scholarly journals An Activity of Thioacyl Derivatives of 4-Aminoquinolinium Salts towards Biofilm Producing and Planktonic Forms of Coagulase-Negative Staphylococci

2015 ◽  
Vol 2015 ◽  
pp. 1-10 ◽  
Author(s):  
Robert D. Wojtyczka ◽  
Andrzej Zięba ◽  
Arkadiusz Dziedzic ◽  
Małgorzata Kępa ◽  
Danuta Idzik
Keyword(s):  
Biofilm Formation ◽  
Hospital Environment ◽  
Initial Assessment ◽  
Coagulase Negative Staphylococci ◽  
Planktonic Form ◽  
The Mean ◽  
New Compounds ◽  
Derivatives Of ◽  
Mean Concentration ◽  
Mic Value

Microorganisms present in different environments have developed specific mechanisms of settling on various abiotic and biotic surfaces by forming a biofilm. It seems to be well justified to search for new compounds enabling biofilm reduction, which is highly resistant to antibiotics. This study was thus an initial assessment of the antibacterial activity of two new quinoline derivatives of a structure of 3-thioacyl 1-methyl 4-arylaminoquinolinium salts against coagulase-negative staphylococci (CoNS) isolated from a hospital environment, in a form of both biofilms and in planktonic form. Thirty-three stains of CoNS isolated from the hospital environment (air, surfaces) and seven reference strains from the ATCC collection were selected for the study. The mean MIC value for 1-methyl-3-benzoylthio-4-(4-chlorophenylamino)quinolinum chloride (4-chlorophenylamino derivative) was 42.60 ± 19.91 μg/mL, and in the case of strains subjected to 1-methyl-3-benzoylthio-4-(4-fluorophenylamino)quinolinum chloride (4-fluorophenylamino derivative) activity, the mean MIC value was 43.20 ± 14.30 μg/mL. The mean concentration of 4-chlorophenylamino derivative that inhibited biofilm formation was 86.18 ± 30.64 μg/mL. The mean concentration of 4-fluorophenylamino derivatives that inhibited biofilm formation was higher and amounted to 237.09 ± 160.57 μg/mL. Based on the results, both derivatives of the examined compounds exhibit high antimicrobial activity towards strains growing both in planktonic and biofilm form.

scholarly journals New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation

Marine Drugs ◽  
2018 ◽  
Vol 16 (8) ◽  
pp. 274 ◽  
Author(s):  
Anna Carbone ◽  
Barbara Parrino ◽  
Maria Cusimano ◽  
Virginia Spanò ◽  
Alessandra Montalbano ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Biofilm Formation ◽  
Microbial Growth ◽  
Bacterial Biofilm ◽  
Dependent Manner ◽  
Gram Negative ◽  
Ic50 Values ◽  
Planktonic Form ◽  
New Compounds ◽  
Dose Dependent

New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40–2.03 µM. The new compounds showed a typical anti-virulence profile, being able to inhibit the biofilm formation without affecting the microbial growth in the planktonic form.

4-Hydroxy-2-pyridone Derivatives and the δ-pyrone Isostere as Novel Agents Against Mycobacterium smegmatis Biofilm Inhibitors

2019 ◽  
Vol 15 (1) ◽  
pp. 28-37 ◽  
Author(s):  
Maheshkumar R. Borkar ◽  
Santosh Nandan ◽  
Harish K.M. Nagaraj ◽  
Jayashree Puttur ◽  
Jisha Manniyodath ◽  
...  
Keyword(s):  
Small Molecules ◽  
Mycobacterium Smegmatis ◽  
Biofilm Formation ◽  
Antibacterial Agents ◽  
Free Form ◽  
Antimycobacterial Agents ◽  
Planktonic Form ◽  
The Individual ◽  
Antibiofilm Agents ◽  
Derivatives Of

