scholarly journals Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5354
Author(s):  
Chiara Greco ◽  
Rosa Catania ◽  
Dario Leonardo Balacco ◽  
Vincenzo Taresco ◽  
Francesca Musumeci ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Protein Kinases ◽  
Heterocyclic Compounds ◽  
Bacterial Infections ◽  
Kinase Inhibitors ◽  
Antimicrobial Properties ◽  
Important Class ◽  
Prevention And Treatment ◽  
Antibacterial Evaluation

Pyrazolo[3,4-d]pyrimidines represent an important class of heterocyclic compounds well-known for their anticancer activity exerted by the inhibition of eukaryotic protein kinases. Recently, pyrazolo[3,4-d]pyrimidines have become increasingly attractive for their potential antimicrobial properties. Here, we explored the activity of a library of in-house pyrazolo[3,4-d]pyrimidines, targeting human protein kinases, against Staphylococcus aureus and Escherichia coli and their interaction with ampicillin and kanamycin, representing important classes of clinically used antibiotics. Our results represent a first step towards the potential application of dual active pyrazolo[3,4-d]pyrimidine kinase inhibitors in the prevention and treatment of bacterial infections in cancer patients.

Garlic Extract (Allium sativum L.) Effectively Inhibits Staphylococcus aureus and Escherichia coli by Invitro Test

2020 ◽  
Vol 2 (2) ◽  
pp. 61-68
Author(s):  
Agnina Listya Anggraini ◽  
Ratih Dewi Dwiyanti ◽  
Anny Thuraidah
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Bacterial Infections ◽  
Allium Sativum ◽  
Antibacterial Properties ◽  
Herbal Medicines ◽  
Garlic Extract ◽  
Dilution Method ◽  
Initial Stage

Infection is a disease caused by the presence of pathogenic microbes, including Staphylococcus aureus and Escherichia coli. Garlic (Allium sativum L.) has chemical contents such as allicin, alkaloids, flavonoids, saponins, tannins, and steroids, which can function as an antibacterial against Staphylococcus aureus and Escherichia coli. This study aims to determine the antibacterial properties of garlic extract powder against Staphylococcus aureus and Escherichia coli. This research is the initial stage of the development of herbal medicines to treat Staphylococcus aureus and Escherichia coli infections. The antibacterial activity test was carried out by the liquid dilution method. The concentrations used were 30 mg/mL, 40 mg/mL, 50 mg/mL, 60 mg/mL and 70 mg/mL. The results showed that the Minimum Inhibitory Concentration (MIC) against Staphylococcus aureus and Escherichia coli was 40 mg/mL and 50 mg / mL. Minimum Bactericidal Concentration (MBC) results for Staphylococcus aureus and Escherichia coli are 50 mg/mL and 70 mg/mL. Based on the Simple Linear Regression test, the R2 value of Staphylococcus aureus and Escherichia coli is 0.545 and 0.785, so it can be concluded that there is an effect of garlic extract powder on the growth of Staphylococcus aureus and Escherichia coli by 54.5% and 78.5%. Garlic (Allium sativum L.) extract powder has potential as herbal medicine against bacterial infections but requires further research to determine its effect in vivo.

scholarly journals A Novel Antimicrobial Phenanthrene Alkaloid from Bryopyllum pinnatum

2011 ◽  
Vol 8 (3) ◽  
pp. 1456-1461 ◽  
Author(s):  
Donatus Ebere Okwu ◽  
Fred Uchenna Nnamdi
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Ethanolic Extract ◽  
Klebsiella Pneumonia ◽  
Antimicrobial Studies ◽  
Prevention And Treatment ◽  
Kalanchoe Pinnata ◽  
Isolated Compound

Phenenthrene alkaloid identified as 1-ethanamino 7 hex-1-yne-5I-one phenanthrene was isolated from the ethanolic extract of the leaves ofBryophyllum pinnatum(syn. B. calcinum kalanchoe pinnata) a versatile Nigeria medicinal plant. The structure was elucidated using NMR, IR, UV and MS spectral data. Antimicrobial studies showed that the isolated compound successfully inhibitedPsuedomonas aeruginosa, Klebsiella pneumonia, Staphylococcus aureus, Escherichia coli, Candida albicansandAspergillus niger. This result authenticates the use ofbryophyllum pinantumin phytomedicine for disease prevention and treatment of infections.

scholarly journals Investigation of the antimicrobial activity of danofoloxacin against bacteria pathogens in goats

2020 ◽  
Vol 22 (97) ◽  
pp. 74-78
Author(s):  
T. I. Stetsko ◽  
Ya. M. Liubenko ◽  
V. N. Padovskyi ◽  
L. L. Ostrovska ◽  
O. Yo. Kalinina ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Bacterial Infections ◽  
Chemotherapeutic Agents ◽  
Diffusion Method ◽  
Bacteriostatic Activity ◽  
Intestinal Infection ◽  
Sensitivity Testing ◽  
First Choice

