Amr Negm

Chemotherapeutic agents for the treatment of hepatocellular carcinoma: efficacy and mode of action

Hepatocellular carcinoma (HCC) is a dreaded malignancy that every year causes half a million deaths worldwide. Being an aggressive cancer, its incidence exceeds 700,000 new cases per year worldwide with a median survival of 6-8 months. Despite advances in prognosis and early detection, effective HCC chemoprevention or treatment strategies are still lacking, therefore its dismal survival rate remains largely unchanged. This review will characterize currently available chemotherapeutic drugs used in the treatment of HCC. The respective mode(s) of action, side effects and recommendations will be also described for each drug.

Expeditious Entry to Functionalized Pseudo-peptidic Organoselenide Redox Modulators via Sequential Ugi/SN Methodology

An efficient route towards the synthesis of symmetrical diselenide and seleniumcontaining quinone pseudopeptides via one-pot Ugi and sequential nucleophilic substitution (SN) methodology was developed. Compounds were evaluated for their antimicrobial and anticancer activities and their corresponding antioxidant/pro-oxidant profiles were assesed employing 2,2-diphenyl-1-picrylhydrazyl (DPPH), bleomycin dependent DNA damage and glutathione peroxidase (GPx)-like activity assays. Selenium based quinones were among the most potent cytotoxic compounds with a slight preference for MCF-7 compared to HepG2 cells and good free radical scavenging activity. Furthermore, symmetrical diselenides exhibited the most potent GPx-like activity compared to ebselen. Moreover, compounds 7, 8, 9 and 10 exhibited similar antifungal activity to the antifungal drug clotrimazole with modest activity against the Gram-positive bacterium S. aureus. These results indicate that some of the synthesized organoselenides are redox modulating agent with promising anti-cancer and antifungal potentials.

Conductometric and volumetric study of copper sulphate in aqueous ethanol solutions at different temperatures

Abstract An Anton Par Model 55 densimeter was used to measure the densities of copper sulphate solutions in H2O and EtOH–H2O at 298.15 K, 303.15 K, 308.15 K, and 313.15 K. The acquired information was used to ascertain the apparent molar volumes, limiting partial molar volumes, and transfer partial molar volumes of copper sulphate. These computed parameters were utilized to decipher the solute–solute and solute–solvent interactions of copper sulphate in an aqueous ethanol solution. The ion solvation behavior of copper sulphate in water and aqueous ethanol over the range of 298.15–313.15 K was studied using the electrical conductivity principle. The Kraus–Bray and Shedlovsky models of conductivity were used to analyze the obtained conductance data. From the obtained data, the limiting molar conductance λ°m, association constant KA, energy of activation of the rating process (Ea), and related thermodynamic parameters were determined. The Walden product (λ°mη0) was determined. The standard thermodynamic parameters of association (ΔG°A, ΔH°A) were calculated and discussed. Increased ion–solvent and solvent–solvent interactions are indicated by limiting molar conductance values with an increasing amount of ethanol. The negative ΔG°A values indicate that the association processes in all of the studied systems are spontaneous processes. The negative estimation of (ΔH°A) demonstrates that the association processes is exothermic in nature.

Sucrose diester of aryldihydronaphthalene-type lignans from Echium angustifolium Mill. and their antitumor activity

Four previously undescribed sucrose diester of aryldihydronaphthalene-type lignans, named echiumins A-D, were isolated from the butanol fraction of Echium angustifolium Mill, in addition to a known compound, trigonotin A, which is reported for the first time from the title plant. The structures of isolated compounds were elucidated using spectroscopic methods such as HRESIMS and 1D and 2D NMR spectroscopy. The isolated compounds displayed strong to weak antitumor activity against HepG2 and MCF7 cancer cell lines, with echiumins A and D showed the most potent activity.

Cytoprotective and antioxidant properties of organic selenides for the myelin-forming cells, oligodendrocytes

Here a new series of twenty-one organoselenides, of potential protective activity, were synthesized and tested for their intrinsic cytotoxicity, anti-apoptotic and antioxidant capacities in oligodendrocytes. Most of the organoselenides were able to decrease the ROS levels, revealing antioxidant properties. Compounds 5b and 7b showed a high glutathione peroxidase (GPx)-like activities, which were 1.5 folds more active than ebselen. Remarkably, compound 5a diminished the formation of the oligodendrocytes SubG1 peak in a concentration-dependent manner, indicating its anti-apoptotic properties. Furthermore, based on the SwissADME web interface, we performed an in-silico structure-activity relationship to explore the drug-likeness of these organoselenides, predicting the pharmacokinetic parameters for compounds of interest that could cross the blood-brain barrier. Collectively, we present new organoselenide compounds with cytoprotective and antioxidant properties that can be considered as promising drug candidates for myelin diseases.