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Solid polymer electrolytes containing methylcellulose:dextran (MC-DEX), ammonium hexafluorophosphate (NH4PF6), and glycerol have been prepared via the solution cast method. Various techniques have been used to characterize the prepared electrolyte samples. Fourier transform infrared spectroscopy (FTIR) analysis revealed the interaction between polymers and electrolyte components. According to the electrical impedance spectroscopy (EIS), the highest conducting plasticized system achieves a conductivity of 6.71 × 10-4 S cm−1 at ambient temperature. The mobility, number density, and diffusion coefficient of ions were measured using both FTIR and EIS methods, and it was found that their values rise as the amount of glycerol increases. Polarization due to ion migration is responsible for the high value of dielectric parameters. According to transference number measurement (TNM), the transport ion (tion) is 0.92, verifying that the ions are the primary charge carriers. The electrochemical stability window of the maximum conducting plasticized system is 1.58 V, based on linear sweep voltammetry (LSV) analysis. The electrical double-layer capacitor (EDLC) device is fabricated using the highest conducting plasticized system. The cyclic voltammetry (CV) curve is roughly rectangular in shape and with no presence of Faradaic peaks with its specific capacitance of 32.69F/g at 10 mV/s.

Hydroxyethyl cellulose (HEC) doped with 3 wt% erbium nitrate film was prepared by casting from solution. The effect of plasma treatment on optical properties of composite film was investigated. The optical absorbance was measured in the wavelength region of 200–800 nm. . Electronic transition was proved to be direct allowed for pristine and plasma treated film. Tauc’s plots were used to determine the optical band gap (Eopt) of the samples under study. The energy gap was 5.30 eV for untreated composite film and the treated samples at 10, 20 and 30 min have lower values of optical band gap, 5.22, 5.20 and 4.90 eV respectively. It was also found that the Urbach energy values (Ee) were decreased under different plasma treatment times. It begins with 1.46 eV for untreated sample till it reaches 0.72 eV for 30-minute treated sample. Wemple–DiDomenico model parameters such as, oscillator energy, dispersion energy and zero-frequency refractive index values were calculated and their variations with plasma were studied. The color parameters for composite film are noticeably affected under plasma treatment.

In this study, biosynthesized nanoparticles using chitosan, Ulva fasciata, and Avicennia marina leaves extracts (A, B, and C, respectively), were evaluated as paint additives to control marine fouling on different substrates. These biocidal nanoparticle compounds were prepared using a green biosynthesis method. Their characterizations were conducted using Fourier-Transform Infrared spectroscopy and Transmission electron microscopy. Each nanoparticle compound was mixed with a prepared paint, resulting in three formulations for each (e.g. 1C, 2C, 3C), containing 20%, 40%, and 60% by weight. Painted PVC, wood, and steel with these nine paints, and the control were immersed in seawater for different periods. After two months of immersion, the least number of fouling species, (one species) was recorded on both the wood and steel panels that were coated with paint (1C). Meanwhile, after four months, the least numbers of fouling (four and six species) were recorded on wood and steel panels that were coated with paint (3C). After around seven months of immersion, the least numbers of fouling species (five and ten) were recorded on wood and steel panels that were coated with paints (1C and 3C), respectively. The steel panel coated with (3C), harbored ∼2% of the total number of barnacles found on the control, after 7 months of immersion. The superior antifouling agent efficiency of extract (C) nanoparticles can be attributed to its constituents of polyphenols, ammonium compounds, and high concentrations of alcohols, besides the presence of both aromatic and aliphatic amide and amide derivatives.

Cytotoxicity and antibacterial activities of Euphorbia schimperiana total extract, fractions, and isolated secondary metabolites were investigated. The cytotoxicity assays were assessed against four human cancer cell lines HCT116, MCF7, HePG2, and PC3 as well as against normal cell line RPE1. The plant total extract, fractions, and pure compounds were more effective against PC3 and HepG2 cell lines than HCT116 and MCF7. Significant results were observed for ethyl acetate and n-hexane fractions against PC3 with IC50 of 4.7 μg/ml for ethyl acetate, however, n-hexane exhibited 100% cytotoxicity up to 6.25 μg/ml. The antibacterial potential activity was achieved on four pathogenic Gram-positive and four Gram-negative bacteria. The results showed that ethyl acetate and n-butanol fractions had more valuable results (p

