scholarly journals A Novel Peptide Antibiotic, Pro10-1D, Designed from Insect Defensin Shows Antibacterial and Anti-Inflammatory Activities in Sepsis Models

2020 ◽  
Vol 21 (17) ◽  
pp. 6216
Author(s):  
Manigandan Krishnan ◽  
Joonhyeok Choi ◽  
Ahjin Jang ◽  
Yangmee Kim
Keyword(s):  
Antibacterial Activity ◽  
Bacterial Cell ◽  
Film Formation ◽  
Systemic Infection ◽  
Nuclear Factor Κb ◽  
Peptide Antibiotic ◽  
Gram Negative Bacteria ◽  
Peptide Antibiotics ◽  
Gram Negative ◽  
Cell Selectivity

Owing to the challenges faced by conventional therapeutics, novel peptide antibiotics against multidrug-resistant (MDR) gram-negative bacteria need to be urgently developed. We had previously designed Pro9-3 and Pro9-3D from the defensin of beetle Protaetia brevitarsis; they showed high antimicrobial activity with cytotoxicity. Here, we aimed to develop peptide antibiotics with bacterial cell selectivity and potent antibacterial activity against gram-negative bacteria. We designed 10-meric peptides with increased cationicity by adding Arg to the N-terminus of Pro9-3 (Pro10-1) and its D-enantiomeric alteration (Pro10-1D). Among all tested peptides, the newly designed Pro10-1D showed the strongest antibacterial activity against Escherichia coli, Acinetobacter baumannii, and MDR strains with resistance against protease digestion. Pro10-1D can act as a novel potent peptide antibiotic owing to its outstanding inhibitory activities against bacterial film formation with high bacterial cell selectivity. Dye leakage and scanning electron microscopy revealed that Pro10-1D targets the bacterial membrane. Pro10-1D inhibited inflammation via Toll Like Receptor 4 (TLR4)/Nuclear factor-κB (NF-κB) signaling pathways in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Furthermore, Pro10-1D ameliorated multiple-organ damage and attenuated systemic infection-associated inflammation in an E. coli K1-induced sepsis mouse model. Overall, our results suggest that Pro10-1D can potentially serve as a novel peptide antibiotic for the treatment of gram-negative sepsis.

scholarly journals Identification of a Novel Cathelicidin from the Deinagkistrodon acutus Genome with Antibacterial Activity by Multiple Mechanisms

Toxins ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 771
Author(s):  
Lipeng Zhong ◽  
Jiye Liu ◽  
Shiyu Teng ◽  
Zhixiong Xie
Keyword(s):  
Electron Microscopy ◽  
Antibacterial Activity ◽  
Bacterial Cell ◽  
Resistant Bacteria ◽  
Bacterial Invasion ◽  
Gram Negative Bacteria ◽  
Cell Integrity ◽  
Gram Positive ◽  
Destructive Effect ◽  
Gram Negative

The abuse of antibiotics and the consequent increase of drug-resistant bacteria constitute a serious threat to human health, and new antibiotics are urgently needed. Research shows that antimicrobial peptides produced by natural organisms are potential substitutes for antibiotics. Based on Deinagkistrodonacutus (known as five-pacer viper) genome bioinformatics analysis, we discovered a new cathelicidin antibacterial peptide which was called FP-CATH. Circular dichromatic analysis showed a typical helical structure. FP-CATH showed broad-spectrum antibacterial activity. It has antibacterial activity to Gram-negative bacteria and Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA). The results of transmission electron microscopy (TEM) and scanning electron microscopy (SEM) showed that FP-CATH could cause the change of bacterial cell integrity, having a destructive effect on Gram-negative bacteria and inducing Gram-positive bacterial surface formation of vesicular structure. FP-CATH could bind to LPS and showed strong binding ability to bacterial DNA. In vivo, FP-CATH can improve the survival rate of nematodes in bacterial invasion experiments, and has a certain protective effect on nematodes. To sum up, FP-CATH is likely to play a role in multiple mechanisms of antibacterial action by impacting bacterial cell integrity and binding to bacterial biomolecules. It is hoped that the study of FP-CATH antibacterial mechanisms will prove useful for development of novel antibiotics.