Background: The treatment of a bacterial infection when the bacterium is growing in a biofilm is a vexed issue. This is because the bacteria in a biofilm behaves differently compared to the individual planktonic free-form. As a result, traditional antibacterial agents lose their activity. Objective: Presently, there are not many drugs that are effective against bacteria growing in biofilms. Based on literature reports, we have sought to develop novel derivatives of 4-hydroxy-2- pyridone as both antimycobacterial and antibiofilm agents. </P><P> Methods: The pyridone derivatives were synthesized by reacting 4-hydroxy-6-methyl-2H-pyran-2- one with appropriate amines and followed by reaction with substituted phenyl isocyanates as reported in the literature. Results: Four compounds in this series significantly inhibit the growth and formation of biofilm by Mycobacterium smegmatis (mc2 155 strain) at 50 µg/ml. Further, in silico evaluation of the ADME parameters shows that these compounds possess good drug-like properties and have the potential to be developed both as antibiofilm and as oral antimycobacterial agents. Conclusion: This finding is of significance as presently very few small molecules are known to inhibit biofilm formation in mycobacteria. These compounds are unique in the sense that they are more potent against Mycobacterium smegmatis in the biofilm state compared to the planktonic form.

scholarly journals ANTIBIOTIC RESISTANCE, MECA GENE DETECTION, AND BIOFILM FORMATION ABILITY AMONG COAGULASE-NEGATIVE STAPHYLOCOCCI IN CANCER PATIENTS

2021 ◽  
pp. 35-39
Author(s):  
DILSHA TK ◽  
SAJANI SAMUEL ◽  
PARTHIBAN RUDRAPATHY ◽  
SARAVANAN MURUGESAN ◽  
SARATH KE
Keyword(s):  
Antibiotic Resistance ◽  
Biofilm Formation ◽  
Bacterial Species ◽  
Meca Gene ◽  
Hospital Environment ◽  
Clinical Samples ◽  
Automated Identification ◽  
Coagulase Negative Staphylococci ◽  
Increased Risk ◽  
Vitek 2

Objective: The objective of the study was to identify coagulase-negative staphylococci (CoNS) from various clinical samples and to determine the antibiotic resistance of the isolates by means of automation (VITEK-2), as well as to detect biofilm formation using Congo red agar method and to detect mecA gene by automated identification method (VITEK-2). Methods: All the clinical samples (blood, urine, sputum, BAL, throat swab, wound swab, aspirated fluid, pleural fluid, and pus) received in the microbiology laboratory were processed by aseptic techniques. Clinical samples were inoculated on appropriate media (blood agar, MacConkey agar, and chocolate agar [HIMEDIA]). After inoculation, the culture plates were incubated at 37°C aerobically for 18–24 h for growth. Positive cultures were picked up and further bacterial species identification was done using automated techniques (MALDI- TOF). Results: Among 28 isolates, the most recurrent strains of CoNS are Staphylococcus epidermidis, Staphylococcus hominis, Staphylococcus lugdunensis, and Staphylococcus haemolyticus. The assessment of antibacterial drugs sensitivity shows that all the isolates were more sensitive to daptomycin (S. epidermidis 100%, S. hominis 100%, S. lugdunensis 100%, and S. haemolyticus 42.85%) followed by linezolid (S. epidermidis [69.23%], S. hominis [100%], S. lugdunensis [100%], and S. haemolyticus [57.14%]) and vancomycin (S. epidermidis [100%], S. hominis [40%], S. lugdunensis [100%], S. haemolyticus [42.85%]). The analysis revealed the presence of the mecA gene (67.85%) and biofilm production (85.71%), respectively. Conclusion: Our data indicate that the hospital environment can be colonized by biofilm forming CoNS and transmission of these strains can cause an increased risk of serious nosocomial infections.

Reassessment of Suicide Attempters at Home, Shortly After Discharge from Hospital

Crisis ◽  
2010 ◽  
Vol 31 (6) ◽  
pp. 303-310 ◽  
Author(s):  
Bas Verwey ◽  
Jeroen A. van Waarde ◽  
Molla A. Bozdağ ◽  
Iris van Rooij ◽  
Edwin de Beurs ◽  
...  
Keyword(s):  
Suicide Attempt ◽  
General Hospital ◽  
Hospital Environment ◽  
Initial Assessment ◽  
Suicide Attempters ◽  
Systematic Assessment ◽  
Suicide Intent ◽  
Initial Hospital ◽  
Discharge From Hospital ◽  
At Home

