Serum apolipoprotein A-I potentiates the therapeutic efficacy of lysocin E against Staphylococcus aureus

AbstractLysocin E is a lipopeptide with antibiotic activity against methicillin-resistant Staphylococcus aureus. For unclear reasons, the antibacterial activity of lysocin E in a mouse systemic infection model is higher than expected from in vitro results, and the in vitro activity is enhanced by addition of bovine serum. Here, we confirm that serum from various species, including humans, increases lysocin E antimicrobial activity, and identify apolipoprotein A-I (ApoA-I) as an enhancing factor. ApoA-I increases the antibacterial activity of lysocin E when added in vitro, and the antibiotic displays reduced activity in ApoA-I gene knockout mice. Binding of ApoA-I to lysocin E is enhanced by lipid II, a cell-wall synthesis precursor found in the bacterial membrane. Thus, the antimicrobial activity of lysocin E is potentiated through interactions with host serum proteins and microbial components.

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Serum proteins potentiate therapeutic efficacy of lysocin E against S. aureus

10.21203/rs.3.rs-89037/v1 ◽

2020 ◽

Author(s):

Kazuhisa Sekimizu ◽

Hiroshi Hamamoto ◽

Suresh Panthee ◽

Atmika Paudel ◽

Kenichi Ishii ◽

...

Keyword(s):

Antimicrobial Activity ◽

Therapeutic Efficacy ◽

Serum Proteins ◽

Gene Knockout ◽

Binding Capacity ◽

Resistant Bacteria ◽

Infection Model ◽

Therapeutic Effects ◽

Lipid Ii

Abstract The development of antimicrobials that exert therapeutic efficacy by novel mechanisms is crucial toward combatting multidrug-resistant bacteria. We previously reported a novel antibiotic, lysocin E, that is effective against methicillin-resistant Staphylococcus aureus (MRSA)1. Lysocin E exhibits more prominent therapeutic effects against S. aureus in a mouse systemic infection model compared with its basal antibacterial activity in vitro, but the detailed mechanism underlying this discrepancy was unclear. Here we show that serum or plasma from various species, including humans, increases the antimicrobial activity of lysocin E, and identified apolipoprotein A-I (ApoA-I) as an enhancing factor in the serum. Using gene knockout mice, we further revealed that ApoA-I contributes to the therapeutic effects of lysocin E. The binding capacity of lysocin E to ApoA-I was enhanced by lipid II, an intermediate component of S. aureus cell wall synthesis in the membrane, and ApoA-I enhanced the membrane-damaging activity of lysocin E at a sub-minimum inhibitory concentration (sub-MIC). Our results are the first to demonstrate that antimicrobial activity can be potentiated through interactions of host serum proteins with microbial components to enhance the therapeutic effect, which broadens the strategies for developing antimicrobials by taking advantage of host-microbe interactions.

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Antimicrobial activity of essential oils extracted from leaves of native Moroccan plants against clinical bacterial isolates

The International Arabic Journal of Antimicrobial Agents ◽

10.3823/819 ◽

2018 ◽

Vol 8 (1) ◽

Author(s):

Fatima El Malki ◽

Kamal Eddaraji ◽

Rajae Alloudane ◽

Hassane Greche ◽

Haiat Essalmani ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Pseudomonas Aeruginosa ◽

