•Four targeting fluorescent 5-substituted-benzothiazole conjugates (3a, 3b, 6a, and 6b) were synthesized.•The photophysical characteristics of the synthesized conjugates, as well as measurements of ...absorbance and fluorescence maxima in diverse organic solvents.•The conjugates' cytotoxicity was evaluated across different anticancer cell lines.•The inhibitory activity of these conjugates against VEGFR-2 was assessed using an antiphosphotyrosine antibody.•The synthesized 5-substituted-benzothiazole conjugates 3a, 3b, and 6a were stimulated using molecular docking.•The ADME study was performed and showed that conjugates 3b and 6b exhibited enhanced lipophilicity and reduced solubility.
Four targeting fluorescent 2-(N,N-dimethyl/diphenyl-aminophenyl)-5-substituted-benzothiazole conjugates 3a, 3b, 6a and 6b were synthesized. Insight into the photophysical characteristics of the synthesized conjugates, as well as measurements of absorbance and fluorescence maxima in diverse organic solvents, showed conjugate 3b ranged from 302 to 324 nm, whereas the fluorescence maxima ranged from 312 nm (CH2Cl2) to 465 nm. The conjugates' cytotoxicity was evaluated across anticancer cell lines, and the inhibitory action of these conjugates against VEGFR-2 was assessed using an antiphosphotyrosine antibody, with 3b and 6b conjugates showing potent cytotoxic activity against MCF-7 cells with IC50 values of 7.06 ± 0.29 and 8.82 ± 0.37 μM, respectively. Meanwhile, conjugate 6b had the greatest potency of the conjugates for VEGFR-2 inhibition, with an IC50 of 0.23 ± 0.20 μM. Though the binding’s interactions were stimulated using molecular docking, A higher binding score and a variety of interaction types for conjugate 3b, temporarily, indicated a stronger interaction. Moreover, the ADME study was performed and showed that conjugates 3b and 6b exhibited enhanced lipophilicity and reduced solubility, which may influence their pharmacokinetic behavior.
The AcPase exhibits a specific activity of 31.32 U/mg of protein with a 728-fold purification, and the yield of the enzyme is raised to 3.15 %. The Zn2+-dependent AcPase showed a purification factor ...of 1.34 specific activity of 14 U/mg of proteins and a total recovery of 5.14. The SDS-PAGE showed a single band corresponding to a molecular weight of 18 kDa of AcPase and 29 kDa of Zn2+-dependent AcPase. The AcPase enzyme has shown a wide range of substrate specificity for p-NPP, phenyl phosphate and FMN, while in the case of ZnAcPase α and β-Naphthyl phosphate and p-NPP were proved to be superior substrates. The divalent metal ions like Mg2+, Mn2+, and Ca2+ increased the activity, while other substrates decreased the enzyme activity. The Km (0.14 mM) and Vmax (21 μmol/min/mg) values of AcPase were higher than those of Zn2+-AcPase (Km = 0.5 mM; Vmax = 9.7 μmol/min/mg). The Zn2+ ions activate the Zn2+-AcPase while Fe3+, Al3+, Pb2+, and Hg2+ showed inhibition on enzyme activity. Molybdate, vanadate and phosphate were found to be competitive inhibitors of AcPase with Ki values 316 μM, 185 μM, and 1.6 mM, while in Zn2+-AcPase tartrate and phosphate also showed competitive inhibition with Ki values 3 mM and 0.5 mM respectively.
•A novel Acid phosphatases and zinc dependent acid phosphatases were purified from chicken’s brain.•AcPase and zinc-dependent AcPase showed a single protein band on SDS-PAGE corresponding to molecular weights of about 18 kDa and 29 kDa.•The Acid phosphatase and zinc dependent AcPases were optimally active at 45 °C pH 6.0.•The Km of zinc-dependent AcPase and AcPase has been determined to be 0.5 mM and 0.14 mM, respectively. The Vmax 7 μmol/min/mg of protein and 21 μmol/min/mg of protein.
Dietary polyphenols are protective for chronic diseases. Their blood transport has not been well investigated. This work examines multiple classes of polyphenols and their interactions with albumin, ...lipoproteins, and red blood cell (RBC) compartments using four models and determines the % polyphenol in each compartment studied. The RBC alone model showed a dose–response polyphenol association with RBCs. A blood model with flavanones determined the % polyphenol that was inside RBCs and bound to the surface using a new albumin washing procedure. It was shown that RBCs can methylate flavanones. The whole blood model separated the polyphenol into four compartments with the aid of affinity chromatography. More polyphenols were found with albumin and lipoproteins (high-density lipoproteins and low-density lipoproteins) than with RBCs. In the plasma model, the polyphenols associated almost equally between lipoproteins and albumin. RBCs and lipoproteins are shown to be important reservoirs and transporters of polyphenols in blood.
