scholarly journals Synthesis and Antimicrobial Properties of Highly Cross-Linked pH-Sensitive Hydrogels through Gamma Radiation

Polymers ◽  
2021 ◽  
Vol 13 (14) ◽  
pp. 2223
Author(s):  
Moises Bustamante-Torres ◽  
Victor H. Pino-Ramos ◽  
David Romero-Fierro ◽  
Sandra P. Hidalgo-Bonilla ◽  
Héctor Magaña ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Film Formation ◽  
Antimicrobial Properties ◽  
Ph Sensitive ◽  
Scanning Calorimetry ◽  
Polymeric Systems ◽  
E Coli ◽  
High Prevalence

The design of new polymeric systems for antimicrobial drug release focused on medical/surgical procedures is of great interest in the biomedical area due to the high prevalence of bacterial infections in patients with wounds or burns. For this reason, in this work, we present a new design of pH-sensitive hydrogels copolymerized by a graft polymerization method (gamma rays), intended for localized prophylactic release of ciprofloxacin and silver nanoparticles (AgNPs) for potential topical bacterial infections. The synthesized hydrogels were copolymerized from acrylic acid (AAc) and agar. Cross-linked hydrogel film formation depended on monomer concentrations and the degree of radiation used (Cobalt-60). The obtained hydrogel films were characterized by attenuated total reflectance Fourier-transform infrared spectroscopy (ATR-FTIR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), and mechanical testing. The swelling of the hydrogels was evidenced by the influence of their pH-sensitiveness. The hydrogel was loaded with antimicrobial agents (AgNPs or ciprofloxacin), and their related activity was evaluated. Finally, the antimicrobial activity of biocidal-loaded hydrogel was tested against Escherichia coli (E. coli) and methicillin-resistant Staphylococcus aureus (MRSA) on in vitro conditions.

Antimicrobial Evaluation, Molecular Docking and ADME Properties of Indole Amide Derivatives

2021 ◽  
Vol 18 ◽  
Author(s):  
Derya Doğanay ◽  
Sevval M. Özcan ◽  
Ahmet M. Şentürk ◽  
Süreyya Ölgen
Keyword(s):  
Molecular Docking ◽  
In Silico ◽  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Antimicrobial Activities ◽  
In Vitro Tests ◽  
Lipinski’S Rule ◽  
Amide Derivatives

Background: Besides the viral infections, bacterial infections can cause serious and life-threatening complications and drug resistance is an important problem to fight bacterial infections. Therefore, it is important to discover novel antimicrobial agents to fight such infections. Objective: Several indole containing antimicrobial drug development studies have been reported in literature that provided strong evidences for good antimicrobial activities against a variety of microorganisms. Taken into consideration from these findings, antimicrobial properties of previously synthesized 16 indole amide derivatives were evaluated by in vitro tests against 14 different microorganisms, and also molecular docking and in silico prediction studies were used to identify structure-activity relationship of compounds. Methods: Antimicrobial activity of compounds was determined by disc diffusion and tube dilution methods. Molecular docking of compounds was studied to determine the relationship between the structure of compounds with DNA gyrase interactions of microorganisms by using the version of Autodock vina 4.2.6. Mol inspiration and Swiss ADME prediction online software programs were also used to identify drug-like properties of compounds. Results: The results showed that some compounds exhibited quite pronounced antibacterial and antifungal activities compared to reference drugs. These results were also supported by molecular docking studies and in silico ADME calculations presented that all tested compounds obey the Lipinski’s Rule of Five and are metabolized by CYP450 enzymes. Conclusion: It can be concluded that these results can be taken as reference in the development of new indole-based antimicrobial agents.

scholarly journals Synergy of Silver Nanoparticles and Aztreonam against Pseudomonas aeruginosa PAO1 Biofilms

