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•New coumarine derivatives and palladium(II) complexes were synthesized.•Characterized by microanalysis, infrared, 1H and 13C NMR spectroscopy and DFT methods.•In vitro antitumor ...activity for ligands and complexes is investigated.•In vitro antimicrobial activity for ligands and complexes is investigated.•Molecular docking studies with epidermal growth factor receptor (EGFR).
In the present manuscript, palladium(II) complexes (C1, C2) with newly synthesized coumarine ligands 3-(1-((3-chlorophenyl)amino)ethylidene)-chroman-2,4-dione (L1) and 3-(1-((4-chlorophenyl)amino)ethylidene)-chroman-2,4-dione (L2) were prepared and structurally characterized by spectroscopic techniques (FT-IR, 1H NMR, 13C NMR) in combination with elemental analysis and theoretical methods (DFT). The structures of all compounds were fully optimized using the B3LYP-D3BJ theoretical method. Cytotoxic activity of investigated compounds was tested against two cells lines (human colorectal carcinoma, HCT-116, and human fibroblast lung MRC-5), while their antimicrobial activity was screened against nine strains of pathogenic bacteria, five mould species and two yeast species. Unfortunately, their cytotoxic and antibacterial activities were weak. Docking studies for all compounds with epidermal growth factor receptor (EGFR) were performed. It was found that hydrophobic interactions that include chlorine atom have somewhat lower values of the pairwise interaction energies compared to the purely hydrophobic interactions. In addition, it was found the chlorine atom in the para position contributes to the slightly higher binding free energy and lower values of constant of inhibition.
Objective
The objective of this study was to evaluate the probiotic potential as well as the ability of adhesion and aggregation of natural and autochthonous lactic acid bacteria, isolated from ...traditionally made cheese.
Results
Lactic acid bacteria from natural food sources can be promising probiotic candidates and they can be used in natural food preservation or like starter cultures. Tested autochthonous isolates showed tolerance to the simulated gastrointestinal condition as well as the sensitivity to clinically relevant antibiotics, especially to ampicillin (MIC at 0.195 μg mL
−1
for lactobacilli and from 0.195 to 3.125 μg mL
−1
for lactococci). Among isolates, the highest percentage of adhesion was detected with chloroform, while the adhesion ability of selected isolates to pig intestinal epithelium was in the correlation with the results of adhesion ability with solvents. The auto-aggregation ability of isolates was demonstrated, while co-aggregation with
Escherichia coli
was strain specific.
Conclusion
The results indicated the potential probiotic properties of the isolates and give evidence for further investigation and potential application in the dairy industry.
Objective
The objectives of this research project were isolation, identification, and evaluation of the safety aspect and probiotics properties of 21
Enterococcus faecium
strains isolated from ...sausages originated from southeastern Serbia.
Results
Analyzed
E. faecium
isolates showed tolerance to simulated gastrointestinal conditions. All the examined isolates grew well on media with 0.1% and 0.2% of phenol. None of the tested isolates were histamine-producers, while the synthesis of tyramine was observed for
E. faecium
sk8-1 and sk8-17. Full resistance to antibiotics was not observed for any examined isolate of
E. faecium
(penicillin, amoxicillin, and ofloxacin showed the effect on all tested isolates). An inhibition zone against examined pathogens was exhibited by all strains, with the largest inhibition zone against
Pseudomonas
spp.,
Proteus
spp. and
E. coli
(12–30 mm/MIC values ranged from 0.5 to 12 mg mL
−1
).
Conclusion
The results indicated that
E. faecium
isolates from spontaneously fermented sausage showed a potential for further investigation and possible application as probiotics.
Trapa natans L. (water chestnut or water caltrop) is a widespread aquatic plant, which has been cultivated for food and traditional medicine since ancient times. Pharmacological studies showed that ...water chestnut exhibits the wide range of biological activities, such as antimicrobial, antioxidative, analgesic, anti-inflammatory, as well as antiulcer.
Evaluation of anti-virulence potential and toxicity of T. natans methanol (TnM), acetone (TnA) and ethyl acetate (TnEA) leaf extracts.