Fluoroquinolones are critical antimicrobials for both human and veterinary medicine. Due to their unique mechanism of antimicrobial action and good pharmacokinetic properties, they are often the first choice drugs in the treatment of bacterial infections in animals. The purpose of the investigation was to study the antimicrobial activity of a third-generation fluoroquinolone antibiotic of danofloxacin against bacteria, pathogens of respiratory and intestinal infection in goats. The samples of the nasal outflows (respiratory infection) and fecal masses (intestinal infection) were collected from clinically ill goats for microbiological studies. The sensitivity test of the microflora of the biomaterial, carried out by the disco-diffusion method, showed that the microorganisms of all the samples were sensitive to danofloxacin. Bacteria Streptococcus pneumonia (n = 10), Staphylococcus aureus (n = 4) and Escherichia coli (n = 2) were isolated and identified from nasal exudate samples (n = 10). Pathogenic strains of Escherichia coli were isolated from all faecal samples (n = 12). The degree of bacteriostatic activity of danofloxacin was determined by establishing its minimum inhibitory concentration (MIC) for bacterial isolates by sequential dilutions in a liquid nutrient medium. The average MIC of danofloxacin for Streptococcus pneumoniae isolates was 0.26 ± 0.13 μg/ml and for Staphylococcus aureus isolates – 0.25 ± 0.075 μg/ml. For Escherichia coli strains isolated from faeces of goats suffering from coli infection, the average MIC of danofloxacin was 0.38 ± 0.12 μg/ml (range 0.2 to 0.8 μg/ml). Antimicrobial sensitivity testing have shown a high level of bacteriostatic activity of danofloxacin against bacteria, pathogens of respiratory and intestinal infections in goats. This may be the argument for the use of danofloxacin-based chemotherapeutic agents in the treatment of bacterial infections in goats, especially for the empirical approach to therapy.

scholarly journals ESTUDO FITOQUÍMICO E DE ATIVIDADE ANTIMICROBIANA DE Ptychopetalum olacoides Bentham

2002 ◽  
Vol 3 (2) ◽  
Author(s):  
P. D. MONTRUCCHIO ◽  
O. G. MIGUEL
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Fusarium Oxysporum ◽  
Staphylococcus Epidermidis ◽  
Antimicrobial Properties ◽  
Colletotrichum Acutatum ◽  
Alcoholic Extract ◽  
Phytochemical Study ◽  
North Brazil ◽  
Long Time

A espécie Ptychopetalum olacoides Bentham, popularmente conhecida como “marapuama” ou “muirapuama”, é uma Olacaceae nativa da região norte do Brasil, há muito conhecida e utilizada por suas propriedades estimulantes e afrodisíacas, sendo inclusive exportada para diversos países. O estudo fitoquímico do lenho desta árvore, neste trabalho representado pelos galhos da planta, revelou a presença majoritária de vários ácidos graxos, esteróides e xantinas, sendo eles: ácido palmítico, ácido esteárico, -sitosterol, estigmasterol, lupeol, glutinol, a-amirina, cafeína, teobromina e adenina, sendo que as três últimas não haviam ainda sido reportadas na espécie. O estudo das atividades antimicrobianas revelou que os extratos da planta não apresentam atividade inibitória sobre o desenvolvimento de cepas de Escherichia coli, Staphylococcus aureus ou Staphylococcus epidermidis. Porém, o resíduo do extrato alcoólico apresenta uma significativa ação inibitória do crescimento micelial de Colletotrichum acutatum, e ação menos pronunciada sobre o crescimento de Fusarium oxysporum. PHYTOCHEMICAL STUDY AND ANTIMICROBIAL ACTIVITY OF Ptychopetalumolacoides Bentham Abstract Ptychopetalum olacoides Bentham, popularly known as “marapuama” or “muirapuama”, is an Olacaceae native from north Brazil, known and used for its stimulating and aphrodisiac properties for a long time, being also exported to several countries all over the world. The phytochemical study of the wood of this tree, represented by its stems, revealed the presence of several fatty acids, sterols and xanthines, including palmitic acid, stearic acid, -sitosterol, stigmasterol, lupeol, glutinol, a-amirin, caffeine, theobromine and adenine, and the latest three substances have not been reported in this specie yet. The study of antimicrobial properties revealed that the plant extracts don’t have any inhibitory activity against strains of Escherichia coli, Staphylococcus aureus or Staphylococcus epidermidis. However, the alcoholic extract residue does have a remarkable inhibitory action on the mycelial growth of Colletotrichum acutatum and Fusarium oxysporum.26

scholarly journals Systems developed for application as self-cleaning surfaces and/or antimicrobial properties: a short review on materials and production methods