2014 ◽  
Vol 58 (10) ◽  
pp. 5818-5830 ◽  
Author(s):  
Marc B. Habash ◽  
Amber J. Park ◽  
Emily C. Vis ◽  
Robert J. Harris ◽  
Cezar M. Khursigara
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Silver Nanoparticles ◽  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Cell Envelope ◽  
Antimicrobial Properties ◽  
Planktonic Cell ◽  
Chronic Infections ◽  
Content Type

ABSTRACTPathogenic bacterial biofilms, such as those found in the lungs of patients with cystic fibrosis (CF), exhibit increased antimicrobial resistance, due in part to the inherent architecture of the biofilm community. The protection provided by the biofilm limits antimicrobial dispersion and penetration and reduces the efficacy of antibiotics that normally inhibit planktonic cell growth. Thus, alternative antimicrobial strategies are required to combat persistent infections. The antimicrobial properties of silver have been known for decades, but silver and silver-containing compounds have recently seen renewed interest as antimicrobial agents for treating bacterial infections. The goal of this study was to assess the efficacy of citrate-capped silver nanoparticles (AgNPs) of various sizes, alone and in combination with the monobactam antibiotic aztreonam, to inhibitPseudomonas aeruginosaPAO1 biofilms. Among the different sizes of AgNPs examined, 10-nm nanoparticles were most effective in inhibiting the recovery ofP. aeruginosabiofilm cultures and showed synergy of inhibition when combined with sub-MIC levels of aztreonam. Visualization of biofilms treated with combinations of 10-nm AgNPs and aztreonam indicated that the synergistic bactericidal effects are likely caused by better penetration of the small AgNPs into the biofilm matrix, which enhances the deleterious effects of aztreonam against the cell envelope ofP. aeruginosawithin the biofilms. These data suggest that small AgNPs synergistically enhance the antimicrobial effects of aztreonam againstP. aeruginosain vitro, and they reveal a potential role for combinations of small AgNPs and antibiotics in treating patients with chronic infections.

scholarly journals Electrospun Scaffolds in Periodontal Wound Healing

Polymers ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 307
Author(s):  
Mária Budai-Szűcs ◽  
Marco Ruggeri ◽  
Angela Faccendini ◽  
Attila Léber ◽  
Silvia Rossi ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Bacterial Infections ◽  
Antimicrobial Properties ◽  
Periodontal Pocket ◽  
Scanning Calorimetry ◽  
Electrospun Scaffolds ◽  
Inflammatory Conditions ◽  
Nanofibrous Scaffolds ◽  
High Degree

Periodontitis is a set of inflammatory conditions affecting the tissues surrounding the teeth predominantly sustained by bacterial infections. The aim of the work was the design and the development of scaffolds based on biopolymers to be inserted in the periodontal pocket to restore tissue integrity and to treat bacterial infections. Nanofibrous scaffolds were prepared by means of electrospinning. Gelatin was considered as base component and was associated to low and high molecular weight chitosans and alginate. The scaffolds were characterized by chemico–physical properties (morphology, solid state-FTIR and differential scanning calorimetry (DSC)-surface zeta potential and contact angle), and mechanical properties. Moreover, preclinical properties (cytocompatibility, fibroblast and osteoblast adhesion and proliferation and antimicrobial properties) were assessed. All the scaffolds were based on cylindrical and smooth nanofibers and preserved their nanofibrous structure upon hydration independently of their composition. They possessed a high degree of hydrophilicity and negative zeta potentials in a physiological environment, suitable surface properties to enhance cell adhesion and proliferation and to inhibit bacteria attachment. The scaffold based on gelatin and low molecular weight chitosan proved to be effective in vitro to support both fibroblasts and osteoblasts adhesion and proliferation and to impair the proliferation of Streptococcus mutans and Aggregatibacter actinomycetemcomitans, both pathogens involved in periodontitis.

