scholarly journals Nanotechnological Advancement in Antimicrobial Drug Designing

2021 ◽  
Author(s):  
Mohammad Oves ◽  
Mohd Ahmar Rauf
Keyword(s):  
Antibacterial Properties ◽  
Multidrug Resistant ◽  
Global Public Health ◽  
Drug Designing ◽  
Global Spread ◽  
Microbial Infections ◽  
Biological Contaminants ◽  
Significant Area ◽  
Improved Methods ◽  
The Way

The global spread of multidrug-resistant (MDR) microbial infections is currently one of the most severe risks to global public health, with 10 million fatalities expected by 2050 unless action is taken. Nanotechnology has revolutionized science and medicine. The reliance on nanotechnology is growing. Nanoparticles have distinct properties that improve biological, chemical, and physical properties studied for various uses. A significant area of attention in the synthesis of nanoscale modulators is the utilization of crude formulations, retro-synthesized, and pure chemicals, mainly from herbal sources, with fewer adverse effects. Green chemistry has devised a tangential technique for synthesizing metals and metal oxides to produce nanoparticles. Plant extracts (leaves, stems, and shoots) and microorganisms (bacteria, fungus, and yeast) are used as reducing intermediates to make nanoparticles. Studies in microbiology have shown that nanoparticles kill bacteria, fungi, viruses, and protozoa. These green nanoparticles contain antibacterial, antifungal, and anti-inflammatory effects. Most nanoparticles have high antibacterial properties, indicating they may be used to combat diseases and biological contaminants. These nanoparticles have antibacterial action against pathogenic microorganisms that cause serious illnesses, including multidrug-resistant pathogens. The current research will pave the way for future applications and improved methods for producing nanoparticles, paving the way for an innovative route in nano-life sciences with widespread recognition.

scholarly journals Synthesis, Structure Elucidation, Antibacterial Activities, and Synergistic Effects of Novel Juglone and Naphthazarin Derivatives Against Clinical Methicillin-Resistant Staphylococcus aureus Strains

2021 ◽  
Vol 9 ◽  
Author(s):  
Valentin Duvauchelle ◽  
Chaimae Majdi ◽  
David Bénimélis ◽  
Catherine Dunyach-Remy ◽  
Patrick Meffre ◽  
...  
Keyword(s):  
Synergistic Effects ◽  
Antibacterial Properties ◽  
Clinical Importance ◽  
Antibacterial Activities ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Global Public Health ◽  
Gram Positive ◽  
Drug Resistant Bacteria ◽  
Mrsa Strains

Infections caused by drug-resistant bacteria are a serious threat to human and global public health. Moreover, in recent years, very few antibiotics have been discovered and developed by pharmaceutical companies. Therefore, there is an urgent need to discover and develop new antibacterial agents to combat multidrug-resistant bacteria. In this study, two novel series of juglone/naphthazarin derivatives (43 compounds) were synthesized and evaluated for their antibacterial properties against various clinical and reference Gram-positive MSSA, clinical Gram-positive MRSA, and clinical and reference Gram-negative bacteria E. coli and P. aeruginosa. These strains are of clinical importance because they belong to ESKAPE pathogens. Compounds 3al, 5ag, and 3bg showed promising activity against clinical and reference MSSA (MIC: 1–8 µg/ml) and good efficacy against clinical MRSA (MIC: 2–8 µg/ml) strains. 5am and 3bm demonstrated better activity on both MSSA (MIC: 0.5 µg/ml) and MRSA (MIC: 2 µg/ml) strains. Their MICs were similar to those of cloxacillin against clinical MRSA strains. The synergistic effects of active compounds 3al, 5ag, 5am, 3bg, and 3bm were evaluated with reference antibiotics, and it was found that the antibiotic combination with 3bm efficiently enhanced the antimicrobial activity. Compound 3bm was found to restore the sensitivity of clinical MRSA to cloxacillin and enhanced the antibacterial activity of vancomycin when they were added together. In the presence of 3bm, the MIC values of vancomycin and cloxacillin were lowered up to 1/16th of the original MIC with an FIC index of 0.313. Moreover, compounds 3al, 5ag, 5am, 3bg, and 3bm did not present hemolytic activity on sheep red blood cells. In silico prediction of ADME profile parameter results for 3bm is promising and encouraging for further development.

