The antibacterial activity of 1,2,3-triazole- and 1,2,4-triazole-containing hybrids against Staphylococcus aureus: An updated review (2020-present)

2021 ◽  
Vol 21 ◽  
Author(s):  
Jie Li ◽  
Junwei Zhang
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Broad Spectrum ◽  
Bacterial Infections ◽  
Bacterial Pathogen ◽  
Temperature Sensitive ◽  
Protein Z ◽  
Topoisomerase Iv ◽  
Antibiotic Resistant ◽  
Clinically Significant

: Staphylococcus aureus (S. aureus), a prominent, highly contagious nosocomial and community-acquired bacterial pathogen, can cause a broad spectrum of diseases. Antibiotic-resistant S. aureus strains, which pose potential causes of morbidity and mortality, have continuously emerged in recent years, calling for novel anti-S. aureus agents. 1,2,3-Triazole and 1,2,4-triazole, the bioisostere of amides, esters, and carboxylic acids, are potent inhibitors of DNA gyrase, topoisomerase IV, efflux pumps, filamentous temperature-sensitive protein Z, and penicillin-binding protein. In particular, 1,2,3-triazole- and 1,2,4-triazole-containing hybrids have the potential to exert dual or multiple antibacterial mechanisms of action. Moreover, 1,2,3-triazole-cephalosporin hybrid cefatrizine, 1,2,3-triazole-oxazolidinone hybrid radezolid, and 1,2,4-triazolo[1,5-a]pyrimidine hybrid essramycin, have already been used in clinical practice to treat bacterial infections. Hence, 1,2,3-triazole- and 1,2,4-triazole-containing hybrids possess promising broad-spectrum antibacterial activity against diverse clinically significant organisms, including drug-resistant forms. This review is an update on the latest development of 1,2,3-triazole- and 1,2,4-triazole-containing hybrids with anti-S. aureus activity, covering articles published between January 2020 and July 2021.

scholarly journals MODERN APPROACHES TO ANTIVIRULENT THERAPY OF DISEASES ASSOCIATED WITH STAPHYLOCOCCUS AUREUS

2019 ◽  
Vol 23 (3-4) ◽  
pp. 26-31
Author(s):  
T.O. Kryuchko ◽  
O.Ya. Tkachenko ◽  
N.V. Kuzmenko ◽  
I.N. Nesina ◽  
S.M. Tanianska ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Virulence Factors ◽  
Bacterial Infections ◽  
Effective Means ◽  
Bacterial Pathogen ◽  
Cross Reactivity ◽  
Main Function ◽  
Virulence Proteins ◽  
New Antibiotics ◽  
Active Research

Staphylococcus aureus is a universal bacterial pathogen, which is able to develop the resistance to new antibiotics, by means of virulence factors, whose main function is the spread of diseases by inhibiting the immune factors of host defense. Its wide spread at in-patient departments and also the presence of clinical probationary wards Staphylococcus aureus, resistant to methicillin at out-patient departments, deprive the doctors of effective means for control of the infection. Complications caused by MRSA lead to hospitalization and indices of lethality. The aim of the paper is to analyze the main factors of S. аureus virulence and ways the of its interaction as a result of etiological and pathogenetic treatment. Complexity of treatment of bacterial infections is determined by alternative ways of prevention and treatment of diseases to which bacteria are not able to develop resistance. Along with general mechanisms that form antibiotic resistance, S. aureus produces many individual virulence factors that model the immune response, affecting the survival of the microorganism. The virulence factors produced by S. aureus are diverse and have the ability not only to cause cell lysis, but also to stimulate tissue rejection and destruction. It is important to determine that many specific factors of virulence caused by S. aureus, have ability to change both congenital and adaptive immune reactions including inhibition of complement activation, neutrophils neutralization, phagocytes inhibition. Strategies for inhibiting virulence factors can range from using small inhibitor molecules or full-fledged antibodies to creating toxoids and virulence proteins. Great interest is focused upon those inhibitors that have cross-reactivity with respect to multiple virulence factors, as well as inhibitors, the main target of which is a global regulator with multi-purpose activity, for example, agr operon. Active research into the specific alternative antivirulent treatments for severe diseases caused by S. aureus can potentially settle a number of problems and difficulties of post-antibiotic era.

