scholarly journals The Synthesis and Evaluation of Aminocoumarin Peptidomimetics as Cytotoxic Agents on Model Bacterial E. coli Strains

Materials ◽  
2021 ◽  
Vol 14 (19) ◽  
pp. 5725
Author(s):  
Paweł Kowalczyk ◽  
Monika Wilk ◽  
Parul Parul ◽  
Mateusz Szymczak ◽  
Karol Kramkowski ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Free Acid ◽  
Antimicrobial Properties ◽  
Acid Group ◽  
Ester Group ◽  
Biological Properties ◽  
Cytotoxic Agents ◽  
Coumarin Derivatives ◽  
Bacterial Strains ◽  
E Coli

This work presents the successful synthesis of a library of novel peptidomimetics via Ugi multicomponent reaction. Most of these peptidomimetics contain differently substituted aminocoumarin; 7-amino-4-methylcoumarin and 7-amino-4-(trifluoromethyl) coumarin. Inspired by the biological properties of coumarin derivatives and peptidomimetics, we proposed the synthesis of coumarin incorporated peptidomimetics. We studied the potential of synthesized compounds as antimicrobial drugs on model E. coli bacterial strains (k12 and R2–R4). To highlight the importance of coumarin in antimicrobial resistance, we also synthesized the structurally similar peptidomimetics, using benzylamine. Preliminary cellular studies suggest that the compounds with coumarin derivatives have more potential as antimicrobial agents compared to the compounds without coumarin. We also analyzed the effect of aldehyde, free acid group and ester group on the course of their antimicrobial properties.

Organic additives as antimicrobial agents in thermoplastics compounds

2016 ◽  
Vol 1817 ◽  
Author(s):  
Daiane Tomacheski ◽  
Michele Pittol ◽  
Vanda F. Ribeiro ◽  
Ruth M. C. Santana
Keyword(s):  
Electron Microscopy ◽  
Mechanical Properties ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Organic Additives ◽  
Bacterial Strains ◽  
Melt Mixing ◽  
Polymeric Matrices ◽  
E Coli ◽  
Scanning Electron

ABSTRACTDevelopment of polymers with antimicrobial characteristics can avoid deterioration and assist in containing spread of pathogens harmful to human health. This study aimed to compare the antimicrobial and mechanical properties of polymeric matrices containing organic antimicrobial additives. Silver organomodified bentonite (Ag_bentonite) and organochlorine molecule in a masterbatch based polyethylene (Cl_PE) were tested in proportion of 2% in a thermoplastic elastomeric formulation. The polymeric matrices were prepared by melt mixing and evaluated in tensile and antimicrobial properties against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli) strains. The additives were characterized by thermogravimetric analysis (TGA) and scanning electron microscopy (SEM). The nanoscale of Ag_bentonite was verified by SEM. TGA assay showed that Cl_PE is more sensitive to heat than Ag_bentonite. As a result of this lower thermal stability, the addition of Cl_PE reduced the tensile properties of the compound. The sample with Cl_PE was effective against both bacterial strains, reducing the populations of S. aureus and E. coli in 99 and 96%, respectively. The addition of Ag_bentonite did not affect the tensile strength and decreased in 97 and 40% S. aureus and E. coli populations, respectively. The results indicate that the use of organic additives is promissory, but further modifications in processing must be necessary.

Modifications of Isoalantolactone Leading to Effective Antibacterial and Antiviral Compounds

2020 ◽  
Vol 17 ◽  
Author(s):  
Sergey S. Patrushev ◽  
Lyubov G. Burova ◽  
Anna A. Shtro ◽  
Tatyana V. Rybalova ◽  
Dmitry S. Baev ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antiviral Activity ◽  
Influenza A ◽  
Antimicrobial Agents ◽  
Sesquiterpene Lactones ◽  
Biological Properties ◽  
Bacterial Strains ◽  
E Coli ◽  
Wide Range