Background: Assessment of suicide attempters in a general hospital may be influenced by the condition of the patient and the unfavorable circumstances of the hospital environment. Aims: To determine whether the results of a reassessment at home shortly after discharge from hospital differ from the initial assessment in the hospital. Methods: In this prospective study, systematic assessment of 52 suicide attempters in a general hospital was compared with reassessment at home, shortly after discharge. Results: Reassessments at home concerning suicide intent, motives for suicide attempt, and dimensions of psychopathology did not differ significantly from the initial hospital assessment. However, patients’ motives for the suicide attempt had changed to being less impulsive and more suicidal, worrying was significantly higher, and self-esteem was significantly lower. A third of the patients had forgotten their aftercare arrangements and most patients who initially felt no need for additional help had changed their mind at reassessment. Conclusions: Results from this group of suicide attempters suggest that a brief reassessment at home shortly after discharge from hospital should be considered.

Instant 99mTc-Labelled Glucoheptonate Kit for Kidney Imaging

1983 ◽  
Vol 22 (05) ◽  
pp. 246-250 ◽  
Author(s):  
M. Al-Hilli ◽  
H. M. A. Karim ◽  
M. H. S. Al-Hissoni ◽  
M. N. Jassim ◽  
N. H. Agha
Keyword(s):  
Sodium Hydroxide Solution ◽  
Normal Subjects ◽  
Organ Distribution ◽  
Stable Complex ◽  
Scintillation Camera ◽  
Ph Adjustment ◽  
The Mean ◽  
The Stability ◽  
Kidney Imaging ◽  
Mean Concentration

Gelchromatography column scanning has been used to study the fractions of reduced hydrolyzed 99mTc, 99mTc-pertechnetate and 99mTc-chelate in a 99mTc-glucoheptonate (GH) preparation. A stable high labelling yield of 99mTc-GH complex in the radiopharmaceutical has been obtained with a concentration of 40-50 mg of glucoheptonic acid-calcium salt and not less than 0.45 mg of SnCl2 2 H2O at an optimal pH between 6.5 and 7.0. The stability of the complex has been found significantly affected when sodium hydroxide solution was used for the pH adjustment. However, an alternative procedure for final pH adjustment of the preparation has been investigated providing a stable complex for the usual period of time prior to the injection. The organ distribution and the blood clearance data of 99mTc-GH in rabbits were relatively similar to those reported earlier. The mean concentration of the radiopharmaceutical in both kidneys has been studied in normal subjects for one hour with a scintillation camera and the results were satisfactory.

PROGESTERONE IN THE HUMAN PERIPHERAL BLOOD IN THE PREOVULATORY PERIOD OF THE MENSTRUAL CYCLE

1967 ◽  
Vol 55 (1) ◽  
pp. 91-96 ◽  
Author(s):  
Benno Runnebaum ◽  
Josef Zander
Keyword(s):  
Menstrual Cycle ◽  
Corpus Luteum ◽  
Peripheral Blood ◽  
Human Peripheral Blood ◽  
Progesterone Concentration ◽  
Plasma Progesterone ◽  
Progesterone Secretion ◽  
Graafian Follicle ◽  
The Mean ◽  
Mean Concentration

ABSTRACT Progesterone was determined and identified in human peripheral blood during the preovulatory period of the menstrual cycle, by combined isotope derivative and recrystallization analysis. The mean concentration of progesterone in 1.095 ml of plasma obtained 9 days before ovulation was 0.084 μg/100 ml. However, the mean concentration of progesterone in 1.122 ml of plasma obtained 4 days before ovulation was 0.279 μg/100 ml. These data demonstrate a source of progesterone secretion other than the corpus luteum. The higher plasma-progesterone concentration 4 days before ovulation may indicate progesterone secretion of the ripening Graafian follicle of the ovary.

SOME DIRECTIONS IN THE MODIFICATION OF AZOLES

2020 ◽  
Vol 5 (443) ◽  
pp. 85-91
Author(s):  
Ibrayev M.K., ◽  
◽  
Takibayeva A.T., ◽  
Fazylov S.D., ◽  
Rakhimberlinova Zh.B., ◽  
...  
Keyword(s):  
13C Nmr Spectroscopy ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Synthesis Conditions ◽  
Alkaloid Cytisine ◽  
Azole Ring ◽  
Cyclic Compounds ◽  
New Compounds ◽  
Derivatives Of

