Non‐Antibiotics – An Alternative for Microbial Resistance: Scope and Hope

Chattopadhyay, Debprasad; Das, Soumen; Patra, Arup Ranjan; Bhattacharya, Sujit

doi:10.1002/9783527622931.ch4

Cited by 4 publications

(4 citation statements)

References 132 publications

(283 reference statements)

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“…(5-8) indicated a quite questionable correlation ( Figure 2). The corresponding r values were too low: −0.032 (vectors 6-8) and −0.107 (5). Similar behaviors were observed when exploring the relationships between lipophilicity (C) and activities against the SA strains (5-8).…”

Section: Synergistic Effectsupporting

confidence: 56%

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Dibasic Derivatives of Phenylcarbamic Acid as Prospective Antibacterial Agents Interacting with Cytoplasmic Membrane

et al. 2020

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1-[2-[({[2-/3-(Alkoxy)phenyl]amino}carbonyl)oxy]-3-(dipropylammonio)propyl]pyrrolidinium/azepan- ium oxalates or dichlorides (alkoxy = butoxy to heptyloxy) were recently described as very promising antimycobacterial agents. These compounds were tested in vitro against Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212 (reference and control strains), three methicillin-resistant isolates of S. aureus, and three isolates of vancomycin-resistant E. faecalis. 1-[3-(Dipropylammonio)-2-({[3-(pentyloxy-/hexyloxy-/heptyloxy)phenyl]carbamoyl}oxy)propyl]pyrrolidinium dichlorides showed high activity against staphylococci and enterococci comparable with or higher than that of used controls (clinically used antibiotics and antiseptics). The screening of the cytotoxicity of the compounds as well as the used controls was performed using human monocytic leukemia cells. IC50 values of the most effective compounds ranged from ca. 3.5 to 6.3 µM, thus, it can be stated that the antimicrobial effect is closely connected with their cytotoxicity. The antibacterial activity is based on the surface activity of the compounds that are influenced by the length of their alkoxy side chain, the size of the azacyclic system, and hydro-lipophilic properties, as proven by in vitro experiments and chemometric principal component analyses. Synergistic studies showed the increased activity of oxacillin, gentamicin, and vancomycin, which could be explained by the direct activity of the compounds against the bacterial cell wall. All these compounds demonstrate excellent antibiofilm activity, when they inhibit and disrupt the biofilm of S. aureus in concentrations close to minimum inhibitory concentrations against planktonic cells. Expected interactions of the compounds with the cytoplasmic membrane are proven by in vitro crystal violet uptake assays.

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Section: Synergistic Effectsupporting

confidence: 56%

“…activities against the SA strains (5)(6)(7)(8). The relationships were characterized by r = 0.032 (5) and 0.052 (6)(7)(8).…”

Section: Structure-activity Relationshipsmentioning

confidence: 99%

Dibasic Derivatives of Phenylcarbamic Acid as Prospective Antibacterial Agents Interacting with Cytoplasmic Membrane

et al. 2020

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“…However, the change in pattern of resistance of pathogenic microbes to essential antibiotics, especially multidrug resistant once has diminished the effectiveness of known antibiotics [1]. As the frequencies of resistance are increasing worldwide, this poses a very serious danger to promotion of good health and all kinds of antibiotics, including the major last-ditch drug [2]. Therefore, there is need for evaluating alternative potential therapeutic agents with antimicrobial properties.…”

Section: Introductionmentioning

confidence: 99%

Comparison of Antimicrobial Potential of Honey Samples from Apis mellifera and Two Stingless Bees from Nsukka, Nigeria