In-vitro Antioxidant and Antibacterial Activity of Methanolic Extract of Shorea robusta Gaertn. F. Resin

2016 ◽  
Vol 6 (4) ◽  
pp. 68
Author(s):  
Sushma Vashisht ◽  
Manish Pal Singh ◽  
Viney Chawla
Keyword(s):  
Antibacterial Activity ◽  
Methanolic Extract ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Disc Diffusion ◽  
Gram Positive ◽  
Gram Negative ◽  
Shorea Robusta ◽  
Dose Dependent ◽  
Resin Extract

The methanolic extract of the resin of Shorea robusta was subjected to investigate its antioxidant and antibacterial properties its utility in free radical mediated diseases including diabetic, cardiovascular, cancer etc. The methanol extract of the resin was tested for antioxidant activity using scavenging activity of DPPH (1,1-diphenyl-2-picrylhydrazil) radical method, reducing power by FeCl3 and antibacterial activity against gram positive and gram negative bacteria using disc diffusion method. The phytochemical screening considered the presence of triterpenoids, tannins and flavoniods. Overall, the plant extract is a source of natural antioxidants which might be helpful in preventing the progress of various oxidative stress mediated diseases including aging. The half inhibition concentration (IC50) of resin extract of Shorea robusta and ascorbic acid were 35.60 µg/ml and 31.91 µg/ml respectively. The resin extract exhibit a significant dose dependent inhibition of DPPH activity. Antibacterial activity was observed against gram positive and gram negative bacteria in dose dependent manner.Key Words: Shorea robusta, antioxidant, antibacterial, Disc-diffusion, DPPH.

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.

Structure-Activity Relationship and Antimicrobial Evaluation of N-Phenylpyrazole Curcumin Derivatives

2020 ◽  
Vol 16 (4) ◽  
pp. 481-488
Author(s):  
Heli Sanghvi ◽  
Satyendra Mishra
Keyword(s):  
Antibacterial Activity ◽  
Gram Negative Bacteria ◽  
Pyrazole Derivatives ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Curcumin Derivatives ◽  
Structure Activity ◽  
Electron Donating Groups ◽  
Derivatives Of

Background: Curcumin, one of the most important pharmacologically significant natural products, has gained significant consideration among scientists for decades since its multipharmacological activities. 1, 3-Dicarbonyl moiety of curcumin was found to be accountable for the rapid degradation of curcumin molecule. The aim of present work is to replace 1, 3-dicarbonyl moiety of curcumin by pyrazole and phenylpyrazole derivatives with a view to improving its stability and to investigate the role of substitution in N-phenylpyrazole curcumin on its antibacterial activity against both Gram-positive as well as Gram-negative bacteria. Methods: Pyrazole derivatives of curcumin were prepared by heating curcumin with phenyhydrazine/ substituted phenyhydrazine derivatives in AcOH. The residue was purified by silica gel column chromatography. Structures of purified compounds were confirmed by 1H NMR and Mass spectroscopy. The synthesized compounds were evaluated for their antibacterial activity by the microdilution broth susceptibility test method against gram positive (S. aureus) and gram negative (E. coli). Results: Effects of substitution in N-phenylpyrazole curcumin derivatives against S. aureus and E. coli were studied. The most active N-(3-Nitrophenylpyrazole) curcumin (12) exhibits twenty-fold more potency against S. aureus (MIC: 10μg/mL)) and N-(2-Fluoroophenylpyrazole) curcumin (5) fivefold more potency against E. coli (MIC; 50 μg/mL) than N-phenylpyrazole curcumin (4). Whereas, a remarkable decline in anti-bacterial activity against S. aureus and E. coli was observed when electron donating groups were incorporated in N-phenylpyrazole curcumin (4). Comparative studies of synthesized compounds suggest the effects of electron withdrawing and electron donating groups on unsubstituted phenylpyrazole curcumin (4). Conclusion: The structure-activity relationship (SAR) results indicated that the electron withdrawing and electron donating at N-phenylpyrazole curcumin played key roles for their bacterial inhibitory effects. The results of the antibacterial evaluation showed that the synthesized pyrazole derivatives of curcumin displayed moderate to very high activity in S. aureus. In conclusion, the series of novel curcumin derivatives were designed, synthesized and tested for their antibacterial activities against S. aureus and E. coli. Among them, N-(3-Nitrophenylpyrazole curcumin; 12) was most active against S. aureus (Gram-positive) and N-(2-Fluoroophenylpyrazole) curcumin (5) against E. coli (Gram-negative) bacteria.