•Synthesis of a new magnesium porphyrin derivative (I).•X-ray molecular structure of (I) showing Hydrogen bands.•Hirshfeld surface of porphyrins complex.•Biological Activity of porphyrin.•Molecular ...docking studies of a magnesium (II) porphyrin.
A new bioactive material of magnesium porphyrin complex Mg(TPP)(H2O)2.2/3(2.2.2).1/3(Bz) (I), (TPP = meso-‑tetraphenylporphyrinato and (2.2.2) = cryptand, and Bz is benzene (C6H6)) has been synthesized and characterized by Single-crystal X-ray diffraction (SCXRD). The title compound crystallizes in trigonal crystal system in space group P-3. The magnesium ion is coordinated to four nitrogen atoms of the porphyrin core and two oxygen atoms of the axial ligands. The crystal packing is stabilized by inter-and intramolecular hydrogen bonds, and by weak C–H…Cg π interactions leading to a bi-dimensional network. In order to confirm the crystal structure, the photophysical properties have been evaluated by infrared (IR), proton nuclear magnetic resonance 1H NMR and UV–Vis spectroscopy. UV–Visible absorption spectrum of complex (I) displayed a red shifted Soret (429 nm) and Q (567 and 609 nm) bands due to the extended conjugation. The IR, and 1H NMR confirm the crystal structure. Finally, bioactivity investigations revealed that free porphyrin H2TPP, Mg(TPP) and complex (I) could be used as potential novel significant antibacterial agents. The docking of the free base porphyrins, metallated and the complex (I), in the active sites of bacterial proteins EEscherichia coli (1ECL) and Aspergillus Niger (3K4P) was carried out to detect the degree of antibacterial activity of recognition.
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•Synthesis of a new porphyrin derivative.•Cobalt (II) picket fence porphyrin.•MS spectroscopy.•X-ray molecular structures.•CH⋯Cg type π interactions.•Biological activity of porphyrin.
In this work, ...we describe the synthesis, spectroscopic and structural properties of the new compound bis(pyridine)(α, β, α, β-tetrakis (o-pivalamidophenyl) porphyrinato) cobalt (II) CoII(TpivPP)(py)2 (I). The molecular structure determined by X-rays of the compound shows that this species is a six-coordinate cobalt (II) metalloporphyrin. The UV–visible spectrum of (I) shows that the value of the Soret band (415 nm) is shifted towards the green with respect to the free base H2TpivPP while the λmax values of the Q band are 530 and 563 nm. The proton NMR spectrum of (I) clearly indicated that these derivatives are cobalt(II) paramagnetic porphyrin complexes. Zones of inhibition are studied against the bacterial strains Escherichia coli, Streptococcus pneumoniae and the fungal strains Aspergillus niger, Aspergillus fumigatus. The reported results show that cobalt porphyrin has better antibacterial and antifungal efficacy against gram-positive and gram-negative strains of bacteria as well as fungal strains.
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We have synthesized and characterized porphyrin structures by UV–visible, IR and fluorescence spectroscopy studies and single crystal XRD analysis; H2(TPP) (I) ...(meso-tetraphenylporphyrin), Mg(TPP)(DMF) (II); (DMF: dimethylformamide) and Mg(TPP)(H2O)0.2(4-CNpy) (III); (4-CNpy: 4-Cyanopyridine). The crystal packing of the porphyrin structures is stabilized by intermolecular hydrogen bonds and by intermolecular CH⋯Cg π interactions where Cg is the centroid of the phenyl and pyrrole rings. UV–Vis spectroscopic data confirmed the creation of Mg-meso-porphyrin complexes by the red-shifted Soret bands for our derivatives compared to the free-base porphyrin. The optical gap energy values of (I), (II) and (III) are 1.92, 2.07 and 2.00 eV. Gram-positive and Gram-negative bacteria were tested against free porphyrin (I), metallated porphyrin (II) and complex (III). The results show that the magnesium porphyrin derivative is highly effective compared to H2TPP free-base porphyrins and metallated porphyrin Mg(TPP) and has higher inhibition character against the tested bacteria. The molecular docking of the complex (III), in the active sites of bacterial proteins was carried out to detect the degree of antibacterial activity of recognition.
Extraction of green tea catechins and antioxidant activity of tea extracts:
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•Extraction of catechins from green tea leaves by microwave-assisted technique.•Effect of solvents, ...microwave power, and extraction time on the catechins yield.•Quantitative and qualitative analysis of the individual catechins by HPLC.•Antioxidant activity of the various green tea infusions extracted at different conditions.