scholarly journals Antibacterial activity of Taxodium ascendens Diterpenes against Methicillin-resistant Staphylococcus aureus

2014 ◽  
Vol 9 (8) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Courtney M. Starks ◽  
Vanessa L. Norman ◽  
Russell B. Williams ◽  
Matt G. Goering ◽  
Stephanie M. Rice ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacterial Infections ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Clinical Isolates ◽  
Drug Resistant ◽  
Methicillin Resistant

One new and seven known diterpenes were identified from an antibacterial chromatographic fraction of Taxodium ascendens. Of these, demethylcryptojaponol (2), 6-hydroxysalvinolone (3), hydroxyferruginol (4), and hinokiol (5) demonstrated potent activity against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA). These compounds represent a class of synthetically accessible compounds that could be further developed for treatment of drug-resistant bacterial infections.

scholarly journals In Vitro Evaluation of CBR-2092, a Novel Rifamycin-Quinolone Hybrid Antibiotic: Studies of the Mode of Action in Staphylococcus aureus

2008 ◽  
Vol 52 (7) ◽  
pp. 2313-2323 ◽  
Author(s):  
Gregory T. Robertson ◽  
Eric J. Bonventre ◽  
Timothy B. Doyle ◽  
Qun Du ◽  
Leonard Duncan ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Rna Polymerase ◽  
Mode Of Action ◽  
Bacterial Infections ◽  
Dna Gyrase ◽  
Topoisomerase Iv ◽  
Dna Topoisomerase ◽  
Resistant Variant ◽  
Proven Efficacy

ABSTRACT Rifamycins have proven efficacy in the treatment of persistent bacterial infections. However, the frequency with which bacteria develop resistance to rifamycin agents restricts their clinical use to antibiotic combination regimens. In a program directed toward the synthesis of rifamycins with a lower propensity to elicit resistance development, a series of compounds were prepared that covalently combine rifamycin and quinolone pharmacophores to form stable hybrid antibacterial agents. We describe mode-of-action studies with Staphylococcus aureus of CBR-2092, a novel hybrid that combines the rifamycin SV and 4H-4-oxo-quinolizine pharmacophores. In biochemical studies, CBR-2092 exhibited rifampin-like potency as an inhibitor of RNA polymerase, was an equipotent (balanced) inhibitor of DNA gyrase and DNA topoisomerase IV, and retained activity against a prevalent quinolone-resistant variant. Macromolecular biosynthesis studies confirmed that CBR-2092 has rifampin-like effects on RNA synthesis in rifampin-susceptible strains and quinolone-like effects on DNA synthesis in rifampin-resistant strains. Studies of mutant strains that exhibited reduced susceptibility to CBR-2092 further substantiated RNA polymerase as the primary cellular target of CBR-2092, with DNA gyrase and DNA topoisomerase IV being secondary and tertiary targets, respectively, in strains exhibiting preexisting rifampin resistance. In contrast to quinolone comparator agents, no strains with altered susceptibility to CBR-2092 were found to exhibit changes consistent with altered efflux properties. The combined data indicate that CBR-2092 may have potential utility in monotherapy for the treatment of persistent S. aureus infections.

Mycoses, bacterial infections and antibacterial activity in sandifies (Psychodidae) and their possible role in the transmission of leishmaniasis

Parasitology ◽  
1985 ◽  
Vol 90 (1) ◽  
pp. 57-66 ◽  
Author(s):  
Y. Schlein ◽  
I. Polacheck ◽  
B. Yuval
Keyword(s):  
Escherichia Coli ◽  
Saccharomyces Cerevisiae ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacterial Infections ◽  
Leishmania Major ◽  
Bacterial Species ◽  
Jordan Valley ◽  
High Incidence ◽  
Group A

High incidence of mycoses were found in the guts and malpighian tubes of Phlebokomus papatasi from the Jordan Valley and P. tobbi from Zakinthos, Greece. Infections with several different bacteria were also found in the guts of female P. tobbi. Fungi cultured from guts of laboratory reared P. papatasi that had similar mycoses were identified as Aspergillus scierotiorum and Saccharomyces cerevisiae. Fungi-infected laboratory reared P. papatasi were refractory to artificial infections with a Leishmania major strain specific to them. The crop contents of P. papatasi, where sugar meals are stored, demonstrated antibacterial activity against the following bacterial species in culture: Escherichia coli, Staphylococcus aureus, Shigella sonnei, Streptococcus group A and Pseudomonas aeruginosa. It is postulated that the bacteria-free gut normal to sandflies is effected by the bacterial inhibitor present in the crop.