Modulation of the drug resistance by Platonia insignis Mart. extract, ethyl acetate fraction and Morelloflavone/Volkensiflavone (biflavonoids) in Staphylococcus aureus strains overexpressing efflux pump genes

2020 ◽  
Vol 21 ◽  
Author(s):  
Andressa Kelly Ferreira e Silva ◽  
Antonielly Campinho dos Reis ◽  
Emanuelly Elanny Andrade Pinheiroc ◽  
Jonas Nascimento de Sousa ◽  
Felipe Araújo de Alcântara Oliveira ◽  
...  
Keyword(s):  
Natural Products ◽  
Ethyl Acetate ◽  
Native Species ◽  
Efflux Pump ◽  
Public Health Problem ◽  
Ethyl Acetate Fraction ◽  
Multidrug Resistant ◽  
Global Public Health ◽  
Minimal Inhibitory Concentrations ◽  
Subinhibitory Concentrations

Background: Microbial resistance to antibiotics is a global public health problem, which requires urgent attention. Platonia insignis is a native species from the eastern Brazilian Amazon, used in the treatment of burns and wounds. Objectives: To evaluate the antimicrobial activity of the hydroalcoholic extract of P. insignis (PIHA), the ethyl acetate fraction (PIAE), and its subfraction containing a mixture of biflavonoids (BF). Moreover, the effect of these natural products on the antibiotic activity against S. aureus strains overexpressing efflux pump genes was also evaluated. Methods: Minimal inhibitory concentrations were determined against different species of microorganisms. To evaluate the modulatory effect on the Norfloxacin-resistance, the MIC of this antibiotic was determined in the absence and presence of the natural products at subinhibitory concentrations. Inhibition of the EtBr efflux assays were conducted in the absence or presence of the natural products. Results: PIHA showed a microbicidal effect against S. aureus and C. albicans, while PIAE was bacteriosctatic for S. aureus. PIAE and BF at subinhibitory concentrations were able to reduce the MIC of Norfloxacin acting as modulating agents. BF was able to inhibit the efflux of EtBr efflux in S. aureus strains overexpressing specific efflux pump genes. Conclusion: P. inignisis a source of efflux pump inhibitors, including volkensiflavone and morelloflavone which were able to potentiate the Norfloxacin activity by NorA inhibition, being also able to inhibit QacA/B, TetK and MsrA. Volkensiflavone and morelloflavone could be used as adjuvant in the antibiotic therapy of multidrug resistant S. aureus strains overexpressing efflux pumps.

scholarly journals A novel chemical biology and computational approach to expedite the discovery of new-generation polymyxins against life-threatening Acinetobacter baumannii

2021 ◽  
Author(s):  
Xukai Jiang ◽  
Nitin A. Patil ◽  
Mohammad A. K. Azad ◽  
Hasini Wickremasinghe ◽  
Heidi Yu ◽  
...  
Keyword(s):  
Public Health ◽  
Chemical Biology ◽  
Multidrug Resistant ◽  
Computational Approach ◽  
Gram Negative Bacteria ◽  
Global Public Health ◽  
Gram Negative ◽  
Life Threatening ◽  
New Generation ◽  
Novel Antibiotics

Multidrug-resistant Gram-negative bacteria have been an urgent threat to global public health. Novel antibiotics are desperately needed to combat these 'superbugs'.

scholarly journals Antibacterial Activity of Moroccan Zantaz Honey and the Influence of Its Physicochemical Parameters Using Chemometric Tools

2021 ◽  
Vol 11 (10) ◽  
pp. 4675
Author(s):  
Youssef Elamine ◽  
Hamada Imtara ◽  
Maria Graça Miguel ◽  
Ofélia Anjos ◽  
Letícia M. Estevinho ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Properties ◽  
Principal Component ◽  
Physicochemical Characteristics ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Coumaric Acid ◽  
Atlas Mountains ◽  
Methyl Syringate ◽  
Chemometric Tools

