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In this study, a novel fluorescent sensor was created on the basis of the Schiff base reaction, where the covalent attachment was achieved by condensation of NH2‐Al‐MOF and 2‐hydroxyacetophenone ligand. The condensation was verified by Fourier transform infrared (FT‐IR), X‐ray diffraction spectrometry (XRD), Brunauer–Emmett–Teller (BET), in addition to (XPS) analysis. Studied fluorescence characteristics in optimum conditions and the results were great, especially the low limit of detection (LOD) and the limit of quantification (LOQ). By examining the impact of some interfering ions, the selectivity of the 2HA = N‐MIL‐53(Al) sensor was determined. The novel sensor was used to measure the presence of As3+ ions in a real water sample. All the data that were examined suggested that the 2HA = N‐MIL‐53(Al) sensor offered excellent detection efficiency while being selective, sensitive, quick, direct, and effective in sensing and detecting As3+ ions in an aqueous solution. [ABSTRACT FROM AUTHOR]

Chemical sensor based on NH2‐UiO‐66(Zr) have been developed for rapid detection of Cd2+ and Hg2+ ions. The developed 2HA = N‐UiO‐66(Zr) sensor was prepared by the condensation of the Zr‐metal–organic framework (MOF) with 2‐hydroxyacetophenone. The NH2‐UiO‐66(Zr) and 2HA = N‐UiO‐66(Zr) sensor were characterized by scanning electron microscopy (SEM), X‐ray diffractometer (XRD), Fourier transform infrared (FT‐IR), X‐ray photoelectron spectroscopy (XPS), and Brunner–Emmet–Teller (BET). The characterization results shown that 2‐hydroxyacetophenone was successfully introduced on the Zr‐based MOF and that the pore structure of 2HA = N‐UiO‐66(Zr) sensor mainly contains mesopores. Many experimental studies have been conducted to find out the optimum conditions for colorimetric and fluorometric determining of the Cd2+ and Hg2+ ions by the 2HA = N‐UiO‐66(Zr) sensor. The response time, for the sensor, that is necessary to achieve a steady spectroscopic signal was less than 30 s. The suggested methods were validated in terms of the lowest limit of detection (LOD), the lowest limit of quantification (LOQ), linearity, and precision according to International Conference on Harmonization (ICH) guidelines. As a result, the 2HA = N‐UiO‐66(Zr) sensor was successfully used to determine Cd2+ and Hg2+ ions in a variety of tap water samples with great sensitivity and selectivity. [ABSTRACT FROM AUTHOR]

Nowadays, quinoline scaffold is among the most vital construction compounds for the development of new drugs. The purpose of this research is to evaluate the anti‐cancer activity of sodium salt of ethyl (E)‐2‐cyano‐3‐(7‐hydroxy‐4‐methyl‐2‐oxoquinoline‐1(2H)‐yl)‐3‐(4‐hydroxyphenyl) acrylate against Ehrlich ascites carcinoma (EAC) cells residing in female mice's peritoneal cavity. The docking study exhibited a favourable interaction between the compound and the receptors 1MOY and 3KJF of osteopontin and caspase 3, respectively. The compound's sodium salt showed potential antioxidant and anti‐cancer effects against Ehrlich ascites carcinoma (EAC) cells in vivo. Herein, the results elucidated that treatment with the compound's sodium salt exerted significant chemopreventive and chemotherapeutic effects, which reduced both EAC cell volume and count. Our results revealed that treatment with the sodium salt of the compound demonstrated a remarkable in vivo apoptotic effect through elevation of the expression of caspase 3 and reduction of osteopontin levels. Histopathological examination confirmed that the compound's sodium salt improved liver and kidney tissues without any apparent adverse effects. [ABSTRACT FROM AUTHOR]

Inflammatory biomarkers provide a minimally invasive means for early detection and specific treatment of metabolic syndrome and related disorders. The objective of this work was to search for inflammatory biomarkers of cardiometabolic risk in obese type 2 diabetics. The study was performed on 165 persons attending the medical outpatient clinic of Ismailia General Hospital. Their mean age was (50.69 ± 10.15) years. They were divided into three groups. The control group was composed of 55 non-obese, non-diabetic healthy volunteers, 32 males and 23 females. Two study groups were included in this study: group 2 was composed of 55 obese, non-diabetic subjects, 25 males and 30 females matched for age and gender. All patients including the control were subjected to clinical history taking, a clinical examination for the measurement of body mass index (BMI). Investigations were carried out for fasting blood glucose, fasting serum insulin, insulin resistance (IR), the lipid profile, lipoprotein band lipoprotein phospholipase A2, and non-high-density lipoprotein cholesterol (non-HDL-C). Urea, albumin and creatinine analysis and liver function tests were performed, and a complete blood count (CBC) was taken. Hemoglobin A1C (HbA1C), serum high-sensitivity C-reactive protein (hs-CRP), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) were tested. There were statistically significant differences among the studied groups in terms of total cholesterol, non-HDL-C, high-density lipoprotein cholesterol (HDL-C), triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), lipoprotein-associated phospholipase A2 and apolipoprotein B. The inflammatory biomarkers hs-CRP, IL-6 and TNF-α were significantly statistically increased in the study groups by (1.62 ± 0.99, 2.32 ± 1.11), (1.73 ± 1.14, 2.53 ± 1.34), and (1.87 ± 1.09, 2.17 ± 0.89) respectively, where p < 0.01. Significant positive correlation was found between Homeostatic Model Assessment (HOMA)-IR, hs-CRP and IL-6. There was a significant positive correlation between non-HDL and hs-CRP, IL-6 and TNF-α and triglycerides and hs-CRP. In conclusion, in this study, CRP, IL-6, and TNF-α were significantly elevated in obese Egyptian type 2 diabetics and were positively correlated with insulin resistance, non-HDL and triglycerides. These inflammatory biomarkers could help in the premature identification of obese type 2 diabetic patients at high cardiometabolic risk. Additionally, these biomarkers are critical for providing prognostics and the validity of future potential anti-inflammatory therapeutic modalities. [ABSTRACT FROM AUTHOR]