This work aimed to develop a microwave-assisted extraction (MAE) method for green tea to efficiently extract catechins. Green tea was extracted with various solvent types, including water, 50 % ethanol–water, and 50 % acetonitrile–water, with a controlled microwave power of 250–800 W for 2–8 min of irradiation at a fixed temperature of 80 °C. Caffeine from the crude extract was separated by partitioning with chloroform, and catechins were separated using ethyl acetate. The HPLC results demonstrated that maximum yield of catechins (24.7 mg/g for EGC; 8.2 mg/g for C; 14.3 mg/g for EC; 39.6 mg/g for EGCG 14.5 mg/g for GCG and 21.7 mg/g DW tea for ECG) was obtained with a 50 % ethanol–water system at 500 W power within 6 min of treatment. The limits of detection and quantification were in the range of 0.15–0.56 and 0.30–1.23 µg mL−1, respectively. Satisfactory recoveries (0.8–2.7 %) and the intra-day and inter-day precisions (RSD% 1.63–3.84 % and 0.76 %–1.95 %, respectively) were found. The catechin components discovered in green tea included relatively high quantities of epicatechin gallate (ECG), (epigallocatechin gallate (EGCG), and epigallocatechin (EGC). The DPPH assay assessed the antioxidant activity of the various infusions prepared at different parameters. The results demonstrated high antioxidant activity (78.4–94.0 %) for the infusions extracted with the ethanol–water mixture at 500 W microwave power within 6 min of treatment, followed by the acetonitrile–water mixture. The antioxidant potentials of the extracts showed a linear correlation with the catechin contents in the extracts.
β-Galactosidase was isolated from Ranunculus arvensis seeds using DEAE-cellulose, Sephadex G-100, and Con A sepharose-4B chromatography. The enzyme was purified to electrophoretic homogeneity with a ...specific activity of 50 U/mg of protein and a yield of 7.1%. The molecular mass of the isolated β-galactosidase, as estimated by SDS-PAGE, was 18 kDa, indicating that it was a monomeric form The purified β-galactosidase has a glycoproteinic nature when applied to Con-A-Sepharose-4B chromatography. An activation energy (Ea) of 11 kcal/mol of lactose, pH 5.0, and 50 °C were found to be the optimum parameters to purify β-galactosidase from R. arvensis seeds. The residual activity test was carried at 55–75 °C, allowing calculating the half-lives of 533–48 min, enthalpy (ΔH° = 110.38–110.21 kJ/mol), free energy (ΔG° = 109.88–109.77 kJ/mol), and entropy (ΔS° = 1.52–1.26 J/mol·K). The β-galactosidase produced from this species is better than the previously described enzyme due to its kinetic and thermodynamic properties, and it could be used in various industrial applications. Purified β-galactosidase, when incubated with high lactose concentration, showed transgalactosylation activity, leading to trisaccharides as a major product of total galactooligosaccharide (GOS). Therefore, the purified β-galactosidase could be used as a potential alternative in the food industry and would be further explained for trisaccharide synthesis.
Ranunculus arvensis β-galactosidase: insights into its purification, kinetics, thermodynamic characterization, and trisaccharide synthesis. Display omitted
•β-Galactosidase from Ranunculus arvensis was purified 185 fold with 7.1% yield.•The enzyme was found thermostable upto 50 °C.•The maximum turnover Vmax for ortho-NPG is 96 μmol/min/mg of protein and a Km of 0.4 mM.•β-Galactosidase is used for the synthesis of galacto-oligosaccharides.•It is a highly thermophilic enzyme that could be suitable for biotechnological applications.
Summary Background A case control study to better characterize the clinical features, laboratory, and radiological abnormalities associated with MERS-CoV infection in order to help with early ...identification of this syndrome from other respiratory infections. Methods Eighty patients admitted to a hospital in Riyadh, diagnosed with MERS-CoV infection based on RT-PCR were matched on age, sex, and the presence of a co-morbid condition on a basis of 1:2 to other patients admitted with respiratory symptoms and tested negative for MERS-CoV on RT-PCR. Results None of the reported MERS-CoV presenting symptoms was significantly associated with being infected with MERS-CoV. On the other hand, WBC count was significantly lower in patients with confirmed MERS-CoV infection (median 5.7 vs 9.3, P: 0.0004). Neutrophil count was as well significantly lower in MERS-CoV patients (median 3.7 vs 6.7, P: 0.0001). Both AST, and ALT values were significantly higher in MERS-CoV infected group (AST median 42 vs 36, P: 0.03, and ALT median 33 vs 28, P: 0.003). Overall our MERS-CoV mortality rate was(10%) below the national figure of (40%). Conclusions None of the presenting symptoms are specific for MERS-CoV infection. And out of all the investigations WBC, neutrophil counts, AST and ALT values have some predictive utility.
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