scholarly journals Neopeptide Antibiotics That Function as Opsonins and Membrane-Permeabilizing Agents for Gram-Negative Bacteria

2005 ◽  
Vol 49 (8) ◽  
pp. 3122-3128 ◽  
Author(s):  
Haim Tsubery ◽  
Hertzig Yaakov ◽  
Sofia Cohen ◽  
Tal Giterman ◽  
Ariella Matityahou ◽  
...  

ABSTRACT We suggest a novel approach to enhancing antimicrobial drug action by utilizing engineered peptide conjugates. Our most potent conjugates, [fMLF]PMBN and [fMLF]PMEN, are nonapeptides derived from polymyxin B's (PMB's) cyclic moiety (Thr-Dab-cyclo[Dab-Dab-d-Phe-Leu-Dab-Dab-Thr], where Dab is 2,4-diaminobutyric acid) and polymyxin E's (PME's) cyclic moiety (Thr-Dab-cyclo[Dab-Dab-d-Leu-Leu-Dab-Dab-Thr]), respectively, attached to a linear tail comprised of formyl-Met-Leu-Phe (fMLF). The cyclic part binds to gram-negative lipopolysaccharides, rendering the bacterial outer membrane permeable to hydrophobic antibiotics. The tail confers chemotactic and opsonic activities upon the conjugates. These two activities appear to be the basis for the conjugates' antibacterial activities. The conjugates are 8 to 10 times less toxic than the parent PMB or PME antibiotics. Fourteen of 18 mice lethally challenged with erythromycin-resistant Klebsiella pneumoniae survived following intraperitoneal administration of erythromycin and [fMLF]PMBN, whereas erythromycin or the peptide conjugate alone had no effect. Moreover, the clearance of Klebsiella from blood was markedly enhanced by intravenous injection of the [fMLF]PMEN peptide conjugate compared to the clearance of the organism from the mice treated with buffer alone as a control and was similar to that achieved by the PME antibiotic. Blood clearance was also significantly enhanced by administration of PMEN either alone or in a mixture with fMLF, although the effect was less than that produced by the peptide conjugate. Since resistance to polymyxins, the parent molecules of the synthetic cyclic peptides, is rare, the emergence of bacteria resistant to the antimicrobial properties of the peptide conjugates may be precluded as well.

2015 ◽  
Vol 70 (1-2) ◽  
pp. 45-50
Author(s):  
Asu Usta ◽  
Hacer Taşkıran

Abstract N-alkyl substituted 2′,3″-thiazachalcones {3-[(1E)-3-(4-methylthiophene-2-yl)-3-oxoprop-1-en-1-yl]-1-alkyl (C5–12,14) pyridinium bromides} were synthesized by a two-step reaction. The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, elemental analysis and mass spectral studies. The synthesized compounds were tested for antibacterial activities and found to be more active against Gram-positive as compared to Gram-negative bacteria.


2021 ◽  
Author(s):  
Mansour Amin ◽  
Sousan Akrami ◽  
Farkhondeh Haghparasty ◽  
Atiyeh Hakimi

Abstract Background: Today, due to the increasing use of chemical drugs and the spread of microbial resistance to synthetic antibiotics, as well as side effects of drugs, the identification and introduction of plant species with medicinal and antimicrobial properties is very important. In this study, the antimicrobial properties of essential oils and extracts of 6 medicinal plants from Ahvaz region, Iran against 12 Gram-positive and Gram-Negative Bacteria were evaluated. Methods: The EOs and extracts were extracted using water distillation with Clevenger apparatus. The antimicrobial properties and determination of the minimum concentration of growth inhibition of herbals were investigated by the modified E-test method. Results: All analyzed extracts and EOs showed antibacterial effects. The antimicrobial activity of Oliveria decumbens was strongest herbals with the least MIC ranges (0.008-0.1 mg/ml for EO, 0.9-20 mg/ml for extract), while the antibacterial effects of Artemisia vulgaris extract and Glycyrrhiza glabra EO with the highest MIC were weaker than the others. According to the effectiveness of plant extracts on bacteria, Pseudomonas aeruginosa was resistant to all extracts except Oliveria decumbens. In contrast, Bacillus cereus was more sensitive than other strains against analyzed EOs and extracts.Conclusions: It seems that due to the antimicrobial properties of the extracts and essential oils observed in this study, they can be used as an alternative to antimicrobial drugs after more extensive studies.


