scholarly journals Unraveling the Molecular Mechanism of Selective Antimicrobial Activity of 2(5H)-Furanone Derivative against Staphylococcus aureus

2019 ◽  
Vol 20 (3) ◽  
pp. 694 ◽  
Author(s):  
Irshad Sharafutdinov ◽  
Anna Pavlova ◽  
Farida Akhatova ◽  
Alsu Khabibrakhmanova ◽  
Elvira Rozhina ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Molecular Mechanism ◽  
Rapid Development ◽  
Direct Interaction ◽  
Bacterial Cells ◽  
Cell Integrity ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Life Threatening

Staphylococcus aureus causes various infectious diseases, from skin impetigo to life-threatening bacteremia and sepsis, thus appearing an important target for antimicrobial therapeutics. In turn, the rapid development of antibiotic resistance and biofilm formation makes it extremely robust against treatment. Here, we unravel the molecular mechanism of the antimicrobial activity of the recently unveiled F105 consisting of three pharmacophores: chlorinated 2(5H)-furanone, sulfone, and l-menthol moieties. F105 demonstrates highly selective activity against Gram-positive bacteria and biofilm-embedded S. aureus and exhibits low risk of resistance development. We show explicitly that the fluorescent analogue of F105 rapidly penetrates into Gram-positive bacteria independently of their cell integrity and viability and accumulates there. By contrast, Gram-negative bacteria remain impermeable and, therefore, insusceptible to F105. Apparently, in bacterial cells, F105 induces reactive oxygen species (ROS) formation and nonspecifically interacts with a number of proteins, including ROS-utilizing ones. Using native and 2D PAGE, we confirm that F105 changes the charge of some proteins by either oxidation or direct interaction with them. Therefore, it seems justified to conclude that being simultaneously a ROS inducer and damaging proteins responsible for ROS utilization, F105 impairs the cellular anti-ROS defense representing a prospective ROS-inducing antibacterial agent.

scholarly journals Antimicrobial Biophotonic Treatment of Ampicillin-Resistant Pseudomonas aeruginosa with Hypericin and Ampicillin Cotreatment Followed by Orange Light

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 641 ◽  
Author(s):  
Seemi Tasnim Alam ◽  
Tram Anh Ngoc Le ◽  
Jin-Soo Park ◽  
Hak Cheol Kwon ◽  
Kyungsu Kang
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Cell Wall ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Wall Structures ◽  
Global Issue ◽  
Life Threatening ◽  
Bacteria And Fungi

Bacterial antibiotic resistance is an alarming global issue that requires alternative antimicrobial methods to which there is no resistance. Antimicrobial photodynamic therapy (APDT) is a well-known method to combat this problem for many pathogens, especially Gram-positive bacteria and fungi. Hypericin and orange light APDT efficiently kill Staphylococcus aureus, methicillin-resistant Staphylococcus aureus (MRSA), and the yeast Candida albicans. Although Gram-positive bacteria and many fungi are readily killed with APDT, Gram-negative bacteria are difficult to kill due to their different cell wall structures. Pseudomonas aeruginosa is one of the most important opportunistic, life-threatening Gram-negative pathogens. However, it cannot be killed successfully by hypericin and orange light APDT. P. aeruginosa is ampicillin resistant, but we hypothesized that ampicillin could still damage the cell wall, which can promote photosensitizer uptake into Gram-negative cells. Using hypericin and ampicillin cotreatment followed by orange light, a significant reduction (3.4 log) in P. aeruginosa PAO1 was achieved. P. aeruginosa PAO1 inactivation and gut permeability improvement by APDT were successfully shown in a Caenorhabditis elegans model.

scholarly journals Antibacterial Properties of Propolis

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2047 ◽  
Author(s):  
Izabela Przybyłek ◽  
Tomasz M. Karpiński
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antibacterial Properties ◽  
Bacterial Strains ◽  
Complex Composition ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
The World

Researchers are continuing to discover all the properties of propolis due to its complex composition and associated broad spectrum of activities. This review aims to characterize the latest scientific reports in the field of antibacterial activity of this substance. The results of studies on the influence of propolis on more than 600 bacterial strains were analyzed. The greater activity of propolis against Gram-positive bacteria than Gram-negative was confirmed. Moreover, the antimicrobial activity of propolis from different regions of the world was compared. As a result, high activity of propolis from the Middle East was found in relation to both, Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) strains. Simultaneously, the lowest activity was demonstrated for propolis samples from Germany, Ireland and Korea.