scholarly journals Joint antibiotic and phage therapy: addressing the limitations of a seemingly ideal phage for treating Staphylococcus aureus infections

2020 ◽  
Author(s):  
Brandon A. Berryhill ◽  
Douglas L. Huseby ◽  
Ingrid C. McCall ◽  
Diarmaid Hughes ◽  
Bruce R. Levin
Keyword(s):  
Staphylococcus Aureus ◽  
Bacterial Infections ◽  
Phage Therapy ◽  
Receptor Site ◽  
Clinical Isolates ◽  
Broad Host Range ◽  
Antibiotic Resistant ◽  
Small Colony Variants ◽  
Small Colony

AbstractIn response to increasing frequencies of antibiotic-resistant pathogens, there has been a resurrection of interest in the use of bacteriophage to treat bacterial infections: phage therapy. Here we explore the potential of a seemingly ideal phage, PYOSa, for combination phage and antibiotic treatment of Staphylococcus aureus infections. (i) This K-like phage has a broad host range; all 83 tested clinical isolates of S.aureus tested were susceptible to PYOSa. (ii) Because of the mode of action of PYOSaS. aureus is unlikely to generate classical receptor-site mutants resistant to PYOSa; none were observed in the 13 clinical isolates tested. (iii) PYOSa kills S. aureus at high rates. On the downside, the results of our experiments and tests of the joint action of PYOSa and antibiotics raise issues that must be addressed before PYOSa is employed clinically. Despite the maintenance of the phage, PYOSa does not clear the populations of S. aureus. Due to the ascent of a phenotypically diverse array of small colony variants following an initial demise, the bacterial populations return to densities similar to that of phage-free controls. Using a combination of mathematical modeling and in vitro experiments, we postulate and present evidence for a mechanism to account for the demise–resurrection dynamics of PYOSa and S. aureus. Critically for phage therapy, our experimental results suggest that treatment with PYOSa followed by bactericidal antibiotics can clear populations of S. aureus more effectively than the antibiotics alone.Significance StatementThe increasing frequency of antibiotic-resistant pathogens has fostered a quest for alternative means to treat bacterial infections. Prominent in this quest is a therapy that predates antibiotics: bacteriophage. This study explores the potential of a phage, PYOSa, for treating Staphylococcus aureus infections in combination with antibiotics. On first consideration, this phage, isolated from a commercial therapeutic cocktail, seems ideal for this purpose. The results of this population dynamic and genomic analysis study identify a potential liability of using PYOSa for therapy. Due to the production of potentially pathogenic atypical small colony variants, PYOSa alone cannot eliminate S. aureus populations. However, we demonstrate that by following the administration of PYOSa with bactericidal antibiotics, this limitation and potential liability can be addressed.

scholarly journals Aktivitas Antibakteri Komposit Ag – Tulang Ikan Cakalang pada Staphylococcus aureus

Jurnal MIPA ◽  
2018 ◽  
Vol 7 (2) ◽  
pp. 29
Author(s):  
Elmi C.J. Pandelaki ◽  
Audy D. Wuntu ◽  
Henry F. Aritonang
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacterial Infections ◽  
Food Industry ◽  
Mixing Time ◽  
Nitrate Solution ◽  
Silver Nitrate Solution ◽  
Inhibition Zone ◽  
Skipjack Tuna ◽  
Fish Bones