The charge-transfer (CT) interactions between the electron donor sulfasalazine (SS) and the acceptors 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), p-chloranil (CHL), picric acid (PA) and iodine have been studied spectrophotometrically in CHCl or CHOH solutions. The formed solid CT complexes were also isolated and characterized through infrared, H-NMR, mass spectra as well as elemental and thermal analysis. The CT complexes were discussed in terms of formation constant (K), molar extinction coefficient (ε), standard free energy (ΔG°), oscillator strength ( f), transition dipole moment (µ), resonance energy (R) and ionization potential (I). The stoichiometry of these complexes was found to be 1:1 molar ratio and having the formulae [(SS)(DDQ)], [(SS)(CHL)], [(SS)(PA)] and [(SS)I]· I, respectively. The charge transfer interaction was successfully applied to the determination of SS drug using mentioned σ and π-acceptors also, the results obtained herein are satisfactory for estimation of SS compound in the pharmaceutical form. Copyright © 2010 John Wiley & Sons, Ltd. The charge-transfer (CT) interactions between the electron donor sulfasalazine (SS) and the acceptors 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), p-chloranil (CHL), picric acid (PA) and iodine have been studied spectrophotometrically in CHCl or CHOH solutions. The formed solid charge-transfer complexes were also isolated and characterized through infrared, H-NMR, mass spectra as well as elemental and thermal analysis. The CT complexes were discussed in terms of formation constant (K), molar extinction coefficient (ε), standard free energy (ΔG°), oscillator strength ( f), transition dipole moment (µ), resonance energy (R) and ionization potential (I). The stoichiometry of these complexes was found to be 1:1 molar ratio and having the formulae [(SS)(DDQ)], [(SS)(CHL)], [(SS)(PA)] and [(SS)I]· I, respectively. The charge transfer interaction was successfully applied to the determination of SS drug using mentioned σ and π-acceptors also, the results obtained herein are satisfactory for estimation of SS compound in the pharmaceutical form. [ABSTRACT FROM AUTHOR]

Abstract: The novel Cu(II) and Zn(II) complexes of first and second generation poly(propylene amine) dendrimers (PPA), comprising 1,8-naphthalimde units on periphery have been synthesized. These new complexes were characterized by elemental analysis, molar conductivity, spectral methods (IR, 1H NMR and UV–vis spectra) and thermal analysis (TG and DTG) techniques. From elemental analysis as well as thermal studies it has found that the first generation dendrimer behaves as bidentate ligand and forming chelates with 1:2 (ligand:metal) and 1:4 (ligand:metal) stoichiometry for second generation dendrimer. Different kinetic parameters namely activation energy (ΔE*), enthalpy of activation (ΔH*), entropy of activation (ΔS*) and free energy change of activation (ΔG*) are calculated using Coats–Redfern equation. The antibacterial activity of dendrimers and their complexes was evaluated against some Gram positive and negative bacteria. [Copyright &y& Elsevier]

Background: Hybrid molecules furnished by merging two or more pharmacophores is an emerging concept in the field of medicinal chemistry and drug discovery. Currently, coumarin hybrids have attracted the keen attention of researchers to discover their therapeutic capability against cancer., Objective: The present study aimed to evaluate the in vitro antitumor activity of a new series of hybrid molecules containing coumarin and quinolinone moieties 4 and 5 against four cancer cell lines., Materials and Methods: A new series of hybrid molecules containing coumarin and quinolinone moieties, 4a-c and 5a-c, were synthesized and screened for their cytotoxicity against prostate PC-3, breast MCF-7, colon HCT- 116 and liver HepG2 cancer cell lines as well as normal breast Hs-371 T., Results: All the synthesized compounds were assessed for their in vitro antiproliferative activity against four cancer cell lines and several compounds were found to be active. Further in vitro cell cycle study of compounds 4a and 5a revealed MCF-7 cells arrest at G2 /M phase of the cell cycle profile and induction apoptosis at pre-G1 phase. The apoptosis-inducing activity was evidenced by up-regulation of Bax protein together with the downregulation of the expression of Bcl-2 protein. The mechanism of cytotoxic activity of compounds 4a and 5a correlated to its topoisomerase II inhibitory activity., Conclusion: Hybrid molecules containing coumarin and quinolinone moieties represents a scaffold for further optimization to obtain promising anticancer agents., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)