Antimicrobial Activity ◽

Antibacterial Activity ◽

Essential Oils ◽

Bactericidal Effect ◽

Antimicrobial Activities ◽

Acinetobacter Baumanii ◽

And Staphylococcus Aureus

Introduction: Medicinal plants are plentiful of bioactive molecules effective against multi-resistance bacteria. The aims of this study were to assess the in vitro antimicrobial activities of essential oils extracted from three Moroccan aromatic plants. Methodology: Analysis of essential oils of Origanum compactum, Rosmarinus officinalis and Pelargonium asperum, collected from different localities in Morocco, were performed using a GC-MS spectrophotometry. Antibacterial activity was evaluated in vitro for five clinical multi-resistant isolates. Results: Origanum showed strong antibacterial activity against tested strains except Pseudomonas aeruginosa while Rosmarinum showed a bactericidal effect against Acinetobacter baumanii, Escherichia coli and Staphylococcus aureus. Pelargonium presented only slight growth inhibition of Staphylococcus aureus on solid medium, but provided bactericidal effect against Acinetobacter baumanii and Staphylococcus aureus. Interestingly, fractions F7 and F8 of Pelargonium which represented only 0.3% and 0.1% of the total mass were found bactericidal respectively against Klebsiella pneumoniae and Pseudomonas aeruginosa. Conclusions: Ours results showed that the antimicrobial activities were variables depending on the chemical composition of essential oils, the fraction used and the microorganism tested.Essential oils fractionation allows detection of bioactive substances, especially those owning antimicrobial activity, present in small quantities.

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Protective Effect of Ethanol Extract of Legundi (Vitex trifolia L.) Leaves against Staphylococcus aureus in Drosophila Infection Model

Biointerface Research in Applied Chemistry ◽

10.33263/briac116.1398913996 ◽

2021 ◽

Vol 11 (6) ◽

pp. 13989-13996

Keyword(s):

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Model Organism ◽

Ethanol Extract ◽

Antibacterial Activities ◽

Infection Model ◽

Bacterial Colony ◽

Survival Assay ◽

Colony Forming Assay

Research to discover certain medicinal plants' antibacterial activity against Staphylococcus aureus was mostly performed in vitro. The purpose of this research was to investigate the antibacterial activity of ethanol extract of legundi leaves (EELL) against S. aureus using model organism Drosophila melanogaster. The extract was prepared by the maceration method using 70% ethanol. The antibacterial activities of EELL were determined by using fly survival assay and bacterial colony-forming assay. Fly survival assay was conducted to investigate the extracts' ability to enhance the survival of D. melanogaster (host) upon S. aureus infection. The results demonstrated that both EELL were able to increase the survival rate of the S. aureus-infected Drosophila. Furthermore, a colony-forming assay was carried out to determine the growth of bacteria in the host body that has been considered an important pathogenic factor for the host. The result found that the number of bacteria recovered from the EELL-treated infected flies was significantly lower than the ones obtained from the infected flies without any treatments. Overall, EELL protects the S. aureus-infected hosts, suggesting the potential antibacterial effect of EELL against S. aureus.

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Nigritanine as a New Potential Antimicrobial Alkaloid for the Treatment of Staphylococcus aureus-Induced Infections

Toxins ◽

10.3390/toxins11090511 ◽

2019 ◽

Vol 11 (9) ◽

pp. 511 ◽

Cited By ~ 17

Author(s):

Bruno Casciaro ◽

Andrea Calcaterra ◽

Floriana Cappiello ◽

Mattia Mori ◽

Maria Loffredo ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Antibacterial Activity ◽

