomes prudent. A water-soluble curcumin derivative (Curaq) was synthesised, employing a Cu (I) catalysed 1, 3-cyclo addition reaction; it has been evaluated as a potential treatment for multidrug-resistant isolates and as an antibiotic adjuvant for meropenem against hypervirulent multidrug-resistant Klebsiella pneumoniae isolates. We also investigated its solubility and effect over carbapenemase activity. Additionally, we investigated its impact on the AcrAB-TolC system. We found that Curaq inhibited bacterial growth at a minimal concentration of 16 µg/mL; at a 32 µg/mL concentration, it killed bacterial growth completely. Only nine (9.4%) Klebsiella isolates were sensitive to meropenem; however, after synergising with Curaq (8 µg/mL), 85 (88.54%) hvKP isolates became sensitive to the drug. The Curaq also inhibited the AcrAB-TolC efflux system at 1 µg/mL concentration by disrupting the membrane potential and causing depolarisation. The kinetic parameters obtained also indicated its promise as a carbapenemase inhibitor. These results suggest that Curaq can be an excellent drug candidate as a broad-spectrum antibacterial and anti-efflux agent. Full article
(This article belongs to the Special Issue Carbohydrate-Based Strategies in Antimicrobial Research)
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