Evaluation of Antimicrobial of P. vesicularis, Streptococcus faecalis, Aeromonas hydrophilia, Salmonela typhae, Stphylococcus cohni, Serratia ficaria and E. coli. of crude and n-butanol fraction fruit latex of Carica papaya L. (Caricaceae)

2021 ◽  
pp. 92-94
Author(s):  
Kandikonda Maneesh ◽  
Kanakam Vijayabhaskar ◽  
Heena Firdouse ◽  
Pingali Srinivasa Rao ◽  
Mothukuri Prajwitha ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Bacterial Species ◽  
Antimicrobial Properties ◽  
Diffusion Method ◽  
Streptococcus Faecalis ◽  
E Coli ◽  
Butanol Fraction ◽  
Test Organisms ◽  
Aeromonas Hydrophilia

The current study was aimed to evaluate the antimicrobial properties of crude and N-Butanol fraction latex of C. papaya. Methods: in vitro antimicrobial activity The test organisms were P.vesicularis, streptococcus faecalis, Aeromonas hydrophilia, Salmonela typhae, Stphylococcus cohni, Serratia ficaria and E.coli. Ciprofloxacin was used as a control for investigating the bacterial species. The Zone of inhibition was determined forconcentration ranging from 12.5mg/ml to 50mg/ml. (12.5mg/ml, 25mg/ml, 37.5mg/ml, and 50mg/ml). Antibacterial activity tested for well diffusion method. Conclusion: It is concluded that the latex of C.papaya probably contains some valuable antimicrobial compounds that are crucial for inhibiting the growth of a wide variety of bacteria, especially Gram-negative bacteria and suggesting this for applying the treatment of a variety of bacterial infections.

scholarly journals Comparative in vitro Activities of Different Antibiotics against Clinical Isolates of Gram-negative Bacilli

2019 ◽  
pp. 1-8
Author(s):  
Sachin H. Jain ◽  
Pradnya Joshi
Keyword(s):  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Therapeutic Option ◽  
Critical Role ◽  
Final Analysis ◽  
Klebsiella Species ◽  
In Vitro Susceptibility ◽  
Gram Negative ◽  
E Coli

Objective: The local anti-microbial susceptibility profile plays a very critical role in guiding clinicians to choose the appropriate empiric therapies. This study was conducted to assess the pathogen characteristics and the in vitro susceptibility of different Gram negative isolates to commonly used antibiotics in our hospital settings. Methods: A total of 110 Gram negative isolates were included in the study.  A retrospective, observational analysis of antibiogram data was performed for four antimicrobial agents including CSE-1034 (ceftriaxone-sulbactam-EDTA), piperacillin-tazobactam (pip-taz), cefoperazone-sulbactam and meropenem.  Results: Of the 200 clinical specimens analysed, Gram negative isolates obtained from 110 samples were included in the final analysis. The most common Gram negative isolates were Klebsiella species (35.5%), E. coli (33.6%) and P. aeruginosa (21.8%). The overall susceptibility was highest to CSE-1034 (100%) followed by meropenem (66.4%), cefoperazone-sulbactam (56.4%) and pip-taz (45.5%). The MIC90 range of CSE-1034 for Enterobacteriaceae was ≤0.5-≤4μg/ml and ≤2μg/ml for susceptible P. aeruginosa isolates. The MIC90 of meropenem for 94.4% of meropenem-susceptible Enterobacteriaceae strains was <0.25μg/ml and 64.3% of P. aeruginosa were having MIC ≤0.25μg/ml. The MIC90 of pip-taz for 82.5% of the pip-taz susceptible Enterobacteriaceae strains was 4μg/ml and 63.6% of P. aeruginosa was ≤8.0μg/ml. The MIC90 of cefoperazone-sulbactam susceptible strains were between ≤8 to ≤16μg/ml and 45.8% isolates of susceptible P. aeruginosa were having MIC between ≤8 to ≤16μg/ml. Conclusions: Overall, this in vitro surveillance study suggests that CSE-1034 can be considered an important therapeutic option for the treatment of various multi drug resistant Gram-negative bacterial infections and avert the threat of resistance to last resort antibiotics including carbapenems.

