scholarly journals PAMAM-dendrimer Enhanced Antibacterial Effect of Vancomycin Hydrochloride Against Gram-Negative Bacteria

2018 ◽  
Vol 22 ◽  
pp. 10-21 ◽  
Author(s):  
Azadeh Serri ◽  
Arash Mahboubi ◽  
Afshin Zarghi ◽  
Hamid Reza Moghimi
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Concentration ◽  
In Vitro Release ◽  
Pamam Dendrimers ◽  
Dilution Method ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Bacterial Membranes ◽  
Gram Positive Bacteria

Purpose: The antibacterial activity of some antibiotics is specific to either Gram-positive or Gram-negative bacteria.  There are different mechanisms behind such insensitivities like inability of antibiotics to permeate through some bacterial membranes, as is the case for vancomycin in Gram-negative bacteria. The present investigation tries to overcome this problem by dendrimers, in order to make Gram-negative bacteria responsive to vancomycin. Methods: The effects of generations 3 (G3) and 5 (G5) polyamidoamine amine-terminated dendrimers (NH2-PAMAM), on the antibacterial activity of vancomycin, were evaluated. Vancomycin-PAMAM dendrimers complexes were prepared and their antibacterial activities were evaluated by determination of their “minimum inhibitory concentration (MIC)”, “minimum bactericidal concentration” and “fractional inhibitory concentration index” values against two Gram-positive and four Gram-negative bacteria, using broth micro-dilution method. The complexation of vancomycin and dendrimers was also assessed by in vitro release studies across dialysis tubing using a developed HPLC method. Results: Results showed that vancomycin solution was effective against Gram-positive bacteria, but, was not effective in Gram-negative ones. Vancomycin-PAMAM dendrimers exhibited significant antibacterial efficacy against Gram-negative bacteria resulting in a decline of vancomycin MIC values by about 2, 2, 4 and 64 times in E. coli, K. pneumonia, S. typhimurium and P. aeruginosa, respectively. Results also showed that enhanced effect by G5 is more than G3. Dendrimers did not affect antibacterial activity of vancomycin in Gram-positive bacteria, as no permeation problem exists here. Conclusions: The present study revealed that both G3 and G5 cationic PAMAM dendrimers are able to make Gram-negative bacteria sensitive to vancomycin, resulting in decline of MIC values up to 64 times, possibly by increasing its permeation through bacterial membrane. These results look promising for broadening the antibacterial spectrum of vancomycin and such a strategy might be used for increasing the overall life of antibiotics.

SYNTHESIS OF PIPERINE - PIPERAZINE ANALOGUES AND THEIR ANTIBACTERIAL ACTIVITY

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (06) ◽  
pp. 30-35
Author(s):  
Naveen K. Kottakki ◽  
◽  
Amperayani K. Rao ◽  
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Concentration ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Aromatic Nitro ◽  
Heterocyclic Moiety ◽  
Agar Well Diffusion Method

In the current study, a series of piperine – piperazine analogues (5a to 5f) were designed and synthesized. The piperine was isolated from pepper and used for the conjugation with heterocyclic moiety for better biological activity. The piperazine heterocyclic was chosen for conjugation with piperine. The newly synthesized structures were determined by IR, 1H NMR and 13C NMR spectral data. The compounds were examined for their anti‐microbial activity against gram-positive (Bacillus subtilis) and gram-negative (Vibrio cholerae) bacteria using the agar well diffusion method. The newly synthesized compounds exhibited capable activities against V. cholerae and B. subtilis and it showed minimum inhibitory concentration. Among all the synthesized compounds, 5f has the highest activity (26 mm) against gram-positive bacteria and (29mm) against gram-negative bacteria. The remaining compounds showed appreciable antibacterial activity. The enhanced activity of the synthesized compounds may be due to the presence of conjugated amide linkage with the natural product piperine and piperazine heterocyclic molecule. The substituents present on the aromatic (nitro-substituted) ring also influenced the activity of the compound.

Distinct antibacterial activity of a vertically aligned graphene coating against Gram-positive and Gram-negative bacteria

2020 ◽  
Vol 8 (28) ◽  
pp. 6069-6079
Author(s):  
Wei Wei ◽  
Jiurong Li ◽  
Zeyang Liu ◽  
Yuan Deng ◽  
Da Chen ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Gram Negative Bacteria ◽  
Antibacterial Mechanism ◽  
Si Substrate ◽  
Gram Positive ◽  
Gram Negative ◽  
Bacterial Membranes ◽  
Gram Positive Bacteria ◽  
Graphene Coating ◽  
Vertically Aligned

The distinct antibacterial mechanism of vertical graphene Si toward bacteria. Vertical graphene kills Gram-positive bacteria through physical disruption and Si substrate kills Gram-negative bacteria by extracting electrons from bacterial membranes.