Antimicrobial Activity and Chemical Composition of the Essential Oil of Nepeta crispa Willd. from Iran

2004 ◽  
Vol 59 (9-10) ◽  
pp. 653-656 ◽  
Author(s):  
Ali Sonboli ◽  
Peyman Salehi ◽  
Morteza Yousefzadi
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Essential Oil ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Aerial Parts ◽  
Total Oil ◽  
And Staphylococcus Aureus

Abstract The composition and antimicrobial activity of the essential oil of Nepeta crispa Willd., an endemic species from Iran, was studied. The oil was obtained from the aerial parts of the plant and analyzed by GC and GC/MS. Twenty-three compounds, accounting for 99.8% of the total oil, were identified. The main constituents were 1,8-cineol (47.9%) and 4aα,7α,7aβ- nepetalactone (20.3%). The antimicrobial activity of essential oil of N. crispa was tested against seven gram-negative or gram-positive bacteria and four fungi. The results of the bioassays showed the interesting antimicrobial activity, in which the gram-positive bacteria, Bacillus subtilis and Staphylococcus aureus, were the most sensitive to the oil. Also, the oil exhibited a remarkable antifungal activity against all the tested fungi.

scholarly journals Antimicrobial Activity of Tetrabromobisphenol A (TBBPA) against Staphylococcus aureus Skin Infections

2018 ◽  
Author(s):  
Chang Wang ◽  
Fang Ji ◽  
Fengjie Chen ◽  
Bolei Chen ◽  
Zhen Zhou ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Wound Closure ◽  
Tetrabromobisphenol A ◽  
Gram Positive ◽  
Inflammatory Infiltration ◽  
Gram Positive Bacteria ◽  
Bactericidal Effects ◽  
Selective Antimicrobial Activity

AbstractTetrabromobisphenol A (TBBPA) is a brominated flame retardant with selective antimicrobial activity against Gram-positive bacteria. We show that TBBPA exerts bactericidal effects by damaging the cell wall and membrane of Staphylococcus aureus (SA) without inducing antimicrobial resistance. In vivo skin infection assays indicate that a low dose of TBBPA could contribute to wound closure and attenuate SA infection and inflammatory infiltration. TBBPA has potential for use as an antimicrobial agent against Gram-positive pathogens.

scholarly journals Antimicrobial activity and thiosulfinates profile of a formulation based on Allium cepa L. extract

2017 ◽  
Vol 15 (1) ◽  
pp. 175-181
Author(s):  
O. Orăşan ◽  
R. Oprean ◽  
A. Saplonţai-Pop ◽  
M. Filip ◽  
R. Carpa ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Allium Cepa ◽  
High Performance ◽  
Ultrapure Water ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Liquid Extract ◽  
Allium Cepa L

AbstractBackgroundAllium species extracts including Allium cepa L. contain sulfur compounds, known for their antiplatelet, antimicrobial, antineoplasic activities.MethodologyAntibacterial activity of a formulation based on A. cepa extracts-liquid and lyophilized samples, has been demonstrated using two classes of bacteria: Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) and three methods: discs soaked with liquid extract, the wells method in the culture medium, filled with the liquid extract and lyophilized formulation extracts transformed by the incorporation of ultrapure water. The second part of this study includes identification of thiosulfinates compounds from the studied samples by high performance liquid chromatography - mass spectrometry (HPLC-MS).ResultsThe most important inhibition and the highest antibacterial effficiency were observed against Gram-positive bacteria, such as Staphylococcus aureus. The HPLC-MS thiosulfinates profile of the tested formulation extracts shows the presence of seven thiosulfinate compounds, MeS(O)S 1-propenyl (E,Z); n-PrS(O)S 1-propenyl-(E); n-PrS(O)S 1-propenyl-(Z); trans-zwiebelane; n-PrS(O)CHEtSS-1propenyl; 1-propenylS(O)CHEtSS1-propenyl, which may be responsible for antibacterial activity.ConclusionTesting antimicrobial effects using the three mentioned methods confirmed the antimicrobial activity of the tested samples based on A. cepa extracts, with a demonstrated content of seven thiosulfinate compounds.