The anti-quorum sensing activity of Tn extracts was addressed by measuring their effects on biofilm formation, swarming motility and pyocyanin and elastase production in Pseudomonas aeruginosa. Specific P. aeruginosa biosensors were used to identify which of the signaling pathways were affected. The lethal and developmental toxicity of extracts were addressed in vivo using the zebrafish (Danio rerio) model system. The phenolic composition of T. natans leafs extracts was analyzed by a linear ion trap-OrbiTrap hybrid mass spectrometer (LTQ OrbiTrapMS) and UHPLC system configured with a diode array detector (DAD) hyphenated with the triple quadrupole mass spectrometer.
Subinhibitory concentrations of Tn leaf extracts (0.2 MIC) inhibited pyocyanin and elastase production up to 50% and 60%, respectively, and reduced swarming zones, comparing to non-treated P. aeruginosa. TnA inhibited biofilm formation by 15%, TnM showed a stimulatory effect on biofilm formation up to 20%, while TnEA showed no effect. The bioactive concentrations of TnM and TnA were not toxic in the zebrafish model system. Twenty-two phenolic compounds were tentatively identified in TnM, where thirteen of them were identified in T. natans for the first time. Tn extracts, as well as their major components, ellagic and ferulic acids, demonstrated the ability to interfere with P. aeruginosa Las and PQS signaling pathways.
This study demonstrates anti-virulence potential of Tn leaf extracts against medically important pathogen P. aeruginosa and confirms the ethnopharmacological application of this plant against microbial infections.
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In this research paper, the total phenols (TP), flavonoids (TF), and tannins (TT) content in the acetone and ethyl acetate extracts of Najas marina L. and the identification and quantification of ...phenolic acids and flavonoids from the ethyl acetate extract were performed. Antioxidant, antimicrobial, and antibiofilm properties of the mentioned extracts were investigated in vitro. The genotoxic potential was analyzed in cultured human peripheral blood lymphocytes (PBL). The TP and TF content was higher in the ethyl acetate extract, dominated by quercetin (172.4 µg mg-1) and ferulic acid (22.74 µg mg-1), while the TT content was slightly higher in the acetone extract. Both extracts tested showed limited antioxidant effects compared to ascorbic acid. The strongest antibacterial activity was observed with Gram-positive bacteria, particularly Staphylococcus aureus (MIC and MMC at 0.31 mg ml-1) and S. aureus ATCC 25923 (MIC at <0.02 mg ml-1), while antifungal activity was limited. Both extracts tested showed better activity on preformed biofilms. Acetone extract had no genotoxic activity but showed significant genoprotective activity against mitomycin C-induced DNA damage in cultured PBLs. Results of our research demonstrate the potential for the development of plant-based antibacterial and biofilm agents.
A series of new 3d metal complexes with 5-chloro-quinolin-8-ol (ClQ), Mn(ClQ)2 (1), Fe(ClQ)3 (2), Co(ClQ)2(H2O)2 (3), Ni(ClQ)2(H2O)2 (4), Cu(ClQ)2 (5), Zn(ClQ)2(H2O)2 (6), Mn(ClQ)3·DMF (7) and ...Co(ClQ)3·DMF·(EtOH)0.35 (8) (DMF=N,N-dimethylformamide), has been synthesized and characterized by elemental analysis, IR spectroscopy and TG–DTA thermal analysis. X-ray structure analysis of 7 and 8 revealed that these molecular complexes contain three chelate ClQ molecules coordinated to the central atoms in a deformed octahedral geometry and free space between the complex units is filled by solvated DMF and ethanol molecules. Antimicrobial activity of 1–6 was tested by determining the minimum inhibitory concentration and minimum microbicidal concentration against 12 strains of bacteria and 5 strains of fungi. The intensity of antimicrobial action varies depending on the group of microorganism and can be sorted: 1>ClQ>6>3/4>2>5. Complexes 1–6 exhibit high cytotoxic activity against MDA-MB, HCT-116 and A549 cancer cell lines. Among them, complex 2 is significantly more cytotoxic against MDA-MB cells than cisplatin at all tested concentrations and is not cytotoxic against control mesenchymal stem cells indicating that this complex seems to be a good candidate for future pharmacological evaluation. Interaction of 1–6 with DNA was investigated using UV–VIS spectroscopy, fluorescence spectroscopy and agarose gel electrophoresis. The binding studies indicate that 1–6 can interact with CT-DNA through intercalation; complex 2 has the highest binding affinity. Moreover, complexes 1–6 inhibit the catalytic activity of topoisomerase I.