Antibacterial activity of magnesium oxide nanoparticles prepared by Calcination method

2019 ◽  
Vol 10 (03) ◽  
Author(s):  
Elaf Ayad Kadhem ◽  
Miaad Hamzah Zghair ◽  
Sarah , Hussam H. Tizkam, Shoeb Alahmad Salih Mahdi ◽  
Hussam H. Tizkam ◽  
Shoeb Alahmad
Keyword(s):  
Antibacterial Activity ◽  
Magnesium Oxide ◽  
Diffusion Method ◽  
Oxide Nanoparticles ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Magnesium Oxide Nanoparticles ◽  
Agar Disc

magnesium oxide nanoparticles (MgO NPs) were prepared by simple wet chemical method using different calcination temperatures. The prepared NPs were characterized by Electrostatic Discharge (ESD), Scanning Electron Microscope (SEM) and X-ray Diffraction (XRD). It demonstrates sharp intensive peak with the increase of crystallinty and increase of the size with varying morphologies with respect to increase of calcination temperature. Antibacterial studies were done on gram negative bacteria (E.coli) and gram positive bacteria (S.aureus) by agar disc diffusion method. The zones of inhibitions were found larger for gram positive bacteria than gram negative bacteria, this mean, antibacterial MgO NPs activity more active on gram positive bacteria than gram negative bacteria because of the structural differences. It was found that antibacterial activity of MgO NPs was found it has directly proportional with their concentration.

scholarly journals Antibacterial Activity of Macrocyclic Complexes of Cu(II), Ni(II) and VO(II) Derived fromo-Aminobenzaldehyde

2012 ◽  
Vol 9 (1) ◽  
pp. 481-486
Author(s):  
K. Anuradha ◽  
R. Rajavel
Keyword(s):  
Antibacterial Activity ◽  
Elemental Analysis ◽  
Molar Conductance ◽  
Macrocyclic Complexes ◽  
Spectral Studies ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria

Novel Cu(II),Ni(II) and VO(II) complexes are synthesized with N1,N4-bis(2-aminobenzylidene)benzene-1,4-diamine (L). Complexes were characterized by elemental analysis, molar conductance, IR, UV and EPR. Spectral studies reveals a square planner geomentry for Cu(II), Ni(II) complexes and square pyramidal for VO(II) complex. The ligand and its complexes were also evaluated against the growth of gram positive bacteria and gram negative bacteria.

scholarly journals Chemical Composition and Antibacterial Activity of the Essential Oil of Espeletia nana

2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Alexis Peña ◽  
Luis Rojas ◽  
Rosa Aparicio ◽  
Libia Alarcón ◽  
José Gregorio Baptista ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Disk Diffusion Method ◽  
Gram Negative ◽  
Gram Positive Bacteria

The essential oil of the leaves of Espeletia nana Cuatrec, obtained by hydrodistillation, was analyzed by GC-MS, which allowed the identification of 24 components, which made up 99.9% of the oil. The most abundant compounds were α-pinene (38.1%), β-pinene (17.2%), myrcene (15.0%), spathulenol (4.2%), bicyclogermacrene (4.0%), α-zingiberene (4.0%), and γhimachalene (3.7%). Antibacterial activity was tested against Gram-positive and Gram-negative bacteria using the agar disk diffusion method. Activity was observed only against Gram-positive bacteria. MIC values were determined for Staphylococcus aureus ATCC 25923(200 μg/mL) and Enterococcus faecalis ATCC 29212 (600 μg/mL).

scholarly journals Water-dispersible glycosylated poly(2,5′-thienylene)porphyrin-based nanoparticles for antibacterial photodynamic therapy

2019 ◽  
Vol 18 (5) ◽  
pp. 1147-1155 ◽  
Author(s):  
Rehan Khan ◽  
Melis Özkan ◽  
Aisan Khaligh ◽  
Dönüs Tuncel
Keyword(s):  
Antibacterial Activity ◽  
Photodynamic Therapy ◽  
Singlet Oxygen ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Water Dispersible ◽  
Gram Positive Bacteria ◽  
High Yields

Water-dispersible glycosylated poly(2,5′-thienylene)porphyrin-based nanoparticles have the ability to generate singlet oxygen in high yields and exhibit light-triggered antibacterial activity against Gram negative bacteria, E. coli as well as Gram positive bacteria, B. subtilis.

scholarly journals Synthesis and Antibacterial Activity of Chalcones and Pyrimidine-2-ones

2005 ◽  
Vol 2 (2) ◽  
pp. 109-112
Author(s):  
A. K. Parekh ◽  
K. K. Desai
Keyword(s):  
Antibacterial Activity ◽  
Spectral Data ◽  
Elemental Analysis ◽  
Aromatic Aldehydes ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
H Nmr

Some new chalcones have been prepared by Claisen-schmidt condensation of ketone and different aromatic aldehydes. These chalcones on condensation with urea in presence of acid gave Pyrimidine-2-ones. The synthesized compounds have been characterized by elemental analysis, IR and1H NMR spectral data. They have been screened for their antibacterial activity against Gram positive bacteria B. subtillis & S. aureus and Gram negative bacteria E. coli & S. typhi.