Cerâmica ◽  
2019 ◽  
Vol 65 (375) ◽  
pp. 477-484 ◽  
Author(s):  
M. P. Madeira ◽  
A. O. Lobo ◽  
B. C. Viana ◽  
E. C. Silva Filho ◽  
J. A. Osajima
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Photocatalytic Activity ◽  
Medical Devices ◽  
Spin Coating ◽  
Antimicrobial Properties ◽  
Short Review ◽  
Dip Coating ◽  
Production Methods ◽  
Self Cleaning

Abstract Herein we present a short review of different materials and techniques that have been used for the production of surfaces with self-cleaning and/or antimicrobial properties. From this, it was verified that titanium dioxide was the most frequently used compound to obtain surfaces with these properties; however, other materials such as silica, zinc and silver have also been used for this purpose. The spin-coating and dip-coating techniques were the most used techniques, and the bacteria Staphylococcus aureus and Escherichia coli were the most used in the antimicrobial assays. The analyzed studies showed that it is possible to obtain surfaces with both self-cleaning and/or antimicrobial properties, as well as with photocatalytic activity. Regarding possible applications, it is possible to highlight the interest in the production of glass and medical devices with self-cleaning and/or antimicrobial action.

scholarly journals Antimicrobial Activity of Cultivable Endophytic and Rhizosphere Fungi Associated with “Mile-a-Minute,” Mikania cordata (Asteraceae)

2020 ◽  
Vol 2020 ◽  
pp. 1-7 ◽  
Author(s):  
Pavithra L. Jayatilake ◽  
Helani Munasinghe
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antimicrobial Properties ◽  
Pharmaceutical Products ◽  
Diffusion Method ◽  
Molecular Characteristics ◽  
Disk Diffusion Method ◽  
Rhizosphere Fungi

Endophytic and rhizosphere fungi are understood to be aiding the host plant to overcome a range of biotic and abiotic stresses (nutrition depletion, droughts, etc.) hence, they remain to be reservoirs of plethora of natural products with immense use. Consequently, this investigation of endophytic and rhizosphere fungi isolated from Mikania cordata (a perennial vine that is well established in Sri Lanka) for their antimicrobial properties was performed with the aim of future derivation of potential beneficial pharmaceutical products. Leaves, twigs, and roots of M. cordata were utilized to isolate a total of 9 endophytic fungi out of which the highest amount (44%) accounted was from the twigs. A sample of the immediate layer of soil adhering to the root of M. cordata was utilized to isolate 15 rhizosphere fungi. Fusarium equiseti and Phoma medicaginis were endophytes that were identified based on colony and molecular characteristics. The broad spectrum of antimicrobial activity depicted by F. equiseti (MK517551) was found to be significantly greater (p≤0.05, inhibitory against Bacillus cereus ATCC 11778, Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, and Pseudomonas aeruginosa ATCC 25853) than P. medicaginis (MK517550) (inhibitory against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, and Pseudomonas aeruginosa ATCC 25853) as assessed using the Kirby-Bauer disk diffusion method. Trichoderma virens and Trichoderma asperellum were rhizospere fungi that exhibited remarkable antimicrobial properties against the test pathogens chosen for the study. T. asperellum indicated significantly greater bioactivity against all four bacterial pathogens and Candida albicans ATCC 10231 under study. The ranges of minimum inhibitory concentrations (MICs) of the fungi depicting antimicrobial properties were determined. The results obtained suggest that F. equiseti, P. medicaginis, T. asperellum, and T. virens of M. cordata harness bioprospective values as natural drug candidates. This is the first report on isolation and evaluation of the antimicrobial properties of endophytic and rhizosphere fungi of Mikania cordata.

scholarly journals Serum and Lung Pharmacokinetics of ASN100, a Monoclonal Antibody Combination for the Prevention and Treatment of Staphylococcus aureus Pneumonia

2017 ◽  
Vol 4 (suppl_1) ◽  
pp. S310-S310 ◽  
Author(s):  
Zoltan Magyarics ◽  
Fraser Leslie ◽  
Steven A Luperchio ◽  
Johann Bartko ◽  
Christian Schörgenhofer ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Bacterial Infections ◽  
Phase 1 ◽  
Fixed Dose ◽  
Open Label ◽  
Post Dose ◽  
Double Blind ◽  
Dose Time ◽  
Prevention And Treatment ◽  
Acute Bacterial Infections