M(ClQ)2 (M=Mn (1), Cu (5)), Fe(ClQ)3 (2), M(ClQ)2(H2O)2 (M=Co (3), Ni (4), Zn (6)), Mn(ClQ)3·DMF (7) and Co(ClQ)3·DMF·(EtOH)0.35 (8) (ClQ=5-chloro-quinolin-8-ol) were characterized by IR/UV–VIS spectroscopy, thermal analysis, crystallography (7, 8) and biological testing (1–6, ClQ) (antimicrobial activity, cytotoxicity, DNA binding, topoisomerase I inhibition). Display omitted
•Eight 3d complexes with 5-chloro-quinolin-8-ol (ClQ) are characterized.•Complexes interact with DNA by intercalative binding mode.•Complexes target topoisomerase I as mildly effective topoisomerase inhibitors.•Fe(ClQ)3 complex is highly active against human breast MDA-MB cancer cell line.•Fe(ClQ)3 complex is not cytotoxic against control mesenchymal stem cells.
The present work was undertaken to determine the total phenol, flavonoid and tannin content in five extracts of Origanum vulgare growing wild in southwest Serbia as well as to evaluate antioxidant ...and antimicrobial activity towards 29 strains of human pathogenic and food spoilage bacteria and fungi. In order to define a chemotype of this O. vulgare, chemical composition of essential oil was determined. The major compounds were: sabinene, terpinen-4-ol, 1.8 cineole, γ-terpinene and caryophyllene oxide. The concentrations of total phenols were examined using Folin–Ciocalteu reagent and the obtained values ranged from 84.5 to 235 mg GA/g. By using aluminium chloride method, the concentrations of flavonoids were obtained and the values ranged from 57.1 to 132 mg RU/g. In determining the amount of tannins, the method with butanol–HCl reagent was used and the obtained values were between 1.25 and 4.02 mg CCh/g. Antioxidant activity was evaluated by measuring the scavenging capacity of extracts on DPPH. Tested extracts expressed strong scavenger activity with IC50 values between 34.5 and 86 μg/ml. The ethanol extract was the most active. The strongest antibacterial activity, determined by microdilution method, was detected on G+ bacteria such as Bacillus species and Staphylococcus aureus, obtaining minimal inhibitory concentration (MIC) 0.16 mg/ml while antifungal activity was moderate with MICs between 2.5 and 20 mg/mL.
•We determined chemical composition of essential oils.•We examined five different extracts of aerial parts from oregano.•All extracts showed significant antimicrobial effect.•Good antioxidative activity.
Melilotus albus Medic. and Dorycnium herbaceum Vill. (Fabaceae) acetone, ethyl acetate, and ethanol extracts were investigated for their in vitro antimicrobial, antibiofilm, and antioxidant activity ...with quantification of phenolic compound contents. In general, D. herbaceum extracts showed better antibacterial and antioxidant activity than M. albus extracts. Bacteria Bacillus subtilis, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa, and Proteus mirabilis were the most susceptible with the minimum inhibitory concentrations (MICs), determined by microdilution method, between 1.25–10 mg/mL. Antifungal activity was lower with the detectable MICs at 10 mg/mL and 20 mg/mL. The plant extracts, using the crystal violet assay, inhibit P. aeruginosa biofilm formation in concentration range from 5 mg/mL to 20 mg/mL whereas the effect on mature bacterial biofilm was lower. The antioxidant activity was evaluated using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radicals scavenging and reducing power model systems. The intensity of DPPH radicals scavenging activity, expressed as half maximal effective concentration (EC50) values, was from 84.33 μg/mL to >1000 μg/mL. The extracts demonstrated reduced power in a concentration-dependent manner, with ethanol extract as the most active. The total phenols, flavonoids, and proanthocyanidins were determined spectrophotometrically while total extractable tannins were obtained by precipitation method. The phenolic compounds showed differences in their total contents depending on solvents polarities and plant species. Although the plants M. albus and D. herbaceum have not yet been fully explored, these results contribute better understanding of their biotic properties and potential application as antimicrobial and antioxidant agents.