Telah dilakukan penelitian untuk mengetahui aktivitas antibakteri komposit Ag – tulang ikan cakalang pada Staphylococcus aureus. Tulang ikan cakalang dikeringkan, dihaluskan dan diayak 65 mesh kemudian dicampur dengan larutan perak nitrat dengan perbandingan Ag : tulang ikan sebesar 5:1 , 4:2, dan 3:3  selama 1 jam pada suhu 70 ℃. Campuran kemudian di kalsinasi pada suhu 650 ℃ selama 2 jam. Uji aktivitas antibakteri dari komposit yang terbentuk dikerjakan dengan metode sumuran menggunakan bakteri Staphylococcus aureus. Hasil penelitian menunjukkan aktivitas antibakteri pada perbandingan 4:2 dengan lama waktu pencampuran 1 jam paling efektif untuk menghambat bakteri Staphylococcus aureus dengan diameter zona hambat sebesar 25 mm. Penelitian ini menunjukkan valorisasi dari produk sampingan industri makanan seperti tulang ikan untuk membentuk bahan yang berpotensi berharga sebagai bahan implan tulang yang resistan terhadap infeksi bakteriResearch has been conducted to determine the antibacterial activity of Ag - Bone skipjack tuna toward Staphylococcus aureus. Skipjack tuna bone dried, mashed and sifted 65 mesh then mixed with silver nitrate solution with a ratio of Ag : fish bones of 5:1, 4:2, and 3:3 for 1 hour at 70 ℃. The mixture was then calcined at 650 ℃ for 2 hours. Antibacterial activity test of the composites formed was done by the method of wells using the bacteria Staphylococcus aureus. The results showed that antibacterial activity at a ratio of 4: 2 with a one-hour mixing time was most effective for inhibiting Staphylococcus aureus bacteria with a 25 mm inhibition zone diameter. This study shows the valorization of food industry byproducts such as fish bones to form potentially valuable ingredients for bone implants resistant to bacterial infections

scholarly journals Isolation of antibiotics producing bacteria from marine soil and comparative analysis of same with commercially available drugs

2021 ◽  
Vol 16 (1) ◽  
pp. 070-076
Author(s):  
Chinyelu Nkiru Umeaku ◽  
Chisom Faith Ohagwam ◽  
Chiamaka Ijeoma Chris-Umeaku
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Comparative Analysis ◽  
Bacterial Infections ◽  
Streptomyces Griseus ◽  
Zone Of Inhibition ◽  
Preliminary Screening ◽  
Port Harcourt ◽  
Marine Soil

The isolation of antibiotic producing bacteria from marine soil and comparative analysis of same with ciprofloxacin and amoxicillin against staphylococcus aureus and Escherichia coli was carried out in a Microbiology Laboratory of Chukwuemeka Odumegwu Ojukwu University, Uli. This was done to isolate antibiotic producing bacteria and compare same with existing commercially available antibiotics with a view to using marine soil in the treatment of common bacterial infections. Soil samples were collected from Bonny Island Sea, Port Harcourt. One gram of mixed soil sample was serially diluted and spread-plated on nutrient agar plates. The representative isolates obtained were sub-cultured to get a pure culture. Morphological, biochemical, physiological characteristics of the bacteria were analyzed. Agar well diffusion was carried out. One isolate had a substantial antibacterial activity with 3.5mm zone of inhibition against two test bacteria used in the preliminary screening. The isolate was marked as Streptomyces (STR I) and was identified as Streptomyces griseus while other isolates did not show any antibacterial activity. Ciprofloxacin showed the highest antibacterial activity to both Staphylococcus aureus and Escherichia coli of 3.7mm and 4.0mm respectively while Amoxicillin showed antibacterial activity of 3.5mm and 2.7mm respectively. This reveals that antibiotic producing bacteria from marine soil are also effective in antimicrobial activity and could be used for antimicrobial chemotherapy.

scholarly journals Design, Overproduction and Purification of the Chimeric Phage Lysin MLTphg Fighting against Staphylococcus aureus

Processes ◽  
2020 ◽  
Vol 8 (12) ◽  
pp. 1587
Author(s):  
Feng Wang ◽  
Xiaohang Liu ◽  
Zhengyu Deng ◽  
Yao Zhang ◽  
Xinyu Ji ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Antibiotic Resistant ◽  
E Coli ◽  
Conventional Antibiotics ◽  
Phage Lysin ◽  
Shed Light

