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1.
Antibiotics (Basel) ; 12(2)2023 Jan 22.
Article in English | MEDLINE | ID: mdl-36830146

ABSTRACT

The aim of the study is to evaluate the effect of the addition of selected fruits and herbs belonging to the "superfoods" category for the bioactivity of a rapeseed honey matrix. Flavored creamed honeys with nine types of various additives (2 and 4% of content) were prepared and analyzed for the content of total phenols, flavonoids, antioxidant (FRAP, DPPH and ABTS) and antibacterial activity against four strains of bacteria. Additionally, the impact of three months of storage on the antioxidant properties of the products obtained was examined. The significant dose-dependent increase in the content of bioactive ingredients and antioxidant capacity in spiced honeys, as compared to control honey, was observed. The highest enrichment was obtained for the addition of powdered sea buckthorn leaves and black raspberry fruits. Honey with the addition of sea buckthorn leaves inhibited the growth of P. aeruginosa, S. aureus and K. pneumonia, whereas honeys with black raspberry and blackcurrant fruits showed activity only on the latter two strains. Furthermore, what is more interesting, honey supplemented with sea buckthorn leaf and black raspberry fruits inhibited S. aureus biofilm formation at the sub-minimum inhibitory concentrations (sub-MICs), showing a dose-dependent anti-biofilm effect.

2.
Int J Mol Sci ; 23(11)2022 Jun 05.
Article in English | MEDLINE | ID: mdl-35682998

ABSTRACT

A novel series of coumarin-thiadiazole hybrids, derived from substituted coumarin-3-carboxylic acids was isolated and fully characterized with the use of a number of spectroscopic techniques and XRD crystallography. Several of the novel compounds showed intensive fluorescence in the visible region, comparable to that of known coumarin-based fluorescence standards. Moreover, the new compounds were tested as potential antineurodegenerative agents via their ability to act as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors. Compared to the commercial standards, only a few compounds demonstrated moderate AChE and BuChE activities. Moreover, the novel derivatives were tested for their antimicrobial activity against a panel of pathogenic bacterial and fungal species. Their lack of activity and toxicity across a broad range of biochemical assays, together with the exceptional emission of some hybrid molecules, highlights the possible use of a number of the novel hybrids as potential fluorescence standards or fluorescence imaging agents.


Subject(s)
Anti-Infective Agents , Thiadiazoles , Acetylcholinesterase/metabolism , Anti-Infective Agents/pharmacology , Butyrylcholinesterase/metabolism , Cholinesterase Inhibitors/chemistry , Cholinesterase Inhibitors/pharmacology , Coumarins/chemistry , Coumarins/pharmacology , Molecular Docking Simulation , Molecular Structure , Spectrum Analysis , Structure-Activity Relationship , Thiadiazoles/pharmacology
3.
Molecules ; 27(3)2022 Jan 22.
Article in English | MEDLINE | ID: mdl-35163989

ABSTRACT

Nine samples of ethanolic extracts of poplar-type propolis (EEP) originated from South-Eastern Poland were analyzed in terms of the diversity of the flora around the apiary. The mineral composition, antioxidant properties, polyphenolic profile (HPTLC), and main polyphenolic constituents (HPLC-DAD) were determined. Only minor differences in chemical composition and antioxidant capacity between tested EEPs were found regardless of their botanical origin. However, the biological activity of the EEPs was more diversified. The tested EEPs showed stronger antibacterial activity against Gram-negative bacteria (Escherichia coli) compared to Gram-positive bacteria (Staphylococcus aureus and Staphylococcus epidermidis). Staphylococci biofilm inhibition occurred as a result of exposure to the action of four out of nine EEPs (P1-P4). Due to the various compositions of individual EEPs, a different MCF-7 cellular response was observed according to inhibition of cells migration and proliferation. Almost every sample inhibited the migration of breast cancer cells at a low concentration (0.04 µg/mL) of propolis. Even at the lowest concentration (0.02 µg/mL), each EEP inhibited the proliferation of MCF-7 cells, however, the level of inhibition varied between samples.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Antioxidants/pharmacology , Breast Neoplasms/drug therapy , Plant Extracts/pharmacology , Propolis/chemistry , Staphylococcus/drug effects , Cell Movement , Cell Proliferation , Female , Humans , MCF-7 Cells
4.
Molecules ; 27(3)2022 Jan 28.
Article in English | MEDLINE | ID: mdl-35164156