2019 ◽  
Vol 10 ◽  
pp. 1864-1872
Author(s):  
Prof. Teodora P. Popova

The effect of ionized aqueous solutions (anolytes and catholyte) in the processing of fruits (cherries, morellos, and strawberries) for decontamination has been tested. Freshly prepared analytes and catholyte without the addition of salts were used, as well as stored for 7 months anolytes, prepared with 0.5% NaCl and a combination of 0.5% NaCl and 0.5% Na2CO3. The anolyte prepared with a combination of 0.5% NaCl and 0.5% Na2CO3, as well as the anolyte obtained with 0.5% NaCl, exhibit high antimicrobial activity against the surface microflora of strawberries, cherries, and sour cherries. They inactivate E. coli for 15 minutes. The other species of the fam. Enterobacteriaceae were also affected to the maximum extent, as is the total number of microorganisms, especially in cherries and sour cherries. Even stored for 7 months, they largely retain their antimicrobial properties. Anolyte and catholyte, obtained without the addition of salts, showed a lower effect on the total number of microorganisms, but had a significant effect on Gram-negative bacteria, and especially with regard to the sanitary indicative E. coli.


2006 ◽  
Vol 50 (6) ◽  
pp. 2261-2264 ◽  
Author(s):  
Hee-Soo Park ◽  
Hyun-Joo Kim ◽  
Min-Jung Seol ◽  
Dong-Rack Choi ◽  
Eung-Chil Choi ◽  
...  

ABSTRACT DW-224a showed the most potent in vitro activity among the quinolone compounds tested against clinical isolates of gram-positive bacteria. Against gram-negative bacteria, DW-224a was slightly less active than the other fluoroquinolones. The in vivo activities of DW-224a against gram-positive bacteria were more potent than those of other quinolones.


Chemistry ◽  
2021 ◽  
Vol 3 (4) ◽  
pp. 1271-1285
Author(s):  
Patricia Zimet ◽  
Ruby Valadez ◽  
Sofía Raffaelli ◽  
María Belén Estevez ◽  
Helena Pardo ◽  
...  

Microbial technology offers a green alternative for the synthesis of value-added nanomaterials. In particular, fungal compounds can improve silver nanoparticle production, stabilizing colloidal nanoparticles. Based on a previous study by our group, silver nanoparticles obtained using the extracellular cell-free extracts of Phanerochaete chrysosporium (PchNPs) have shown antimicrobial and antibiofilm activity against Gram-negative bacteria. Moreover, nisin—a bacteriocin widely used as a natural food preservative—has recently gained much attention due its antimicrobial action against Gram-positive bacteria in biomedical applications. Therefore, the aim of this work was to conjugate biogenic silver nanoparticles (PchNPs) with nisin to obtain nanoconjugates (PchNPs@nis) with enhanced antimicrobial properties. Characterization assays were conducted to determine physicochemical properties of PchNPs@nis, and also their antibacterial and antibiofilm activities were studied. The formation of PchNPs@nis was confirmed by UV-Vis, TEM, and Raman spectroscopy analysis. Different PchNPs@nis nanobioconjugates showed diameter values in the range of 60–130 nm by DLS and surface charge values between −20 and −13 mV. Nisin showed an excellent affinity to PchNPs, with binding efficiencies higher than 75%. Stable synthesized PchNPs@nis nanobioconjugates were not only able to inhibit biofilm formation by S. aureus, but also showed inhibition of the planktonic cell growth of Staphyloccocus aureus and Escherichia coli, broadening the spectrum of action of the unconjugated antimicrobials against Gram-positive and Gram-negative bacteria. In conclusion, these results show the promising application of PchNPs@nis, prepared via green technology, as potential antimicrobial nanomaterials.