Biological Activities ◽

Human Keratinocytes ◽

Chemical Diversity ◽

Bioactive Molecules ◽

Bacterial Strains ◽

Wide Range

Staphylococcus aureus is a major human pathogen causing a wide range of nosocomial infections including pulmonary, urinary, and skin infections. Notably, the emergence of bacterial strains resistant to conventional antibiotics has prompted researchers to find new compounds capable of killing these pathogens. Nature is undoubtedly an invaluable source of bioactive molecules characterized by an ample chemical diversity. They can act as unique platform providing new scaffolds for further chemical modifications in order to obtain compounds with optimized biological activity. A class of natural compounds with a variety of biological activities is represented by alkaloids, important secondary metabolites produced by a large number of organisms including bacteria, fungi, plants, and animals. In this work, starting from the screening of 39 alkaloids retrieved from a unique in-house library, we identified a heterodimer β-carboline alkaloid, nigritanine, with a potent anti-Staphylococcus action. Nigritanine, isolated from Strychnos nigritana, was characterized for its antimicrobial activity against a reference and three clinical isolates of S. aureus. Its potential cytotoxicity was also evaluated at short and long term against mammalian red blood cells and human keratinocytes, respectively. Nigritanine showed a remarkable antimicrobial activity (minimum inhibitory concentration of 128 µM) without being toxic in vitro to both tested cells. The analysis of the antibacterial activity related to the nigritanine scaffold furnished new insights in the structure–activity relationships (SARs) of β-carboline, confirming that dimerization improves its antibacterial activity. Taking into account these interesting results, nigritanine can be considered as a promising candidate for the development of new antimicrobial molecules for the treatment of S. aureus-induced infections.

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EFFICACY EVALUATION OF EXTRACTS OF BRASSICA JUNCEA AND BRASSICA ALBA SEEDS AS POTENTIAL ANTIBACTERIAL AGENT-IN VITRO STUDY, AGAINST PYOGENIC MICROBES - STREPTOCOCCUS PYROGENS, STAPHYLOCOCCUS AUREUS AND E.COLI

November 2020 - International Ayurvedic Medical Journal ◽

10.46607/iamj0409072021 ◽

2021 ◽

Vol 9 (7) ◽

pp. 1344-1348

Author(s):

Seema Nishant Parma ◽

Madhusudan N Pawar ◽

Rehman M. K. ◽

Madhuri Wagh

Keyword(s):

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Antibacterial Activity ◽

Microbial Activity ◽

Brassica Juncea ◽

Broad Spectrum ◽

In Vitro Study ◽

Vitro Study ◽

World Health

The World Health Organization (WHO) reported that about 80% of the world’s population depends primarily on traditional medicine.[1] Ayurveda is the science of life, which aims at building a healthy body with a sound mind. During the past few decades, and in recent Covid-19 Pandaemic situations traditional systems of medicines have become a topic of global importance. The number of emerging multidrug-resistant microbial strains is continuously increasing and has become one of the most serious threats to the successful treatment of infectious diseases. In this study, the antibacterial potentials of the extracts of water, Petroleum ether, methanol & Chloroform of Brassica juncea & Brassica alba seeds were tested against mentioned pyogenic bacteria. Given reports of Brassica species in the treatment of various infections since the Vedic period & Ayurveda, the seed oil had been investigated for its anti-microbial activity by several research workers. Some herbs from Rakshoghna Gana [2] were screened for their in vitro anti-microbial activity on E.Coli and Staphylococcus Aureus. Hence as a part of further research, Brassicajuncea and Brassica alba various extracts and crude oils were evaluated for antibacterial activity against pyogenic bacteria Streptococcus aureus, Staphylococcus aureus and E.Coli by Agar Cup Dilution Technique against standard chemotherapeutic agents, by using 12 antibiotics, sensitivity discs. In vitro study revealed out that crude oil of Brassica juncea and Brassica alba is not potent as standard antimicrobial agents, but water extract and methanol extract possess significant antimicrobial activity in Vitro. Both the extract possesses antimicrobial activity against all 3 pyogenic bacteria and potent as standard 12 antimicrobial drugs. The extracts showed a broad spectrum of antibacterial activity, inhibition zones of bacteria strains ranged from 3-12 mm for Staphylococcus aureus,3-15mm for Streptococcus pyrogens 5-12mm for E. coli. The result of the study supports the immense medicinal properties of Brassica juncea which has revealed a significant scope to develop a novel broad spectrum of antibacterial herbal formulation. Again Brassica alba was found superior in antibacterial action as compared to Brassica juncea as its mention in Ayurved Lexicon Bhavprakash Nighantu,[3,4] results substantiate the same. This is further open for re- search workers to carry out further research work on this project and to see the phagocytic action of the drug, fix the dose of the drug, fractionization of water and methanol extracts by HPTLC separation of active principle as further drug development. Keywords: Brassica juncea, Brassica alba, antibacterials agents, herbal medicine.