This article presents studies on the targeted search for new derivatives of azoles, such as benzthiazole, 3,5-dimethylpyrazole, 1,3,4-oxadiazole-2-thione, 1,3,4-thiadiazole. The possibility of combining in one molecule of the azole ring with other cyclic compounds: the alkaloid cytisine, morpholine, furan and some arenes has been studied. To obtain new compounds, the reactions of bromination, acylation, and interaction with isothiocyanates were studied. Optimal synthesis conditions were studied for all reactions. It was found that the reaction of 4-bromo-3,5-dimethylpyrazole with isothiocyanates, in contrast to the previously written derivatives of anilines, takes a longer time and requires heating the reaction mixture. The combination of a pirasol fragment with halide substituents often results in an enhanced therapeutic effect. The synthesized 2-bromine-N-(6-rodanbenzo[d]thiazole-2-yl)acetamide, due to the alkylbromide group, is an important synth in the synthesis of new benzthiazole derivatives. Its derivatives combine in one molecule the rest of rhodanbenzthiazole with alkaloid cytisine and biogenic amine morpholine and are potentially biologically active compounds, since the molecule structure contains several pharmacophoric fragments: benzthiazole and alkaloid (amine) heterocycles, rhodane and urea groups. The mechanism of formation of 1,3,4-oxadiazole-2-tyons from hydrazides under action on them by carbon disulfide was studied and assumed. It was shown that dithiocarbamates in acidic medium decompose with the release of hydrogen sulfide and the formation of highly reactive isothiocyanate group. Then, intra-molecular cyclization occurs, with the formation of end products - 1,3,4-oxadiazole-2-thions. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy. All synthesized substances are potentially biologically active compounds, since they contain several pharmacophore fragments in their structure.

Synthesis and Antimicrobial activities of Some Polyphenol compounds by Nano ZnO-TBAB as a Heterogeneous Catalytic Media

2020 ◽  
Vol 17 ◽  
Author(s):  
Rahele Bargebid ◽  
Ali Khalafi-Nezhad ◽  
Kamiar Zomorodian ◽  
Leila Zamani ◽  
Ali Ahmadinejad ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Reusable Catalyst ◽  
Nano Zno ◽  
Antifungal Activities ◽  
Chemical Structures ◽  
Heterogeneous Catalytic ◽  
Solvent Free Conditions ◽  
New Compounds ◽  
Derivatives Of

Introduction: Mannich reaction is a typical example of a three-component condensation reaction and the chemistry of Mannich bases has been the matter of search by researchers. Here an efficient procedure for the synthesis of some new Mannich derivatives of simple phenols is described. Methods: In this procedure a microwave-assisted and solvent less condensation were done between different phenols, secondary amines and paraformaldehyde. The reactions proceed in the presence of catalytic amount of nano ZnO and tetrabutylammonium bromide (TBAB) in excellent yields. 10 new compounds were synthesized (A1-A10). Chemical structures of all new compounds were confirmed by different spectroscopic methods. We optimized the chemical reactions in different conditions. Optimization reactions were done in the presence of different mineral oxides, different amount of TBAB and also different solvents. Nano ZnO and TBAB in catalytic amounts and solvent free conditions were the best conditions. All the synthesized compounds were screened for their antimicrobial activities. Antifungal and antibacterial activities of the synthesized compounds were evaluated against some Candida, filaments fungi, gram positive and gram negative bacteria by broth micro dilution method as recommended by CLSI. Results: The result showed that compounds A2, A3 and A4 against most of the tested Candida species and compounds A5 and A7 against C. parapsilosis and C. tropicalis, exhibited considerable antifungal activities. Also Compounds A8 and A10 showed desirable antifungal activities against C. neoformance and C. parapsilosis, respectively. The antibacterial activities of the synthesized compounds were also evaluated. Compounds A6 - A10 against E. Fecalis and compounds A5, A7, A9 and A10 against P. aeruginosa showed desirable antibacterial activities. Discussion: We have synthesized some new Mannich adducts of poly-hydroxyl phenols in the presence of nano-ZnO as a reusable catalyst, with the hope of discovering new lead compounds serving as potent antimicrobial agents. The advantages of this method are generality, high yields with short reaction times, simplicity, low cost and matching with green chemistry protocols. The antimicriobial studies of Mannich derivatives of phenols showed desirable results in vitro.