Background: Natural sesquiterpene lactones are an important class of heterocyclic compounds in drug discovery since they are possessed a wide range of biological properties including antibacterial activity. Objective: The objective of this study was to synthesize of isoalantolactone derivatives with a furo[2,3-d]pyrimidin-2-оne moiety and to evaluate their antibacterial and antiviral activity. Methods: The Sonogashira cross-coupling and subsequent Ag-catalyzed cyclization reactions were the main routes of synthesis. The antibacterial activity and the ability to inhibit biofilms formation on E. coli, S. aureus, A. viscosus, P. aeruginosa and E. faecalis bacterial strains were evaluated. A study of the molecular interactions of new compounds with the multiple virulence factor regulators was performed using docking simulations. The antiviral activity against influenza A virus and human orthopneumovirus H-2А was also studied. Results: The in vitro antibacterial activity for 4 (MIC = 58.33±4.41 μg/mL) concerning E. coli and 5 (MIC = 96.5±3.25 μg/mL) against A. viscosus and the inhibition of biofilm formation for compounds 2, 4, and 5 on E. coli, S. aureus, P. aeruginosa and E. faecalis bacterial strains has been of interest for the search of improved antimicrobial agents. Compound 3 was endowed with antiviral activity to human orthopneumovirus H-2А with SI >33. The activity of the new type of hybrid compounds is depended on the substituent in the 6th position of furo[2,3-d]pyrimidin-2-one fragment. Conclusion: The decoration of isoalantolactone with a furo[2,3-d]pyrimidin-2-one fragment led to perspective antiviral and antimicrobial agents. Due to antimicrobial activity, pyridine-4-yl substituted isoalantolactone-furopyrimidinone hybrid is considered as a candidate compound to participate in further research.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

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.

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.

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.

scholarly journals DPPH-Scavenging and Antimicrobial Activities of Asteraceae Medicinal Plants on Uropathogenic Bacteria

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Phan-Canh Trinh ◽  
Le-Thi-Thanh Thao ◽  
Hoang-Tran-Viet Ha ◽  
TuAnh Nguyen
Keyword(s):  
Antimicrobial Agents ◽  
Natural Antioxidants ◽  
Ethyl Acetate Fraction ◽  
Antimicrobial Activities ◽  
Chrysanthemum Morifolium ◽  
Bacterial Strains ◽  
Ageratum Conyzoides ◽  
Potent Effect ◽  
E Coli ◽  
Dpph Scavenging

Asteraceae species were widely applied in traditional medicines in Asian countries as sources of natural antioxidants and antimicrobial agents. This study aimed to evaluate DPPH-scavenging capacities and antimicrobial activities of nine Asteraceae species collected from Southern Vietnam. Antioxidant and antimicrobial activities were determined by standard protocols. Essential oils from Ageratum conyzoides, Helianthus annuus, and Artemisia vulgaris indicated significant inhibitory effects on Staphylococcus aureus and Candida spp. Crude extracts and fractions from Taraxacum officinale, Chrysanthemum morifolium, A. conyzoides, and Tagetes erecta showed inhibitory ability on at least one testing bacterial strains including S. aureus, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. In a study on clinical isolates, ethyl acetate fraction from A. conyzoides flower displayed the most potent effect on uropathogenic E. coli and K. pneumoniae with MIC at 1.25–10 mg/ml and 5–12.5 mg/ml, respectively. DPPH-scavenging assay indicated that T. erecta extract had the lowest IC50 (17.280 μg/ml) and is 2.4 times higher than vitamin C (7.321 μg/ml). This study revealed that A. conyzoides has good potential against uropathogenic E. coli and K. pneumoniae, and therefore could be applied for prophylactic treatment of urinary infection.

scholarly journals Viability of lactic acid bacteria in different components of Ogi with anti diarrhoeagenic E. coli activities

2019 ◽  
Vol 3 (6) ◽  
pp. 206-213
Author(s):  
Roseline Eleojo Kwasi ◽  
Iyanuoluwa Gladys Aremu ◽  
Qudus Olamide Dosunmu ◽  
Funmilola A. Ayeni
Keyword(s):  
Lactic Acid ◽  
Lactic Acid Bacteria ◽  
Antimicrobial Properties ◽  
Culture Method ◽  
Antimicrobial Activities ◽  
Drying Methods ◽  
Bacterial Strains ◽  
E Coli ◽  
Log Reduction ◽  
Freeze Dried