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Synthesis and Evaluation of Some New Thiazolidin-4-One Derivatives as Potential Antimicrobial Agents

Journal of Chemistry ◽

10.1155/2013/656271 ◽

2013 ◽

Vol 2013 ◽

pp. 1-6 ◽

Cited By ~ 1

Author(s):

B. A. Baviskar ◽

S. S. Khadabadi ◽

S. L. Deore

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Pseudomonas Aeruginosa ◽

Antimicrobial Activity ◽

Antibacterial Activity ◽

Antimicrobial Agents ◽

Salmonella Typhi ◽

Zone Of Inhibition ◽

Structure Activity

A new series ofN-{4-methyl-5-[4-(4-oxo-2-phenyl(1,3-thiazolidin-3-yl)]-5-sulfanyl(1,2,4-triazol-3-yl)-1,3-thiazol-2-yl }acetamide (7a-l) was synthesized in order to determine their antimicrobial activity and feasible structure–activity relationships. The compounds were synthesized in good yield and the structures of all newly synthesized compounds were established on the basis of their IR,1HNMR, and elemental analysis. The synthesized compounds were testedin vitroantibacterial activity againstStaphylococcus aureus,Escherichia coli,Pseudomonas aeruginosaandSalmonella typhiand antifungal activity againstAspergillus niger,Candida albicansby measuring the zone of inhibition in mm.

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Antibacterial Activity of a Promising Antibacterial Agent: 22-(4-(2-(4-Nitrophenyl-piperazin-1-yl)-acetyl)-piperazin-1-yl)-22-deoxypleuromutilin

Molecules ◽

10.3390/molecules26123502 ◽

2021 ◽

Vol 26 (12) ◽

pp. 3502

Author(s):

Xiang-Yi Zuo ◽

Hong Gao ◽

Mei-Ling Gao ◽

Zhen Jin ◽

You-Zhi Tang

Keyword(s):

Antibacterial Activity ◽

Galleria Mellonella ◽

Systemic Infection ◽

Effect Study ◽

Infection Model ◽

Oral Toxicity ◽

Reference Drug ◽

Antibiotic Effect

A novel pleuromutilin derivative, 22-(4-(2-(4-nitrophenyl-piperazin-1-yl)-acetyl)-piperazin-1-yl)-22-deoxypleuromutilin (NPDM), was synthesized in our laboratory and proved excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA). In this study, more methods were used to further study its preliminary pharmacological effect. The antibacterial efficacy and toxicity of NPDM were evaluated using tiamulin as the reference drug. The in vitro antibacterial activity study showed that NPDM is a potent bactericidal agent against MRSA that induced time-dependent growth inhibition and a concentration-dependent post-antibiotic effect (PAE). Toxicity determination showed that the cytotoxicity of NPDM was slightly higher than that of tiamulin, but the acute oral toxicity study proved that NPDM was a low-toxic compound. In an in vivo antibacterial effect study, NPDM exhibited a better therapeutic effect than tiamulin against MRSA in a mouse thigh infection model as well as a mouse systemic infection model with neutropenia. The 50% effective dose (ED50) of NPDM in a Galleria mellonella infection model was 50.53 mg/kg. The pharmacokinetic properties of NPDM were also measured, which showed that NPDM was a rapid elimination drug in mice.

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Synthesis and Antibacterial Activity of New Azole, Diazole and Triazole Derivatives Based on p-Aminobenzoic Acid

Molecules ◽

10.3390/molecules26092597 ◽

2021 ◽

Vol 26 (9) ◽

pp. 2597

Author(s):

Birutė Sapijanskaitė-Banevič ◽

Vykintas Palskys ◽

Rita Vaickelionienė ◽

Jūratė Šiugždaitė ◽

Povilas Kavaliauskas ◽

...