scholarly journals Antimicrobial Activity of Novel Furanonaphthoquinone Analogs

1998 ◽  
Vol 42 (3) ◽  
pp. 700-702 ◽  
Author(s):  
Kumiko Nagata ◽  
Kei-Ichi Hirai ◽  
Junko Koyama ◽  
Yasunao Wada ◽  
Toshihide Tamura
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Helicobacter Pylori ◽  
Amphotericin B ◽  
Pathogenic Species ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Gram Positive Bacteria

ABSTRACT Analogs of furanonaphthoquinone (FNQ) from Tecoma ipeMart had MICs ranging from 1.56 to 25 μg/ml against gram-positive bacteria. FNQ showed significantly lower MICs against methicillin-resistant Staphylococcus aureus than against methicillin-sensitive S. aureus. FNQ inhibitedHelicobacter pylori with an MIC of 0.1 μg/ml. Fungi, including pathogenic species, were sensitive to FNQ with MICs similar to those of amphotericin B.

scholarly journals Ruthenium based antimicrobial theranostics – using nanoscopy to identify therapeutic targets and resistance mechanisms in Staphylococcus aureus

2020 ◽  
Vol 11 (1) ◽  
pp. 70-79 ◽  
Author(s):  
Kirsty L. Smitten ◽  
Simon D. Fairbanks ◽  
Craig C. Robertson ◽  
Jorge Bernardino de la Serna ◽  
Simon J. Foster ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Specific Resistance ◽  
Therapeutic Targets ◽  
Resistance Mechanisms ◽  
Wild Type ◽  
Gram Positive ◽  
Gram Positive Bacteria

A detailed study on the uptake and antimicrobial activity of a RuII theranostic complex with wild-type S. aureus, MRSA, and other mutants has identified the specific resistance mechanisms that Gram-positive bacteria display against this lead.

scholarly journals Packed Like Sardines – How Surface Crowdedness Impacts Accessibility to Peptidoglycan of Staphylococcus aureus

2020 ◽  
Author(s):  
Noel J. Ferraro ◽  
Marcos M. Pires
Keyword(s):  
Staphylococcus Aureus ◽  
Bacterial Cell ◽  
Dense Layer ◽  
Bacterial Cells ◽  
Gram Positive ◽  
Teichoic Acids ◽  
Gram Positive Bacteria ◽  
Wide Range ◽  
Small Molecule Therapeutics ◽  
Live Bacterial Cells

AbstractBacterial cell walls are essential barriers that protect bacteria against the onslaught of potentially lethal molecules from the outside. Small molecule therapeutics, proteins from bacterial foes, and host immune proteins must navigate past a dense layer of bacterial biomacromolecules (e.g., capsular proteins, teichoic acids, and anchored proteins) to reach the peptidoglycan (PG) layer of Gram-positive bacteria. A subclass of molecules (e.g., antibiotics with intracellular targets) must also permeate through the PG (in a molecular sieving manner) to reach the cytoplasmic membrane. In the case of Staphylococcus aureus (S. aureus), teichoic acids are the major biopolymers that decorate bacterial cell surfaces. Despite the biological and therapeutic importance of surface accessibility, systematic analyses in live bacterial cells have been lacking. We describe a novel live cell fluorescence assay that reports on the permeability of molecules to and within the PG scaffold. The assay has robust reproducibility, is readily adoptable to any Gram-positive organism, and is compatible with high-throughput sample processing. Analysis of the factors controlling permeability to S. aureus and the methicillin resistant MRSA revealed that molecular flexibility plays a central role in molecular permeability. Moreover, teichoic acids impeded permeability of molecules of a wide range of sizes and chemical composition.