The emergence of multidrug-resistant bacteria has prompted the development of alternative therapies, including the use of natural products with antibacterial properties. The antibacterial properties of Zantaz honey produced in the Moroccan Atlas Mountains against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus was evaluated and analyzed using chemometric tools. Minimum inhibitory concentration (MIC) and Minimum bactericidal concentration (MBC) against S. aureus were the lowest (112.5 ± 54.5 mg/mL), revealing that this species was most sensitive to Zantaz honey. P. aeruginosa showed an intermediate sensitivity (MIC= 118.75 ± 51.9 mg/mL), while E. coli was the most resistant to treatment (MIC = 175 ± 61.2 mg/mL). Content of monosaccharides, certain minerals, and phenolic compounds correlated with antibacterial activity (p < 0.05). Principal component analysis of physicochemical characteristics and antibacterial activity indicated that the parameters most associated with antibacterial activity were color, acidity, and content of melanoidins, fructose, epicatechin, methyl syringate, 4-coumaric acid, and 3-coumaric acid.

Antibacterial properties of phenothiazine derivatives against multidrug‐resistant Acinetobacter baumannii strains

2021 ◽  
Author(s):  
Laura Aguilar‐Vega ◽  
Luis Esaú López‐Jácome ◽  
Bernardo Franco ◽  
Sergio Muñoz‐Carranza ◽  
Naurú Vargas‐Maya ◽  
...  
Keyword(s):  
Acinetobacter Baumannii ◽  
Antibacterial Properties ◽  
Multidrug Resistant ◽  
Phenothiazine Derivatives

scholarly journals The Synergistic Effect of Biosynthesized Silver Nanoparticles and Phage ZCSE2 as a Novel Approach to Combat Multidrug-Resistant Salmonella enterica

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 678
Author(s):  
Abdallah S. Abdelsattar ◽  
Rana Nofal ◽  
Salsabil Makky ◽  
Anan Safwat ◽  
Amera Taha ◽  
...  
Keyword(s):  
Silver Nanoparticles ◽  
Color Change ◽  
Antibacterial Properties ◽  
Multidrug Resistant ◽  
Inhibitory Effect ◽  
Health Concern ◽  
Resistant Bacteria ◽  
Mortality And Morbidity ◽  
Novel Approach ◽  
Transmission Electron

The emergence and evolution of antibiotic-resistant bacteria is considered a public health concern. Salmonella is one of the most common pathogens that cause high mortality and morbidity rates in humans, animals, and poultry annually. In this work, we developed a combination of silver nanoparticles (AgNPs) with bacteriophage (phage) as an antimicrobial agent to control microbial growth. The synthesized AgNPs with propolis were characterized by testing their color change from transparent to deep brown by transmission electron microscopy (TEM) and Fourier-Transform Infrared Spectroscopy (FTIR). The phage ZCSE2 was found to be stable when combined with AgNPs. Both minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were evaluated for AgNPs, phage, and their combination. The results indicated that MIC and MBC values were equal to 23 µg/mL against Salmonella bacteria at a concentration of 107 CFU/mL. The combination of 0.4× MIC from AgNPs and phage with Multiplicity of Infection (MOI) 0.1 showed an inhibitory effect. This combination of AgNPs and phage offers a prospect of nanoparticles with significantly enhanced antibacterial properties and therapeutic performance.

scholarly journals 166. Activity of a Novel β-lactamase Inhibitor QPX7728 Combined With β-lactams Against st258 klebsiella Pneumoniae and st131 escherchia Coli Isolates Producing β-lactamases

2020 ◽  
Vol 7 (Supplement_1) ◽  
pp. S212-S213
Author(s):  
Mariana Castanheira ◽  
Jill Lindley ◽  
Timothy B Doyle ◽  
Andrew P Davis ◽  
Olga Lomovskaya
Keyword(s):  
Multidrug Resistant ◽  
Chemical Diversity ◽  
Sequencing Analysis ◽  
E Coli ◽  
Escherchia Coli ◽  
Global Spread ◽  
Encoding Genes ◽  
Center Research ◽  
Lactamase Inhibitor ◽  
Research Grant