Light mediated, switchable, antibacterial activity of cerium dioxide nanoparticles on gram positive and gram negative bacteria

2020 ◽  
Author(s):  
Rekhachandran Prasanna Ramachandran ◽  
Archana Valliyamma ◽  
Nitha Nellithanathu Thomas ◽  
Mangalaraja Ramalinga Viswanathan ◽  
Boby Theophilofe Edwin ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cerium Dioxide ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative

scholarly journals Proteomic response of Escherichia coli to a membrane lytic and iron chelating truncated Amaranthus tricolor defensin

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Tessa B. Moyer ◽  
Ashleigh L. Purvis ◽  
Andrew J. Wommack ◽  
Leslie M. Hicks
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Antimicrobial Peptides ◽  
Mechanism Of Action ◽  
Gram Negative Bacteria ◽  
Amaranthus Tricolor ◽  
Core Motif ◽  
Gram Negative ◽  
E Coli ◽  
Membrane Lysis

Abstract Background Plant defensins are a broadly distributed family of antimicrobial peptides which have been primarily studied for agriculturally relevant antifungal activity. Recent studies have probed defensins against Gram-negative bacteria revealing evidence for multiple mechanisms of action including membrane lysis and ribosomal inhibition. Herein, a truncated synthetic analog containing the γ-core motif of Amaranthus tricolor DEF2 (Atr-DEF2) reveals Gram-negative antibacterial activity and its mechanism of action is probed via proteomics, outer membrane permeability studies, and iron reduction/chelation assays. Results Atr-DEF2(G39-C54) demonstrated activity against two Gram-negative human bacterial pathogens, Escherichia coli and Klebsiella pneumoniae. Quantitative proteomics revealed changes in the E. coli proteome in response to treatment of sub-lethal concentrations of the truncated defensin, including bacterial outer membrane (OM) and iron acquisition/processing related proteins. Modification of OM charge is a common response of Gram-negative bacteria to membrane lytic antimicrobial peptides (AMPs) to reduce electrostatic interactions, and this mechanism of action was confirmed for Atr-DEF2(G39-C54) via an N-phenylnaphthalen-1-amine uptake assay. Additionally, in vitro assays confirmed the capacity of Atr-DEF2(G39-C54) to reduce Fe3+ and chelate Fe2+ at cell culture relevant concentrations, thus limiting the availability of essential enzymatic cofactors. Conclusions This study highlights the utility of plant defensin γ-core motif synthetic analogs for characterization of novel defensin activity. Proteomic changes in E. coli after treatment with Atr-DEF2(G39-C54) supported the hypothesis that membrane lysis is an important component of γ-core motif mediated antibacterial activity but also emphasized that other properties, such as metal sequestration, may contribute to a multifaceted mechanism of action.

Two structurally diverse Zn-based coordination polymers with excellent antibacterial activity

CrystEngComm ◽  
2018 ◽  
Vol 20 (24) ◽  
pp. 3353-3362 ◽  
Author(s):  
Ian R. Colinas ◽  
Mauricio D. Rojas-Andrade ◽  
Indranil Chakraborty ◽  
Scott R. J. Oliver
Keyword(s):  
Antibacterial Activity ◽  
Structural Properties ◽  
Coordination Polymers ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative

Two novel Zn-based coordination polymers with unique structural properties display an exceptional antibacterial activity against Gram-positive and Gram-negative bacteria.

Carbon–carbon-linked (pyrazolylphenyl)oxazolidinones with antibacterial activity against multiple drug resistant gram-positive and fastidious gram-negative bacteria

2001 ◽  
Vol 9 (12) ◽  
pp. 3243-3253 ◽  
Author(s):  
Chi Sing Lee ◽  
Debra A Allwine ◽  
Michael R Barbachyn ◽  
Kevin C Grega ◽  
Lester A Dolak ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Multiple Drug ◽  
Gram Negative Bacteria ◽  
Drug Resistant ◽  
Gram Positive ◽  
Gram Negative ◽  
Multiple Drug Resistant
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