With the increasing spread of multidrug-resistant bacterial pathogens, it is of great importance to develop alternatives to conventional antibiotics. Here, we report the generation of a chimeric phage lysin, MLTphg, which was assembled by joining the lysins derived from Meiothermus bacteriophage MMP7 and Thermus bacteriophage TSP4 with a flexible linker via chimeolysin engineering. As a potential antimicrobial agent, MLTphg can be obtained by overproduction in Escherichia coli BL21(DE3) cells and the following Ni-affinity chromatography. Finally, we recovered about 40 ± 1.9 mg of MLTphg from 1 L of the host E. coli BL21(DE3) culture. The purified MLTphg showed peak activity against Staphylococcus aureus ATCC6538 between 35 and 40 °C, and maintained approximately 44.5 ± 2.1% activity at room temperature (25 °C). Moreover, as a produced chimera, it exhibited considerably improved bactericidal activity against Staphylococcus aureus (2.9 ± 0.1 log10 reduction was observed upon 40 nM MLTphg treatment at 37 °C for 30 min) and also a group of antibiotic-resistant bacteria compared to its parental lysins, TSPphg and MMPphg. In the current age of growing antibiotic resistance, our results provide an engineering basis for developing phage lysins as novel antimicrobial agents and shed light on bacteriophage-based strategies to tackle bacterial infections.

scholarly journals Broad spectrum antibacterial photodynamic and photothermal therapy achieved with indocyanine green loaded SPIONs under near infrared irradiation

2020 ◽  
Vol 8 (16) ◽  
pp. 4616-4625 ◽  
Author(s):  
K. Bilici ◽  
N. Atac ◽  
A. Muti ◽  
I. Baylam ◽  
O. Dogan ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Indocyanine Green ◽  
Broad Spectrum ◽  
Photothermal Therapy ◽  
Bacterial Infections ◽  
Near Infrared ◽  
Alternative Therapies ◽  
Antimicrobial Photodynamic Therapy ◽  
Infrared Irradiation ◽  
Antibiotic Resistant

Antimicrobial photodynamic therapy (aPDT) and antimicrobial photothermal therapy (aPTT) are promising local and effective alternative therapies for antibiotic resistant bacterial infections and biofilms.

scholarly journals Studies on the Antibacterial Activity and Chemical Composition of Methanol Extract of Cochlospermum tinctorium Root

2019 ◽  
pp. 1-11
Author(s):  
R. Abdulaziz ◽  
M. H. Usman ◽  
U. B. Ibrahim ◽  
B. M. Tambari ◽  
A. Nafiu ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Plant Extract ◽  
Methanol Extract ◽  
Antibiotic Resistant ◽  
Food Borne Pathogens ◽  
Food Borne ◽  
Layer Chromatography

The aim of study was to evaluate the antibacterial activity of Cochlospermum tinctorium against ten (10) strains of antibiotic resistant food-borne pathogens Staphylococcus aureus and Listeria monocytogene. Ten (10) strains of antibiotic resistant food-borne pathogens Staphylococcus aureus and Listeria monocytogene procured from Microbiology Research Laboratory Usman Danfodiyo University Sokoto. The roots of Cochlospermum tinctorium were collected from the rock side in Dambu Gomo, Zuru Local Government Area of Kebbi State, Nigeria. The roots were washed, air-dried and milled to powder using mortal and pestle and sieved to obtained fine powder. Maceration was used for extraction using methanol as solvent. The antibacterial activity of the plant was determined on Mueller Hinton agar using agar well diffusion method. Minimum concentration (MIC) and minimum inhibitory concentration (MBC) of plant extract was also determined. Thin layer chromatography and column chromatography was employed for separation and fraction of different compounds in the plant extract. The fractions were screened for antibacterial activity and active fractions having high antibacterial activity were subjected Gas Chromatography Mass Spectoscopy (GC-MS) analysis. The result of methanol extraction yield 5.17% extracts. The methanol extract of Cochlospermum tinctorium was effective in inhibiting the isolates at high concentration of 10 mg/mL. The results thin layer chromatography revealed four spots with Rf values 0.02, 0.37, 0.44 and 0.80 respectively. The GC-MS analysis of the active methanol extract of Cochlospermum tinctorium root powder revealed the existence of major peaks 1-(+)-Ascorbic acid 2,6-dihexadecanoate (R.T: 13.666), Diethyl phthalate (R.T: 10.440), Undecyl acetate (R.T: 10.007), 3-tetradecanone (R.T: 9.793), 3-hexadecanone (R.T: 12.427). It therefore concluded that the root of Cochlospermum tinctorium has immense potential to be used in the area of pharmacology as it possess antimicrobial activity against the antibiotic resistant food-borne pathogens, thus could be exploited as alternative antimicrobial drugs.

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