Synthesis, In Vitro and In Silico Studies of Indolequinone Derivatives against Clinically Relevant Bacterial Pathogens

2020 ◽  
Vol 20 (3) ◽  
pp. 192-208 ◽  
Author(s):  
Talita Odriane Custodio Leite ◽  
Juliana Silva Novais ◽  
Beatriz Lima Cosenza de Carvalho ◽  
Vitor Francisco Ferreira ◽  
Leonardo Alves Miceli ◽  
...  
Keyword(s):  
In Silico ◽  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Mass Spectrometry Analysis ◽  
World Health ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Dione Derivative ◽  
In Silico Studies

Background: According to the World Health Organization, antimicrobial resistance is one of the most important public health threats of the 21st century. Therefore, there is an urgent need for the development of antimicrobial agents with new mechanism of action, especially those capable of evading known resistance mechanisms. Objective: We described the synthesis, in vitro antimicrobial evaluation, and in silico analysis of a series of 1H-indole-4,7-dione derivatives. Methods: The new series of 1H-indole-4,7-diones was prepared with good yield by using a copper(II)- mediated reaction between bromoquinone and β-enamino ketones bearing alkyl or phenyl groups attached to the nitrogen atom. The antimicrobial potential of indole derivatives was assessed. Molecular docking studies were also performed using AutoDock 4.2 for Windows. Characterization of all compounds was confirmed by one- and two-dimensional NMR techniques 1H and 13C NMR spectra [1H, 13C – APT, 1H x 1H – COSY, HSQC and HMBC], IR and mass spectrometry analysis. Results: Several indolequinone compounds showed effective antimicrobial profile against Grampositive (MIC = 16 µg.mL-1) and Gram-negative bacteria (MIC = 8 µg.mL-1) similar to antimicrobials current on the market. The 3-acetyl-1-(2,5-dimethylphenyl)-1H-indole-4,7-dione derivative exhibited an important effect against different biofilm stages formed by a serious hospital life-threatening resistant strain of Methicillin-Resistant Staphylococcus aureus (MRSA). A hemocompatibility profile analysis based on in vitro hemolysis assays revealed the low toxicity effects of this new series. Indeed, in silico studies showed a good pharmacokinetics and toxicological profiles for all indolequinone derivatives, reinforcing their feasibility to display a promising oral bioavailability. An elucidation of the promising indolequinone derivatives binding mode was achieved, showing interactions with important sites to biological activity of S. aureus DNA gyrase. These results highlighted 3-acetyl-1-(2-hydroxyethyl)-1Hindole- 4,7-dione derivative as broad-spectrum antimicrobial prototype to be further explored for treating bacterial infections. Conclusion: The highly substituted indolequinones were obtained in moderate to good yields. The pharmacological study indicated that these compounds should be exploited in the search for a leading substance in a project aimed at obtaining new antimicrobials effective against Gram-negative bacteria.

scholarly journals Silver (I) N-Heterocyclic Carbene Complexes: A Winning and Broad Spectrum of Antimicrobial Properties

2021 ◽  
Vol 22 (5) ◽  
pp. 2497
Author(s):  
Filippo Prencipe ◽  
Anna Zanfardino ◽  
Michela Di Napoli ◽  
Filomena Rossi ◽  
Stefano D’Errico ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Resistance Mechanisms ◽  
Heterocyclic Carbenes ◽  
Significant Activity ◽  
Bacterial Strains ◽  
Development Of Resistance ◽  
Starting Point ◽  
Catalytic Chemistry