Starting from well-defined NH2(CH3)2PdCl2(XQ) complexes, coordination compounds of general formula CatPdCl2(XQ) have been prepared by cationic exchange of NH2(CH3)2+ and Cat cations, where XQ are ...biologically active halogen derivatives of quinolin-8-ol (5-chloro-7-iodo-quinolin-8-ol (CQ), 5,7-dibromo-quinolin-8-ol (dBrQ) and 5,7-dichloro-quinolin-8-ol (dClQ)) and Cat is K+ or Cs+. The cation exchange of all prepared complexes, KPdCl2(CQ) (1), KPdCl2(dClQ) (2), KPdCl2(dBrQ) (3), CsPdCl2(CQ) (4), CsPdCl2(dClQ) (5) and CsPdCl2(dBrQ) (6) was approved using IR spectroscopy, their structures in DMSO solution were elucidated by one- and two-dimensional NMR experiments, whereas their stability in solution was verified by UV–VIS spectroscopy. Interaction of complexes to ctDNA was investigated using UV–VIS and fluorescence emission spectroscopy. The minimum inhibitory concentration and the minimum microbicidal concentration values were detected against 15 bacterial strains and 4 yeast strains to examine the antimicrobial activity for the complexes. The in vitro antitumor properties of the complexes were studied by testing the complexes on leukemic cell line L1210, ovarian cancer cell line A2780 and non-cancerous cell line HEK293. The majority of the prepared compounds exhibited moderate antimicrobial and very high cytotoxic activity.
Six new CatPdCl2(XQ) complexes (Cat=K+ or Cs+, XQ=biologically active halogen derivatives of quinolin-8-ol) were synthesized by cationic exchange between NH2(CH3)2+ and alkali metals cations. All prepared complexes were characterized by IR, UV–VIS, NMR, elemental and thermal analyses, and their interaction to DNA, antimicrobial and antitumor activities were evaluated. Display omitted
•Six new ionic Pd(II) complexes with halogen derivatives of quinolin-8-ol were prepared.•Complexes interact with DNA by intercalative binding mode.•Antimicrobial activity of complexes was tested against 19 strains of microorganisms.•Antitumor properties were studied on three cancerous and non-cancerous cell lines.•Complexes are selective cytotoxic against leukemic cell line L1210.
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•New coumarine derivatives and palladium(II) complexes were synthesized.•Characterized by microanalysis, infrared, 1H and 13C NMR spectroscopy.•Monocrystal X-ray structural analysis ...and DFT calculations.•Antimicrobial activity for ligands and complexes is investigated.
The five coumarin derivatives 3-(1-(2-hydroxypropylamino)ethylidene)-chroman-2,4-dione (L1), 3-(1-(phenylamino)ethylidene)-chroman-2,4-dione (L2), 3-(1-(o-toluidino)ethylidene)-chroman-2,4-dione (L3), 3-(1-(m-toluidino)ethylidene)-chroman-2,4-dione (L4), 3-(1-(2-mercaptoethylamino)ethylidene)-chroman-2,4-dione (L5) and its corresponding complexes 3-(1-(2-hydroxypropylamino)-ethylidene)-chroman-2,4-dione-palladium(II) (C1), 3-(1-(phenylamino)-ethylidene)-chroman-2,4-dione-palladium(II) (C2), 3-(1-(o-toluidino)-ethylidene)-chroman-2,4-dione-palladium(II) (C3), 3-(1-(m-toluidino)ethylidene)-chroman-2,4-dione-palladium(II) (C4), 3-(1-(2-mercaptoethylamino)ethylidene)-chroman-2,4-dione-palladium(II) (C5), were synthesized and characterized with microanalysis, infrared, 1H and 13C NMR spectroscopy. The proposed structures of ligands L3 and L4 were confirmed on the basis of the X-ray structural study. The ligands and their complexes were tested for their in vitro antimicrobial activity against 17 species of bacteria and fungi. Testing is performed by the microdilution method, with the minimum inhibitory concentration (MIC) and the minimum microbicidal concentration (MMC) being determined.
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