scholarly journals The Relationship between Inflammation Markers (CRP, IL-6, sCD40L) and Colorectal Cancer Stage, Grade, Size and Location

Diagnostics ◽  
2021 ◽  
Vol 11 (8) ◽  
pp. 1382
Author(s):  
Olga Martyna Koper-Lenkiewicz ◽  
Violetta Dymicka-Piekarska ◽  
Anna Justyna Milewska ◽  
Justyna Zińczuk ◽  
Joanna Kamińska
Keyword(s):  
Colorectal Cancer ◽  
Linear Regression ◽  
Tumor Size ◽  
Distal Colon ◽  
Proximal Colon ◽  
Model Parameters ◽  
Grade Group ◽  
Who Grade ◽  
The Mean ◽  
Mean Concentration

The aim of the study was the evaluation whether in primary colorectal cancer (CRC) patients (n = 55): age, sex, TNM classification results, WHO grade, tumor location (proximal colon, distal colon, rectum), tumor size, platelet count (PLT), mean platelet volume (MPV), mean platelet component (MCP), levels of carcinoembryonic antigen (CEA), cancer antigen (CA 19-9), as well as soluble lectin adhesion molecules (L-, E-, and P-selectins) may influence circulating inflammatory biomarkers: IL-6, CRP, and sCD40L. We found that CRP concentration evaluation in routine clinical practice may have an advantage as a prognostic biomarker in CRC patients, as this protein the most comprehensively reflects clinicopathological features of the tumor. Univariate linear regression analysis revealed that in CRC patients: (1) with an increase in PLT by 10 × 103/μL, the mean concentration of CRP increases by 3.4%; (2) with an increase in CA 19-9 of 1 U/mL, the mean concentration of CRP increases by 0.7%; (3) with the WHO 2 grade, the mean CRP concentration increases 3.631 times relative to the WHO 1 grade group; (4) with the WHO 3 grade, the mean CRP concentration increases by 4.916 times relative to the WHO 1 grade group; (5) with metastases (T1-4N+M+) the mean CRP concentration increases 4.183 times compared to non-metastatic patients (T1-4N0M0); (6) with a tumor located in the proximal colon, the mean concentration of CRP increases 2.175 times compared to a tumor located in the distal colon; (7) in patients with tumor size > 3 cm, the CRP concentration is about 2 times higher than in patients with tumor size ≤ 3 cm. In the multivariate linear regression model, the variables that influence the mean CRP value in CRC patients included: WHO grade and tumor localization. R2 for the created model equals 0.50, which indicates that this model explains 50% of the variance in the dependent variable. In CRC subjects: (1) with the WHO 2 grade, the mean CRP concentration rises 3.924 times relative to the WHO 1 grade; (2) with the WHO 3 grade, the mean CRP concentration increases 4.721 times in relation to the WHO 1 grade; (3) with a tumor located in the rectum, the mean CRP concentration rises 2.139 times compared to a tumor located in the distal colon; (4) with a tumor located in the proximal colon, the mean concentration of CRP increases 1.998 times compared to the tumor located in the distal colon; if other model parameters are fixed.

scholarly journals Virulence Factors in Coagulase-Negative Staphylococci

Pathogens ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 170
Author(s):  
Angela França ◽  
Vânia Gaio ◽  
Nathalie Lopes ◽  
Luís D. R. Melo
Keyword(s):  
Antibiotic Resistance ◽  
Virulence Factors ◽  
Resistance Genes ◽  
Biofilm Formation ◽  
Antibiotic Resistance Genes ◽  
Coagulase Negative Staphylococci ◽  
Healthcare Associated ◽  
Major Pathogens

Coagulase-negative staphylococci (CoNS) have emerged as major pathogens in healthcare-associated facilities, being S. epidermidis, S. haemolyticus and, more recently, S. lugdunensis, the most clinically relevant species. Despite being less virulent than the well-studied pathogen S. aureus, the number of CoNS strains sequenced is constantly increasing and, with that, the number of virulence factors identified in those strains. In this regard, biofilm formation is considered the most important. Besides virulence factors, the presence of several antibiotic-resistance genes identified in CoNS is worrisome and makes treatment very challenging. In this review, we analyzed the different aspects involved in CoNS virulence and their impact on health and food.

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