Combination Therapy for Bacterial Pathogens: Naturally Derived Antimicrobial Drugs Augmented with Ulva lactuca Extract

2021 ◽  
Vol 21 ◽  
Author(s):  
Nilushi Indika Bamunuarachchi ◽  
Fazlurrahman Khan ◽  
Young-Mog Kim
Keyword(s):  
Antibacterial Activity ◽  
Pathogenic Bacteria ◽  
Inhibitory Concentration ◽  
Bacterial Pathogens ◽  
Dilution Method ◽  
Gram Positive ◽  
Antimicrobial Drugs ◽  
Gram Negative ◽  
Hexane Extracts ◽  
Conventional Antibiotics

Background: With the growing incidence of microbial pathogenesis, several alternative strategies have been developed. The number of treatments using naturally (e.g., plants, algae, fungi, bacteria, and animals) derived compounds has increased. Importantly, marine-derived products have become a promising and effective approach to combat the antibiotic resistance properties developed by bacterial pathogens. Furthermore, augmenting the sub-inhibitory concentration of the naturally-derived antimicrobial compounds (e.g., hydroxycinnamic acids, terpenes, marine-derived polysaccharides, phenolic compounds) into the naturally derived extracts as a combination therapy to treat the bacterial infection has not been well studied. Objective: The present study was aimed to prepare green algae Ulva lactuca extract and evaluate its antibacterial activity towards Gram-positive and Gram-negative human pathogenic bacteria. Also, revitalize the antibacterial efficiency of the naturally-derived antimicrobial drugs and conventional antibiotics by augmenting their sub-MIC to the U. lactuca extracts. Methods: Extraction was done using a different organic solvent, and its antibacterial activity was tested towards Gram-positive and Gram-negative pathogens. The minimum inhibitory concentration (MIC) of U. lactuca extracts has been determined towards pathogenic bacteria using the micro broth dilution method. The viable cell counting method was used to determine the minimum bactericidal concentration (MBC). The fractional inhibitory concentration (FIC) assay was utilized to examine the combinatorial impact of sub-MIC of two antibacterial drugs using the micro broth dilution method. The chemical components of the extract were analyzed by GC-MS analysis. Results: Among all the extracts, n-hexane extract was found to show effective antibacterial activity towards tested pathogens with the lowest MIC and MBC value. Furthermore, the n-hexane extracts have also been used to enhance the efficacy of the naturally-derived (derived from plants and marine organisms) compounds and conventional antibiotics at their sub-inhibitory concentrations. Most of the tested antibiotics and natural drugs at their sub-MIC were found to exhibit synergistic and additive antibacterial activity towards the tested bacterial pathogens. Conclusions: The augmenting of U. lactuca n-hexane extracts resulted in synergistic and additive bactericidal effects on Gram-positive and Gram-negative human pathogenic bacteria. The present study shows a new alternative strategy to revitalize the antimicrobial activity of naturally derived compounds for treating human bacterial pathogens.

scholarly journals Densely Functionalized 2-methylideneazetidines: Evaluation as Antibacterials

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3891
Author(s):  
Giovanni Petrillo ◽  
Cinzia Tavani ◽  
Lara Bianchi ◽  
Alice Benzi ◽  
Maria Maddalena Cavalluzzi ◽  
...  
Keyword(s):  
Antibacterial Agents ◽  
Inhibitory Concentration ◽  
General Procedure ◽  
Eukaryotic Cells ◽  
Gram Negative Bacteria ◽  
Pharmacological Profile ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Structure Activity

Twenty-two novel, variously substituted nitroazetidines were designed as both sulfonamide and urethane vinylogs possibly endowed with antimicrobial activity. The compounds under study were obtained following a general procedure recently developed, starting from 4-nitropentadienoates deriving from a common β-nitrothiophenic precursor. While being devoid of any activity against fungi and Gram-negative bacteria, most of the title compounds performed as potent antibacterial agents on Gram-positive bacteria (E. faecalis and three strains of S. aureus), with the most potent congener being the 1-(4-chlorobenzyl)-3-nitro-4-(p-tolyl)azetidine 22, which displayed potency close to that of norfloxacin, the reference antibiotic (minimum inhibitory concentration values 4 and 1–2 μg/mL, respectively). Since 22 combines a relatively efficient activity against Gram-positive bacteria and a cytotoxicity on eucharyotic cells only at 4-times higher concentrations (inhibiting concentration on 50% of the cultured eukaryotic cells: 36 ± 10 μM, MIC: 8.6 μM), it may be considered as a promising hit compound for the development of a new series of antibacterials selectively active on Gram-positive pathogens. The relatively concise synthetic route described herein, based on widely available starting materials, could feed further structure–activity relationship studies, thus allowing for the fine investigation and optimization of the toxico-pharmacological profile.

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