Abstract Background ST258 K. pneumoniae and ST131 E. coli clones are considered vectors for the global spread of multidrug resistance. We evaluated the activity of β-lactams in combination with QPX7728, a novel β-lactamase inhibitor active against all β-lactamase classes, against a collection of 210 isolates belonging to these clones collected from a worldwide surveillance study. Methods A total of 118 ST258 K. pneumoniae and 92 ST131 E. coli (single loci variant also included) were susceptibility tested by reference broth microdilution against various β-lactams ± QPX7728 and comparator agents. All isolates were screened for β-lactamases using whole genome sequencing analysis. Results All β-lactam agents had limited activity against 118 ST258 K. pneumoniae (1.7–7.6% susceptible). Among these, 104 carried carbapenemase-encoding genes: 66 KPC variants, 20 NDM and 17 OXA-48-like. One isolate carried 2 carbapenemases. The addition of QPX7728 at 4 mg/L or 8 mg/L lowered the MICs for cefepime (MIC50/90, 0.25/1 mg/L and MIC50/90, 0.12/0.5 mg/L), ceftolozane (MIC50/90, 0.5/ &gt; 32 mg/L and MIC50/90, 0.25/16 mg/L), ertapenem (MIC50/90, 0.12/2 mg/L and MIC50/90, 0.06/0.5 mg/L), and meropenem (MIC50/90, 0.06/0.5 mg/L and MIC50/90, 0.03/0.12 mg/L; Table). QPX7728 at 4 mg/L reduced the ceftibuten (MIC50/90, 0.25/8 mg/L) or tebipenem (MIC50/90, 0.12/2 mg/L) MICs for ST258 isolates. E. coli ST131 carried mainly CTX-M variant (85 isolates), but 6 isolates harbored carbapenemases. Carbapenems were the only β-lactams displaying &gt; 80.0% activity against ST131 E. coli, followed by piperacillin-tazobactam (79.3% susceptible). Only 5.4%and 41.3% ST131 isolates were susceptible to cefepime and ceftibuten, respectively. MIC50/MIC90 values for these agents with QPX7728 were ≤ 0.015/≤ 0.015 mg/L for cefepime and ≤ 0.015/0.06 mg/L for ceftolozane with the inhibitor at 8 mg/L and ≤ 0.015/0.03 mg/L for ceftibuten with the inhibitor at 4 mg/L. Conclusion QPX7728 lowered the MICs for all agents tested to clinically achievable levels when tested against isolates multidrug resistant belonging to important clones responsible to the dissemination of KPC, CTX variants, and metallo-β-lactamases. The development of this broad β-lactamase inhibitor should be pursued. Table 1 Disclosures Mariana Castanheira, PhD, 1928 Diagnostics (Research Grant or Support)A. Menarini Industrie Farmaceutiche Riunite S.R.L. (Research Grant or Support)Allergan (Research Grant or Support)Allergan (Research Grant or Support)Amplyx Pharmaceuticals (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Fox Chase Chemical Diversity Center (Research Grant or Support)GlaxoSmithKline (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Merck (Research Grant or Support)Merck (Research Grant or Support)Merck & Co, Inc. (Research Grant or Support)Merck & Co, Inc. (Research Grant or Support)Paratek Pharma, LLC (Research Grant or Support)Pfizer (Research Grant or Support)Qpex Biopharma (Research Grant or Support) Jill Lindley, Allergan (Research Grant or Support)Qpex Biopharma (Research Grant or Support) Timothy B. Doyle, Allergan (Research Grant or Support)Allergan (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Pfizer (Research Grant or Support)Qpex Biopharma (Research Grant or Support) Olga Lomovskaya, PhD, Qpex Biopharma (Employee)

Effect of Silver Ions on the Structural and Antibacterial Properties of Bone Replacement Material