ABSTRACT

The article presents the modification of ash wood via surface initiated activators regenerated by electron transfer atom transfer radical polymerization mediated by elemental silver (Ag0 SI-ARGET ATRP) at a diminished catalyst concentration. Ash wood is functionalized with poly(methyl methacrylate) (PMMA) and poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA) to yield wood grafted with PMMA-b-PDMAEMA-Br copolymers with hydrophobic and antibacterial properties. Fourier transform infrared (FT-IR) spectroscopy confirmed the covalent incorporation of functional ATRP initiation sites and polymer chains into the wood structure. The polymerization kinetics was followed by the analysis of the polymer grown in solution from the sacrificial initiator by proton nuclear magnetic resonance (1H NMR) and gel permeation chromatography (GPC). The polymer layer covalently attached to the wood surface was observed by scanning electron microscopy (SEM). The hydrophobic properties of hybrid materials were confirmed by water contact angle measurements. Water and sodium chloride salt aqueous solution uptake tests confirmed a significant improvement in resistance to the absorption of wood samples after modification with polymers. Antibacterial tests revealed that wood-QPDMAEMA-Br, as well as wood-PMMA-b-QPDMAEMA-Br, exhibited higher antibacterial activity against Gram-positive bacteria (Staphylococcus aureus) in comparison with Gram-negative bacteria (Escherichia coli). The paper presents an economic concept with ecological aspects of improving wood properties, which gives great opportunities to use the proposed approach in the production of functional hybrid materials for industry and high quality sports equipment, and in furniture production.

5.
Int J Mol Sci ; 22(18)2021 Sep 08.
Article in English | MEDLINE | ID: mdl-34575894

ABSTRACT

A series of coumarin-thiadiazole hybrids and their corresponding Cu(II) and Zn(II) complexes were synthesized and characterized with the use of spectroscopic techniques. The results obtained indicate that all the coumarin-thiadiazole hybrids act as bidentate chelators of Cu(II) and Zn(II) ions. The complexes isolated differ in their ligand:metal ratio depending on the central metal. In most cases, the Zn(II) complexes are characteristic of a 1:1 ligand:metal ratio, while in the Cu(II) complexes the ligand:metal ratio is 2:1. All compounds were tested as potential antibacterial agents against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacterial strains demonstrating activities notably lower than commercially available antibiotics. The more promising results were obtained from the assessment of antineurodegenerative potency as all compounds showed moderate acetylcholinesterase (AChE) inhibition activity.


Subject(s)
Anti-Infective Agents/chemistry , Cholinesterase Inhibitors/pharmacology , Copper/chemistry , Coumarins/chemistry , Thiadiazoles/chemistry , Zinc/chemistry , Acetylcholinesterase/chemistry , Anti-Bacterial Agents/chemistry , Crystallography, X-Ray , Escherichia coli/drug effects , Ligands , Magnetic Resonance Spectroscopy , Metals , Microbial Sensitivity Tests , Neurodegenerative Diseases/drug therapy , Pseudomonas aeruginosa/drug effects , Schiff Bases/chemistry , Spectrometry, Fluorescence , Spectrophotometry, Atomic , Staphylococcus aureus/drug effects , Staphylococcus epidermidis/drug effects , Thiazoles/chemistry
6.
Cent European J Urol ; 73(3): 300-306, 2020.
Article in English | MEDLINE | ID: mdl-33133657

ABSTRACT

INTRODUCTION: The most common malignant neoplasm of the urinary tract is prostate cancer (PCa), which is a heterogeneous disease, ranging from very slowly developing and slightly benign to progressing, aggressive, metastatic and fatal, even when properly treated. Existing, imperfect diagnostic methods often lead to over-diagnosis and over-treatment of PCa. That is why new, better PCa biomarkers are being developed. MATERIAL AND METHODS: This review summarizes the current results of the most promising and clinically used PCa biomarkers, as well as having the potential to create new diagnostic and prognostic tools, based on the Web of Science (www.apps.webofknowledge.com) and Scopus (www.scopus) databases. com). RESULTS: Limited specificity of the prostate-specific antigen (PSA) test brings a need to develop new and better diagnostic tools. In the last few years, new approaches for providing significantly better biomarkers, an alternative to PSA, have been introduced. Modern biomarkers show improvement in being used as not only a diagnostic procedure, but also for staging, evaluating aggressiveness and managing the therapeutic process. We describe the methods recommended in the diagnosis of PCa and new PCa molecular diagnostics technologies. Individual biomarkers are used in various stages of the PCa diagnostic process, which was presented on the developed diagnostic flowchart describing the role of biomarkers in prostate cancer management. CONCLUSIONS: Given the diverse nature of PCa, one diagnostic test will not answer all questions, so the use of several diagnostic methods will allow physicians to provide patients with better, personalized clinical advice.