The evolution of antibacterial resistance has arisen as the main downside in fighting bacterial infections pushing researchers to develop novel, more potent and multimodal alternative drugs.Silver and its complexes have long been used as antimicrobial agents in medicine due to the lack of silver resistance and the effectiveness at low concentration as well as to their low toxicities compared to the most commonly used antibiotics. N-Heterocyclic Carbenes (NHCs) have been extensively employed to coordinate transition metals mainly for catalytic chemistry. However, more recently, NHC ligands have been applied as carrier molecules for metals in anticancer applications. In the present study we selected from literature two NHC-carbene based on acridinescaffoldand detailed nonclassicalpyrazole derived mono NHC-Ag neutral and bis NHC-Ag cationic complexes. Their inhibitor effect on bacterial strains Gram-negative and positivewas evaluated. Imidazolium NHC silver complex containing the acridine chromophore showed effectiveness at extremely low MIC values. Although pyrazole NHC silver complexes are less active than the acridine NHC-silver, they represent the first example of this class of compounds with antimicrobial properties. Moreover all complexesare not toxic and they show not significant activity againstmammalian cells (Hek lines) after 4 and 24 h. Based on our experimental evidence, we are confident that this promising class of complexes could represent a valuable starting point for developing candidates for the treatment of bacterial infections, delivering great effectiveness and avoiding the development of resistance mechanisms.

Antimicrobial Screening, in Silico Studies and QSAR of Chalcone-based 1,4-disubstituted 1,2,3-triazole Hybrids

Drug Research ◽  
2020 ◽  
Author(s):  
Pinki Yadav ◽  
Kashmiri Lal ◽  
Ashwani Kumar
Keyword(s):  
Topoisomerase Ii ◽  
Antimicrobial Properties ◽  
Qsar Model ◽  
Quantitative Structure Activity Relationship ◽  
Binding Modes ◽  
E Coli ◽  
Structure Activity ◽  
In Silico Studies ◽  
Microbial Strains

AbstractThe in vitro antimicrobial properties of some chalcones (1a–1c ) and chalcone tethred 1,4-disubstituted 1,2,3-triazoles (2a–2u) towards different microbial strains viz. Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger and Candida albicans are reported. Compounds 2g and 2u exhibited better potency than the standard Fluconazole with MIC values of 0.0063 µmol/mL and 0.0068 µmol/mL, respectively. Furthermore, molecular docking was performed to investigate the binding modes of two potent compounds 2q and 2g with E. coli topoisomerase II DNA gyrase B and C. albicans lanosterol 14α-demethylase, respectively. Based on these results, a statistically significant quantitative structure activity relationship (QSAR) model was successfully summarized for antibacterial activity against B. subtilis.

scholarly journals An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Resin Composite ◽  
Antimicrobial Properties ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Oral Pathogens

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.

scholarly journals Conditions to Prolonged Release of Microencapsulated Carvacrol on Alginate Films as Affected by Emulsifier Type and PH

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Silvia Matiacevich ◽  
Natalia Riquelme ◽  
María Lidia Herrera
Keyword(s):  
Storage Time ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Edible Film ◽  
Initial Time ◽  
Tween 20 ◽  
Prolonged Release ◽  
E Coli ◽  
Fresh Foods

Alginate from algal biomass is used as edible film and the incorporation of antimicrobial agents improves its performance to increase the shelf-life of fresh foods. However, environmental conditions and intrinsic properties of films influence their release. The aim of this study was to investigate the effect of the concentration and type of encapsulating agent and pH of emulsions on the physical and antimicrobial properties of alginate-carvacrol films. Films containing alginate, carvacrol as antimicrobial agent, and Tween 20 or trehalose (0.25 and 0.75% w/w) as encapsulating agents were obtained from suspensions at pH 4 and pH 8. Physical characterization of emulsions and films and antimicrobial properties (E. coliandB. cinerea) was evaluated. Results showed that droplets size depended on trehalose concentration, but emulsion stability depended on pH and type of encapsulating agent, being more stable samples with trehalose at pH 4. Although films with Tween 20 presented the highest opacity, they showed the best antimicrobial properties at initial time; however, during storage time, they lost their activity before samples with trehalose and relative humidity (RH) was the principal factor to influence their release. Therefore, sample formulated with 0.25% trehalose at pH 4 and stored at 75% RH had the best potential as edible film for fresh fruits.

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