2011 ◽  
Vol 6 (2) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Sandra M. Bach ◽  
Mario A. Fortuna ◽  
Rodgoun Attarian ◽  
Juliana T. de Trimarco ◽  
César A. N. Catalán ◽  
...  

The antimicrobial and cytotoxic activities of chloroform extracts from the weeds Centaurea tweediei and C. diffusa, and the main sesquiterpene lactones isolated from these species, onopordopicrin and cnicin, respectively, were assayed. Results show that the chloroform extracts from both Centaurea species possess antibacterial activities against a panel of Gram-positive and Gram-negative bacteria. Remarkable antibacterial activity against methicillin-resistant Staphylococcus aureus was also measured. Both the extracts and the purified sesquiterpene lactones show high cytotoxicity against human-derived macrophages. Despite this cytotoxicity, C. diffusa chloroform extract and cnicin are attractive candidates for evaluation as antibiotics in topical preparations against skin-associated pathogens.


2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901
Author(s):  
Cholpisut Tantapakul ◽  
Tawanun Sripisut ◽  
Wisanu Maneerat ◽  
Thunwadee Ritthiwigrom ◽  
Surat Laphookhieo

The first phytochemical investigation of Glycosmis puberula twigs led to the isolation and identification of a new quinolone alkaloid, glycosmispuberulone (1), along with ten known compounds (2–11). The structures were elucidated by spectroscopic analyses and comparison with previously reported data. Their antibacterial activities against Gram-positive and Gram-negative bacteria were also evaluated.


2020 ◽  
Vol 11 (38) ◽  
pp. 10344-10353
Author(s):  
Jiajun Wang ◽  
Jigneshkumar Dahyabhai Prajapati ◽  
Ulrich Kleinekathöfer ◽  
Mathias Winterhalter

Divalent cations alter the translocation of antibiotic molecules through the Gram-negative bacteria outer membrane nanopores.


2005 ◽  
Vol 60 (1-2) ◽  
pp. 30-34 ◽  
Author(s):  
Ali Sonboli ◽  
Fereshteh Eftekhar ◽  
Morteza Yousefzadi ◽  
Mohammad Reza Kanani

The chemical composition of the essential oils obtained from two samples (GP1 and GP2) of Grammosciadium platycarpum Boiss. was analyzed by GC and GC-MS. The analysis of the oils resulted in the identification of twenty-two constituents. Linalool (79.0% - GP1, 81.8% - GP2) and limonene (10.0%, 5.8%) were found to be the major components, respectively. The in vitro antibacterial activities of these oils and their main compounds against seven Gram-positive and Gram-negative bacteria were investigated. The results exhibited that the total oils and their major components possess strong to moderate activities against all the tested bacteria except for Pseudomonas aeruginosa.


1999 ◽  
Vol 45 (9) ◽  
pp. 779-785 ◽  
Author(s):  
Barry Ziola ◽  
Sheryl L Gares ◽  
Brandene Lorrain ◽  
Lori Gee ◽  
W M Ingledew ◽  
...  

Nineteen monoclonal antibodies (Mabs) were isolated based on reactivity with disrupted Pectinatus cerevisiiphilus cells. All of the Mabs reacted with cells from which the outer membrane had been stripped by incubation with sodium dodecyl sulphate, suggesting the peptidoglycan (PG) layer was involved in binding. Mab reactivity with purified PG confirmed this. Epitope mapping revealed the Mabs in total recognize four binding sites on the PG. Mabs specific for each of the four sites also bound strongly to disrupted Pectinatus frisingensis, Selenomonas lacticifix, Zymophilus paucivorans, and Zymophilus raffinosivorans cells, but weakly to disrupted Megasphaera cerevisiae cells. No antibody reactivity was seen with disrupted cells of 11 other species of Gram-negative bacteria. These results confirm that a common PG structure is used by several species of anaerobic Gram-negative beer spoilage bacteria. These results also indicate that PG-specific Mabs can be used to rapidly detect a range of anaerobic Gram-negative beer spoilage bacteria, provided the bacterial outer membrane is first removed to allow antibody binding.Key words: beer spoilage, epitope mapping, monoclonal antibodies, Pectinatus, peptidoglycan.


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