7.
Int J Mol Sci ; 21(16)2020 Aug 07.
Article in English | MEDLINE | ID: mdl-32784653

ABSTRACT

Dysregulation of miRNAs has a fundamental role in the initiation, development and progression of prostate cancer (PCa). The potential of miRNA in gene therapy and diagnostic applications is well documented. To further improve miRNAs' ability to distinguish between PCa and benign prostatic hyperplasia (BPH) patients, nine miRNA (-21, -27b, -93, -141, -205, -221, -182, -375 and let-7a) with the highest reported differentiation power were chosen and for the first time used in comparative studies of serum and prostate tissue samples. Spearman correlations and response operating characteristic (ROC) analyses were applied to assess the capability of the miRNAs present in serum to discriminate between PCa and BPH patients. The present study clearly demonstrates that miR-93 and miR-375 could be taken into consideration as single blood-based non-invasive molecules to distinguish PCa from BPH patients. We indicate that these two miRNAs have six common, PCa-related, target genes (CCND2, MAP3K2, MXI1, PAFAH1B1, YOD1, ZFYVE26) that share the molecular function of protein binding (GO:0005515 term). A high diagnostic value of the new serum derived miR-182 (AUC = 0.881, 95% confidence interval, CI = 0.816-0.946, p < 0.0001, sensitivity and specificity were 85% and 79%, respectively) is also described.


Subject(s)
Genes, Neoplasm , MicroRNAs/metabolism , Prostatic Neoplasms/diagnosis , Prostatic Neoplasms/genetics , 3' Untranslated Regions/genetics , Aged , Aged, 80 and over , Binding Sites/genetics , Cyclin D2/genetics , Gene Expression Regulation, Neoplastic , Humans , Male , MicroRNAs/blood , MicroRNAs/genetics , Middle Aged , Neoplasm Invasiveness , Principal Component Analysis , Prostatic Neoplasms/blood , Prostatic Neoplasms/pathology , ROC Curve
8.
Int J Mol Sci ; 21(16)2020 Aug 10.
Article in English | MEDLINE | ID: mdl-32785125

ABSTRACT

Classical synthetic protocols were applied for the isolation of three novel 1,3,4-thiadiazole derivatives which were then complexed with the biologically important Cu(II) and Zn(II) ions. All free ligands and their corresponding complexes were characterized using a number of spectroscopic techniques including Ultraviolet-visible (UV-vis), Fluorescence, Infrared (FT-IR), tandem liquid chromatography-mass (LC-MS), X-ray diffraction (XRD), and Nuclear Magnetic Resonance (NMR) spectroscopy (1H, 13C, HSQC, HMBC). The results obtained are consistent with the formation of dihydrate complexes, in which the chelation of the metal ion occurs via one of the thiadiazole nitrogen atoms and the deprotonated hydroxyl group of the neighboring resorcynyl moiety. The Zn(II) complexes utilize a 1:1 ligand-metal ratio, while in the Cu(II) complexes the ligand-metal ratio is 2:1. Although the antibacterial testing identified moderate activity of the compounds against the tested bacterial strains and additionally modest antioxidant activity, a strong synergistic antibacterial effect against Staphylococcus aureus, using concomitant treatment of thiadiazole derivatives with the commercial antibiotic kanamycin, was observed. The most active thiadiazole derivative demonstrated a minimal inhibitory concentration (MIC) of 500 µg/mL while it was 125 µg/mL in the presence of kanamycin. Moreover, in the presence of few thiadiazole derivatives the MIC value of kanamycin decreased from 0.39 µg/mL to 0.5 µg/mL. The antioxidant activity (IC50) of the most active thiadiazole derivative was determined as 0.13 mM which was nearly three-fold lower compared to that of TROLOX (0.5 mM).


Subject(s)
Anti-Bacterial Agents/pharmacology , Antioxidants/pharmacology , Coordination Complexes/pharmacology , Copper/chemistry , Kanamycin/pharmacology , Thiadiazoles/chemistry , Zinc/chemistry , Chromatography, Liquid , Coordination Complexes/chemical synthesis , Drug Synergism , Ligands , Magnetic Resonance Spectroscopy , Mass Spectrometry , Microbial Sensitivity Tests , Spectroscopy, Fourier Transform Infrared , Staphylococcus aureus/drug effects , X-Ray Diffraction
9.
Molecules ; 25(2)2020 Jan 10.
Article in English | MEDLINE | ID: mdl-31936872

ABSTRACT

One of the key problems of modern infectious disease medicine is the growing number of drug-resistant and multi-drug-resistant bacterial strains. For this reason, many studies are devoted to the search for highly active antimicrobial substances that could be used in therapy against bacterial infections. As it turns out, snake venoms are a rich source of proteins that exert a strong antibacterial effect, and therefore they have become an interesting research material. We analyzed Naja ashei venom for such antibacterial properties, and we found that a specific composition of proteins can act to eliminate individual bacterial cells, as well as the entire biofilm of Staphylococcus epidermidis. In general, we used ion exchange chromatography (IEX) to obtain 10 protein fractions with different levels of complexity, which were then tested against certified and clinical strains of S. epidermidis. One of the fractions (F2) showed exceptional antimicrobial effects both alone and in combination with antibiotics. The protein composition of the obtained fractions was determined using mass spectrometry techniques, indicating a high proportion of phospholipases A2, three-finger toxins, and L-amino acids oxidases in F2 fraction, which are most likely responsible for the unique properties of this fraction. Moreover, we were able to identify a new group of low abundant proteins containing the Ig-like domain that have not been previously described in snake venoms.