2013 ◽  
Vol 795 ◽  
pp. 692-696 ◽  
Author(s):  
Nida Iqbal ◽  
Mohammed Rafiq Abdul Kadir ◽  
Nasrul Humaimi Bin Mahmood ◽  
Micheal Moses ◽  
Mashitah Binti Mad Salim ◽  
...  
Keyword(s):  
Calcium Phosphates ◽  
Bacterial Species ◽  
Calcium Nitrate ◽  
Antibacterial Properties ◽  
Silver Ions ◽  
Antibacterial Activities ◽  
Silver Addition ◽  
Wide Range ◽  
Microbial Infections ◽  
Inorganic Mineral

Antibacterial materials based on calcium phosphates have wide range of biomedical applications in the prevention of microbial infections. The synthesis of inorganic mineral component of bone i.e. hydroxyapatite was done with the addition of silver (Ag) (5-15 wt %) as antibacterial agent. The wet precipitation synthesis was carried out using diammonium hydrogen phosphate and calcium nitrate as P and Ca precursors. The presence and effect of silver addition on the structure was studied using Fourier Transform-Infrared (FTIR) spectroscopy and Energy Dispersive X-ray (EDX) techniques. The antibacterial properties of all samples were evaluated using Disc Diffusion Technique (DDT) againstS. aureus,B. subtilis, P. aeruginosaandE. coli. Antibacterial activities of samples were found to vary depending on the bacterial species and Ag loading percentage. The antibacterial assay suggested that the addition of Ag ions within hydroxyapatite can be effectively provided the required level of antibacterial activity against bacteria.

scholarly journals PUNICA GRANATUM RIND EXTRACT: ANTIBIOTIC POTENTIATOR AND EFFLUX PUMP INHIBITOR OF MULTIDRUG RESISTANT KLEBSIELLA PNEUMONIAE CLINICAL ISOLATES

2017 ◽  
Vol 10 (3) ◽  
pp. 191 ◽  
Author(s):  
Zumaana Rafiq ◽  
Sreevidya Narasimhan ◽  
Magesh Haridoss ◽  
Rosy Vennila ◽  
Rama Vaidyanathan
Keyword(s):  
Klebsiella Pneumoniae ◽  
Efflux Pump ◽  
Ethanol Extract ◽  
Punica Granatum ◽  
Multidrug Resistant ◽  
Synergistic Activity ◽  
Sequential Fractionation ◽  
Efflux Pump Inhibitor ◽  
Fold Reduction ◽  
Significant Area

ABSTRACTObjective: With a rise in multidrug resistant (MDR) bacterial isolates, search for antibiotics or compounds that could act synergistically with themis a significant area of research. Efflux-mediated resistance, in particular, is a great hurdle that needs to be overcome. In an effort to identify suchsynergistic compounds and potential efflux pump inhibitors (EPI), we analyzed the rind of Punica granatum (pomegranate) against MDR clinicalKlebsiella pneumoniae isolates.Methods: Sequential fractionation of P. granatum rind ethanol (PGR) extract was carried out to obtain hexane, butanol and water fractions.Antibacterial activity of the plant extracts was confirmed, and synergistic interaction with antibiotics was determined by the checkerboard assay. Gaschromatography-mass spectrometry (GC-MS) analysis was performed to identify the phytochemical constituents of the hexane extract. To study EPIactivity of the extracts, norfloxacin accumulation assay was carried out.Results: PGR ethanol extract was found to have synergistic activity with ciprofloxacin, levofloxacin, ceftazidime, cefoxitin, meropenem, and gentamicinresulting in fold decrease of minimum inhibitory concentration (MIC) ranging from 2 to 32 fold. The hexane fraction was found to have maximumsynergistic activity resulting in a 32-fold reduction of ciprofloxacin MIC followed by butanol and water fractions. The PGR ethanol extract was alsofound to have efflux inhibition activity by the norfloxacin accumulation assay. Of the sequential fractions, the butanol fraction had maximum effluxinhibition activity.Conclusion: Therefore, our study shows that PGR extract can potentiate the effect of antibiotics on MDR bacteria, and the mode of action is likely tobe due to EPI.Keywords: Punica granatum rind, Pomegranate, Synergy with antibiotics, Multidrug resistant, Klebsiella pneumoniae, Efflux pump inhibition.

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