Nweze¹,

Okafor²,

Nweze³

et al. 2016

J Pharmacogn Nat Prod

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The antimicrobial activity of honey depends on many factors, including its botanical origin, geographical and entomological source. The aim of this study was to evaluate and compare the antimicrobial potential of honey varieties from Apis mellifera, Hypotrigona sp. and Melipona sp. against MDR Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa ATCC 25783, Candida tropicalis, Candida albicans SC 5314 and Cryptococcus neoformans. By using standard microbiological procedure, the agar-well diffusion and broth microdilution methods were used to evaluate honey samples for their antimicrobial and non-peroxidase activity. Different concentrations of the honey samples showed inhibition zones diameter (mm) against the test isolates. The Minimum Inhibitory Concentrations (MICs) of the honey varieties from A. mellifera, Hypotrigona sp. and Melipona sp. ranged from 6.3-25.0%, 3.1-12.5% and 6.3-25.0% (v/v) respectively. There were no statistically significant differences between the mean MICs of honey varieties against E. coli, P. aeruginosa (ATCC 25783) and C. neoformans. Hypotrigona sp. honey had the least mean against most of the test organisms. The Minimum Biocidal Concentration (MBC) of the honey varieties from A. mellifera, Hypotrigona sp. and Melipona sp. against the test organisms varied from 6.3-50%, 3.1-25% and 12-50% (v/v) respectively. There were no significant differences between the mean MBCs of the honeys against MDR S. aureus (p=0.179), E. coli (p=0.564), P. aeruginosa (ATCC 25783) (p=0.846), and C. albicans (SC5314) (p=0.264). The honeys had some levels of non-peroxidase activity against E. coli, P. aeruginosa (ATCC 25783) and C. neoformans. This study has scientifically authenticated the potential use of stingless bee honeys from "Okotobo and Ifufu" as complementary therapeutic agents.

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“…In the last decade, however, research interest in antibiotic combinations has grown from the conventional use of two antibiotics to substituting one antibiotic with an unconventional over-the-counter consumer drug or prescription-only non-antibiotic drug. Examples of these efforts have expanded to include barbiturates, antipsychotics, antivirals and analgesics to improve the efficacy of antibiotic treatment [ 7 , 8 , 9 , 10 , 11 , 12 , 13 ]. Yet, these approaches are still in their infancy, and despite improved activity against some drug-resistant bacteria, some challenges still remain before clinical use is possible.…”

Section: Introductionmentioning

confidence: 99%

Recycling Antibiotics into GUMBOS: A New Combination Strategy to Combat Multi-Drug-Resistant Bacteria

2015

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Abstract:The emergence of multi-drug-resistant bacteria, coupled with the lack of new antibiotics in development, is fast evolving into a global crisis. New strategies utilizing existing antibacterial agents are urgently needed. We propose one such strategy in which four outmoded β-lactam antibiotics (ampicillin, carbenicillin, cephalothin and oxacillin) and a well-known antiseptic (chlorhexidine di-acetate) were fashioned into a group of uniform materials based on organic salts (GUMBOS) as an alternative to conventional combination drug dosing strategies. The antibacterial activity of precursor ions (e.g., chlorhexidine diacetate and β-lactam antibiotics), GUMBOS and their unreacted mixtures were studied with 25 clinical isolates with varying antibiotic resistance using a micro-broth dilution method. Acute cytotoxicity and therapeutic indices were determined using fibroblasts, endothelial and cervical cell lines. Intestinal permeability was predicted using a parallel artificial membrane permeability assay. GUMBOS formed from ineffective β-lactam antibiotics and cytotoxic chlorhexidine diacetate exhibited unique pharmacological properties and profound antibacterial activity at lower concentrations than the unreacted mixture of precursor ions at equivalent stoichiometry. Reduced cytotoxicity to invasive cell OPEN ACCESSMolecules 2015, 20 6467 types commonly found in superficial and chronic wounds was also observed using GUMBOS. GUMBOS show promise as an alternative combination drug strategy for treating wound infections caused by drug-resistant bacteria.

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Non‐Antibiotics – An Alternative for Microbial Resistance: Scope and Hope

Cited by 4 publications

References 132 publications

Dibasic Derivatives of Phenylcarbamic Acid as Prospective Antibacterial Agents Interacting with Cytoplasmic Membrane

Dibasic Derivatives of Phenylcarbamic Acid as Prospective Antibacterial Agents Interacting with Cytoplasmic Membrane

Comparison of Antimicrobial Potential of Honey Samples from Apis mellifera and Two Stingless Bees from Nsukka, Nigeria

Recycling Antibiotics into GUMBOS: A New Combination Strategy to Combat Multi-Drug-Resistant Bacteria

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