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Pseudomonas Aeruginosa ◽

Antimicrobial Activity ◽

Antibacterial Activity ◽

Salmonella Enteritidis ◽

Antimicrobial Compounds ◽

Aminobenzoic Acid ◽

Substituted 1

The p-aminobenzoic acid was applied for the synthesis of substituted 1-phenyl-5-oxopyrrolidine derivatives containing benzimidazole, azole, oxadiazole, triazole, dihydrazone, and dithiosemicarbazide moieties in the structure. All the obtained compounds were evaluated for their in vitro antimicrobial activity against Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes, Salmonella enteritidis, Escherichia coli, and Pseudomonas aeruginosa by using MIC and MBC assays. This study showed a good bactericidal activity of γ-amino acid and benzimidazoles derivatives. The antimicrobial activity of the most promising compounds was higher than ampicillin. Furthermore, two benzimidazoles demonstrated good antimicrobial activity against L. monocytogenes (MIC 15.62 µg/mL) that was four times more potent than ampicillin (MIC 65 µg/mL). Further studies are needed to better understand the mechanism of the antimicrobial activity as well as to generate antimicrobial compounds based on the 1-phenyl-5-oxopyrrolidine scaffold.

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Purpurin Esters Containing a Saturated Cyclic Fragment with Antimicrobial Activity

Eurasian Chemico-Technological Journal ◽

10.18321/ectj929 ◽

2020 ◽

Vol 22 (1) ◽

pp. 43 ◽

Cited By ~ 1

Author(s):

Т.V. Kharlamova ◽

R.B. Seidakhmetova ◽

K.D. Praliyev

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Pseudomonas Aeruginosa ◽

Antimicrobial Activity ◽

Antibacterial Activity ◽

Acid Chlorides ◽

Bacillus Subtilis Atcc ◽

Cyclic Fragment ◽

Mic Value

The present study is a continuation of the scientific research works for the synthesis of anthraquinonе-containing derivatives with cyclic ring systems by the interaction of 1,2,4-trihydroxyanthraquinone (purpurin) with cyclic carboxylic acid chlorides. Series of purpurin esters containing a saturated cyclic fragment was studied for antibacterial activity about museum strains of microorganisms. The effects of these preparations in vitro about Staphylococcus aureus ATCC 6538, Bacillus subtilis ATCC 6633, Escherichia coli ATCC 25922, Pseudomonas aeruginosa АТСС 27853 and fungus Сandida albicans АТСС 10231 were studied. It has been found that the compounds with the cyclohexane fragment have possess an antimicrobial activity with strains of microorganisms Staphylococcus aureus АТСС 6538 for which the MIC value was 31.25 μg/ml.

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Chemical Composition and in vitro Antibacterial Activity of the Essential Oil of Verbesina negrensis from the Venezuelan Andes

Natural Product Communications ◽

10.1177/1934578x1501000743 ◽

2015 ◽

Vol 10 (7) ◽

pp. 1934578X1501000 ◽

Cited By ~ 1

Author(s):

Flor D. Mora ◽

Yesenia L. Rojas ◽

Viviana González ◽

Judith Velasco ◽

Tulia Díaz ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Antibacterial Activity ◽

Chemical Composition ◽

Essential Oil ◽

Enterococcus Faecalis ◽

In Vitro Activity ◽

Gram Positive Bacteria ◽

In Vitro Antibacterial Activity

The composition and antimicrobial activity of the essential oil from Verbesina negrensis Steyerm. leaves is reported. Analysis was performed by GC/MS. Major constituents were α-pinene (43.1%), α-humulene (13.8%), δ-cadinene (8.1%), limonene (4.6%) and bicyclogermacrene (4.2%). The essential oil showed in vitro activity against the Gram-positive bacteria Staphylococcus aureus ATCC 25923 and Enterococcus faecalis ATCC 29212 (MIC 500 and 350 μL/mL respectively).

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