Background: Ogi constitutes a rich source of lactic acid bacteria (LAB) with associated health benefits to humans through antimicrobial activities. However, the high viability of LAB in Ogi and its supernatant (Omidun) is essential. Aims: This study was carried out to assess the viability of LAB in various forms of modified and natural Ogi and the antimicrobial properties of Omidun against diarrhoeagenic E coli. Methods and Material: The viability of LAB was assessed in fermented Ogi slurry and Omidun for one month and also freeze-dried Ogi with and without added bacterial strains for two months. A further 10 days viability study of modified Omidun, refrigerated Omidun, and normal Ogi was performed. The antimicrobial effects of modified Omidun against five selected strains of diarrhoeagenic E. coli (DEC) were evaluated by the co-culture method. Results: Both drying methods significantly affected carotenoids and phenolic compounds. The Ogi slurry had viable LAB only for 10 days after which, there was a succession of fungi and yeast. Omidun showed 2 log10cfu/ml reduction of LAB count each week and the freeze-dried Ogi showed progressive reduction in viability. Refrigerated Omidun has little viable LAB, while higher viability was seen in modified Omidun (≥2 log cfu/ml) than normal Omidun. Modified Omidun intervention led to 2-4 log reduction in diarrhoeagenic E. coli strains and total inactivation of shigella-toxin producing E. coli H66D strain in co-culture. Conclusions: The consumption of Ogi should be within 10 days of milling using modified Omidun. There are practical potentials of consumption of Omidun in destroying E. coli strains implicated in diarrhea. Keywords: Ogi, Omidun, lactic acid bacteria, diarrhoeagenic Escherichia coli strains, Viability.

Antimicrobial Properties of Human Lysozyme Transgenic Mouse Milk

1998 ◽  
Vol 61 (1) ◽  
pp. 52-56 ◽  
Author(s):  
ELIZABETH A. MAGA ◽  
GARY B. ANDERSON ◽  
JAMES S. CULLOR ◽  
WAYNE SMITH ◽  
JAMES D. MURRAY
Keyword(s):  
Staphylococcus Aureus ◽  
Transgenic Mice ◽  
Antimicrobial Properties ◽  
Transgenic Animals ◽  
Average Concentration ◽  
Bacterial Strains ◽  
Human Lysozyme ◽  
Pseudomonas Fragi ◽  
E Coli ◽  
Industry Standard

The antimicrobial properties of standard human lysozyme and the milk of transgenic mice expressing human lysozyme were investigated using bacterial strains important to the dairy industry. Standard human lysozyme was found to be effective at significantly slowing the growth of the milk cold-spoilage organism Pseudomonas fragi (P < 0.001), of a clinical isolate of the mastitis-causing organism Staphylococcus aureus (P < 0.005), and of a nonpathogenic strain of E. coli (P < 0.05). Milk from transgenic mice secreting human lysozyme in their milk at an average concentration of 0.38 mg/ml was found to be bacteriostatic against the cold-spoilage organisms Pseudomonas fragi and Lactobacillus viscous and a mastitis-causing strain of Staphylococcus aureus, but not against a pathogenic strain of E. coli. These results demonstrate that transgenic animals producing human lysozyme in their milk can affect the microbial nature of milk.

scholarly journals Antimicrobial Ionic Liquids with Fumarate Anion

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Biyan He ◽  
Guangnan Ou ◽  
Changyi Zhou ◽  
Meihong Wang ◽  
Suyan Chen
Keyword(s):  
Ionic Liquids ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Research Field ◽  
Potassium Sorbate ◽  
Gravimetric Analysis ◽  
Antimicrobial Drugs ◽  
Active Research

The shortage of new antimicrobial drugs and increasing resistance of microbe to antimicrobial agents have been of some concern. The formulation studies of new antibacterial and antifungal agents have been an active research field. Ionic liquids are known as designed liquids with controllable physical/chemical/biological properties and specific functions, which have been attracting considerable interest over recent years. However, no attention has been made towards the preparation of ionic liquids with antimicrobial activities. In this paper, a new class of ionic liquids (ILs) with fumarate anion was synthesized by neutralization of aqueous 1-butyl-3-methylimidazolium hydroxide with equimolar monoester fumarate and characterized using NMR and thermal gravimetric analysis. The ILs are soluble in water and polar organic solvents and also soluble in the common ILs. The antimicrobial activities of the ILs are more active than commercially available potassium sorbate and are greatly affected by the alkyl chain length. The significant antimicrobial properties observed in this research suggest that the ILs may have potential applications in the modern biotechnology.

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