scholarly journals Volatiles and Lipoidal Composition: Antimicrobial Activity of Flowering Aerial Parts of Lavandula pubescens Decne

2017 ◽  
Vol 9 (08) ◽  
Author(s):  
Gouda B. ◽  
Mousa O. ◽  
Salama M. ◽  
Kassem H.
Keyword(s):  
Fatty Acids ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Unsaponifiable Matter ◽  
Volatile Oil ◽  
Gram Positive ◽  
Gram Negative ◽  
Butanol Fraction ◽  
Gram Positive Bacteria ◽  
Aerial Parts

The hydro-distilled volatile oil of the flowering aerial parts of Lavandula pubescens Decne. was analyzed using gas chromatography-mass spectrometry (GC/MS). Twenty eight components were identified representing 87.39% of the total oil. Carvacrol (22.39 %), cis-β-Farnesene (13.25 %) and β-Bisabolene (12.9 %) were the major constituents. Lipoids were detected in the n-hexane extract. Unsaponifiable lipoids (USL) and fatty acids methyl esters (FAME) of the n-hexane extract were analyzed by GC/MS. The percentage of the total identified unsaponifiable matter was 83.51%, while that of fatty acids was 40.83%. 5-Hydroxy1,3,4-trimethoxy-7-methyl-6-propar-naphthalene was the major identified component in the unsaponifiable matter representing 36.64 %, followed by Hentriacontane (8.09 %). Octadecenoic acid was the major fatty acid identified representing 12.72 %.The antimicrobial potential of the methanol extract and its fractions (n-hexane, methylene chloride, ethyl acetate and n-butanol) as well as the hydrodistilled volatile oil were assessed. All the tested samples except the n-butanol fraction exhibited broad spectrum activity against the tested Gram-positive bacteria;Bacillus subtilis, Staphylococcus aureus and Streptococcus faecalisas well as Gram-negative bacteria; Escherichia coli, Pseudomonas aeruginosa and Neisseria gonorrhea. The n-butanol fraction showed antimicrobial activity against all tested Gram-negative and Gram-positive bacteria except Staphylococcus aureus. The growth of Candida albicans and Aspergillus flavus was not affected by any of the tested samples.

scholarly journals Enaminone-Derived Pyrazoles with Antimicrobial Activity

2019 ◽  
Vol 2019 ◽  
pp. 1-10
Author(s):  
Mashooq Ahmad Bhat ◽  
Mohamed A. Al-Omar ◽  
Ahmed M. Naglah ◽  
Abdul Arif Khan
Keyword(s):  
Antimicrobial Activity ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Disc Diffusion ◽  
Initial Screening ◽  
Gram Positive ◽  
Gram Negative ◽  
Disc Diffusion Assay ◽  
Gram Positive Bacteria ◽  
Diffusion Assay

A series of pyrazoles derived from the substituted enaminones were synthesized and were evaluated for antimicrobial activity. All the compounds were characterized by the spectral data and elemental analysis. The synthesized compounds were initially screened for their antimicrobial activity against ATCC 6538, NCTC 10400, NCTC 10418, and ATCC 27853. During initial screening, compounds (P1, P6, and P11) presented significant antimicrobial activity through disc diffusion assay. These compounds were further evaluated for antimicrobial activity at different time points against Gram-positive and Gram-negative bacteria and presented significant activity for 6 hours. The activity was found to be greater against Gram-positive bacteria. In contrast at 24 hours, the activity was found only against Gram-positive bacteria except compound (P11), showing activity against both types of bacteria. Compound (P11) was found to have highest activity against both Gram-positive and Gram-negative bacteria.

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