Abstract Background Monoclonal antibodies (mAbs) are well-suited for the prevention and treatment of acute bacterial infections. ASN100 is a combination of two fully human IgG1 mAbs, ASN-1 and ASN-2 that together neutralize six Staphylococcus aureus cytotoxins, alpha-hemolysin (Hla) and five leukocidins (HlgAB, HlgCB, LukED, LukSF [PVL] and LukGH) that are important in the pathogenesis of S. Aureus pneumonia. We aimed to characterize the pharmacokinetics (PK) of ASN100 in both serum and lung epithelial lining fluid (ELF) in male and female healthy volunteers. Methods The safety, tolerability, and serum and lung PK of single intravenous infusion of ASN100 was evaluated in a Phase 1 study. Eight subjects (3:1 randomization) in two double-blind cohorts received ASN100 (doses of 3600 mg or 8000 mg) or placebo. ASN-1 and ASN-2 were administered in a fixed dose 1:1 ratio. Twelve subjects received ASN100 open-label at doses of 3600 mg or 8000 mg and each underwent two bronchoalveolar lavage (BAL) fluid collections either on days 1 and 30 or on days 2 and 8 post-dosing. ASN-1 and ASN-2 concentrations were determined by ELISA. The ELF concentrations were normalized based on urea concentrations in serum and BAL fluid. Results No dose limiting toxicity was observed. Adverse events (AEs) showed no association of increased incidence with higher dose. All AEs were mild or moderate in severity, with 83.3% of subjects receiving ASN100 reporting at least one AE vs. 100% of placebo subjects. A dose proportional increase in serum peak and exposure (AUC) of ASN-1 and ASN-2 was observed and the serum PK of ASN-1 and ASN-2 were comparable (approximate half-life of each antibody was 3 weeks). Penetration of ASN-1 and ASN-2 into the ELF of the lung was observed at the first post-dose time point of 24 hours, peak concentrations were observed after day 2 and the mAbs remained detectable at day 30. Conclusion ASN100 was safe and well tolerated at doses up to 8000 mg (4000 mg ASN-1 and 4000 mg ASN-2). The PK profiles of ASN-1 and ASN-2 were comparable following simultaneous administration. Significant lung concentrations of each mAb were demonstrated between day 1 and 30 post-dosing. These data support continued clinical development of ASN100 for the prevention and treatment of S. Aureus pneumonia. Disclosures Z. Magyarics, Arsanis Biosciences GmbH: Employee, Salary. Arsanis, Inc.: Shareholder, Share options. F. Leslie, Arsanis., Inc.: Employee and Shareholder, Salary. S. A. Luperchio, Arsanis Inc.: Employee and Shareholder, Salary. B. Jilma, Arsanis Biosciences GmbH: Investigator, Investigator fee. C. Stevens, Arsanis Inc.: Employee and Shareholder, Salary.E. Nagy, Arsanis: Employee and Shareholder, Salary.

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 Антимікробна активність нового комбінованого антибактеріального препарату на основі флуорфеніколу та доксицикліну

2017 ◽  
Vol 19 (77) ◽  
pp. 125-130
Author(s):  
T.I. Stetsko ◽  
V.P. Muzyka ◽  
L.L. Ostrovska ◽  
V.I. Butsyak
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Bacterial Infections ◽  
Streptococcus Suis ◽  
Bordetella Bronchiseptica ◽  
Bacteriostatic Activity ◽  
Active Ingredients ◽  
Combination Drug ◽  
Salmonella Pullorum

Bacterial infections of noncontagious character is one of the most common diseases among livestock and poultry. Often an association of microorganisms is etiological factor for these diseases. In this case, actual is an introduction into clinical practice antibiotics with a broad spectrum of antimicrobial activity, which would cover the most microorganisms, causative agents of bacterial infections. One of appropriate and suitable methods that would increased the effectiveness of chemotherapy of bacterial infections is a rational use of a combination of antimicrobial agents. In the article the results of the study of antimicrobial activity of new combined antibacterial preparation, based on synthetic antibiotic florfenicol from the group amfenicols and doxycycline from the group of tetracyclines, are given. The level of bacteriostatic activity of the combination drug was compared with bacteriostatic activity of monopreparations, active ingredients in ones are separately florfenicol and doxycycline. Were determined the minimum inhibitory concentration (MIC) of the combined drug and monopreparations for gram-positive and gram-negative bacteria such as Staphylococcus aureus, Streptococcus suis, Bordetella bronchiseptica, Escherichia coli and Salmonella pullorum, isolated from biological material, took from pigs and broiler chickens with various bacterial diseases. The results showed that florfenicol and doxycycline in combined preparation act indifferently regarding isolates Staphylococcus aureus, Streptococcus suis and Escherichia coli, when every antibiotic in an combination demonstrates independent action on the organism, not different activity at their separate application. At the same time, the active ingredients of the combined drug showed a synergistic effect against the isolated strains Bordetella bronchiseptica and Salmonella pullorum, demonstrated by increasing the activity of the combination of antibacterial compounds compared to the sum of their independent effects by increasing the activity of one or both of active drug components.

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.

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