Subject(s)
Anti-Bacterial Agents , Biofilms/drug effects , Elapid Venoms , Naja , Staphylococcus epidermidis/physiology , Animals , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Biofilms/growth & development , Elapid Venoms/chemistry , Elapid Venoms/pharmacology
10.
J Contemp Brachytherapy ; 11(6): 541-546, 2019 Dec.
Article in English | MEDLINE | ID: mdl-31969912

ABSTRACT

PURPOSE: Multiparametric magnetic resonance imaging (mpMRI) is an evolving non-invasive imaging modality that increases the accurate localization of prostate cancer (PCa) at the time of MRI targeted biopsy, enhancing clinical risk assessment, and improving the ability to appropriately counsel patients regarding therapy. MATERIAL AND METHODS: A total of forty patients with prostate-specific antigen (PSA), mpMRI and Gleason score (based on MRI template-guided cognitive biopsy) results were analyzed in this study, with eight patients (20%) diagnosed with PCa. The mpMRI was performed to facilitate the decision to perform prostate biopsy. Spearman's coefficient analysis was used to evaluate the relationships between characteristics. Diagnostic performance was assessed measuring the area under the curve (AUC) of the receiver operating characteristic (ROC) analysis. Diagnostic accuracy, sensitivity, and specificity were determined using the best cut-off on each ROC. RESULTS: Out of all the study group, 55% of patients were subjected to primary biopsy and 45% were directed to repeated TRUS-Bx with the suspicion of prostate cancer. Forty suspected lesions on MRI images were identified with 5% of PI-RADS 1, 17.5% of PI-RADS 2, 32.5% of PI-RADS 3, 27.5% of PI-RADS 4 (27.5%) and 17.5% of PI-RADS 5. The highest correlation was observed for mpMRI results and Gleason score with Spearman's coefficient equal to 0.41 (95% CI: 0.104-0.646). ROC analysis revealed that mpMRI discriminates between directing the patients for prostate biopsy or active surveillance with AUC = 0.771 (0.117, 95% CI: 0.542-1.001). CONCLUSIONS: Introducing pre-biopsy mpMRI into our contemporary PCa diagnosis pathway increased the diagnostic yield of transrectal biopsy by increasing the prostate cancer detection. This enabled the introduction of clinically significant prostate cancer (csPCa) treatment. mpMRI application also allowed biopsy to be avoided among patients with no csPCa.

11.
Int Urol Nephrol ; 50(9): 1619-1626, 2018 Sep.
Article in English | MEDLINE | ID: mdl-30014459

ABSTRACT

PURPOSE: Prostate cancer (PCa) is a common tumor disease in western countries and a leading cause of cancer-driven mortality in men. Current methods for prostate cancer detection, like prostate-specific antigen screening, lead to significant overtreatment. The purpose of the study was to analyze circulating microRNAs in serum as non-invasive biomarkers in patients with diagnosis of prostate cancer and healthy individuals. METHODS: This preliminary study included a population of 20 patients with mean age of 68.6 years and mean PSA of 21.3 ng/ml. Eight healthy patients were used as control. MiRNAs were quantified in the total RNA fraction extracted from serum and levels of five microRNAs (miR-106b, miR-141, miR-21, mir-34a, and miR-375) were quantified by RT-qPCR. Statistical analyses evaluated correlation between clinicopathological data and miRNAs expression levels. RESULTS: Relative expression ratios of miR-106b, miR-141-3p, miR-21, and miR-375 were significantly increased (1.8-, 1.9-, 2.4-, and 2.6-fold, respectively) in the PCa group compared to healthy control. Using receiver operating characteristics, the highest area under the curve equal to 0.906 was obtained for miR-357 and indicates a very good diagnostic properties of this biomarker. We found expression level of mir-34a not related with PCa. CONCLUSIONS: Our results support previous findings on the possibility of discriminating prostate cancer patients from healthy controls by detecting miRNA (miR-141-3p, miR-21, and miR-375). Further insights into miRNA abundance and characteristics are necessary to validate the panel of miRNA as surrogate markers in diagnosis of prostate cancer.


Subject(s)
MicroRNAs/blood , Prostatic Neoplasms/blood , Prostatic Neoplasms/diagnosis , Aged , Area Under Curve , Biomarkers, Tumor/blood , Case-Control Studies , Humans , Male , MicroRNAs/genetics , Middle Aged , Prostatic Neoplasms/genetics , ROC Curve , Transcriptome
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