Glasses with the chemical composition of 52B2O3 – 12SiO2–26Bi2O3 – (10 − x)TiO2 - xY2O3, :(0 ≤ x ≤ 10) prepared using the melt-quench method. The goal of this study is to investigate the structural, mechanical, and radiation shielding characteristics of these samples. XRD analysis has explored the nature of the glass system. Molar volume obtained reduced while the density denotes increased in the present system. As the molar volume decrease inter-ionic distance, polaron radius, inter-nuclear distance, and Y-Y separation of the investigated glasses decreased. The mechanical characteristics depend on the glass structure of the current glasses sample. Ultrasonic velocities and elastic moduli (experimental and theoretical) for these glasses obtained they were observed to get enhanced. The radiation shielding efficiency was investigated by Phy-X/PSD software. The mass attenuation coefficient, mean free path, half-value layer, tenth value layer, and effective atomic number of glasses have been designed to simulate gamma photon energies between 0.015 and 15 MeV.

To formulate multiparticulate controlled-release alginate-gelatin (AL-GL) beads in order to modify gliclazide (GLZ) release rate. AL-GL beads were prepared using different glutaraldehyde concentrations and dried using either air or freeze-drying method. For comparison, calcium alginate beads (AL-beads) were prepared at different temperatures. Drug incorporation efficiency, beads swelling%, drug release rate, and kinetics in gradient conditions (USP Apparatus-4) were studied. Selected AL-GL beads, as a test formulation (T), were in-vivo compared with Diamicron® 80 mg conventional tablet (R). AL-beads curing temperature was inversely proportional to GLZ incorporation efficiency and directly proportional to beads swelling%. GLZ release from AL-beads was slow in 0.1 N HCl and very fast in pH 7.4. In case of AL-GL beads, GLZ incorporation efficiency and swelling% were inversely proportional to glutaraldehyde concentration. AL-GL beads showed zero-order release of GLZ for up to 11 h. Scanning electron microscope (SEM) images of the freeze-dried beads showed a highly porous surface. Differential scanning calorimetry (DSC) and Fourier transform infra-red (FT-IR) studies indicated an interaction between alginate and gelatin due to crosslinking, while FT-IR indicated the absence of chemical interaction with GLZ. The relative bioavailability (T/R) was 97.57, 138.34, and 143.53%, for Cmax, AUC0–72, and AUC0–∞, respectively. Tmax of T was significantly higher than R. AL-GL beads could represent promising delivery systems for modulating GLZ release rate and minimizing the variation in its absorption.

Lung cancer is one of the most lethal cancers which is causing up to 3 million deaths annually worldwide. Therefore, management of lung cancer needs searching for new chemopreventive agents. This work was designed to inspect the chemopreventive potential of different extracts prepared from branches and leaves of Synadenium grantii for screening their effects on lung cancer cells (A549), then the most active extract was used for combating lung cancer induced in animal model. The in vitro results showed that, the methanolic extract was the most active extract against A549 cells with a notable cytotoxicity activity (IC50: 4.30±0.44 µg/ml), which was close to the activity of standard drug, doxorubicin (IC50: 3.50±0.40 µg/ml). The results of the in vivo experiment, revealed that in B(a)P-treated group, aspartate (AST) and alanine (ALT) transaminase activities as well as the levels of urea, creatinine, alpha-fetoprotein (AFP) and Phosphotylinosital 3 Kinase (PI3K) were significantly increased comparing to control group. However, treatment with S. grantii ameliorated the increase in these parameters in both after- and before-treatment groups comparing with B(a)P-treated group. This improvement in biochemical results were also supported by improving in morphological and histopathological injuries induced by B(a)P, which indicated that methanolic extract of S. grantii has a chemoprevention effect on lung cancer.

Nanocomposites films based on Poly Vinyl Pyrrolidone/Chitosan (PVP/Chitosan) filled by Vanadium pentoxide nanoparticles (V2O5 NPs) have been produced via solution casting method. Vanadium pentoxide nanoparticles were scattered direct in the blend of PVP/Chitosan by one-potential laser ablation technique. The main purpose in using Vanadium pentoxide nanoparticles is to modify the structural, optical, and electrical characterization of PVP/Chitosan composite. The complexation between Vanadium pentoxide nanoparticles and PVP/Chitosan has been approved via XRD and FTIR-ATR analyses. The average size of V2O5 was 20.5 nm. After the scattering by vanadium pentoxide nanoparticles, AC conductivity improved. The values of dielectric constant and dielectric lose decreased as the frequencies enhanced. At lower frequency, greater values of dielectric constant and dielectric lose have been detected due to the mobile charges inside the polymeric backbone. The fabricated PVP/Chitosan/V2O5 NPs films could be suggested for electrical and optoelectronic applications.

Blends with composition 50/50(wt/wt%)poly(vinyl)alcohol (PVA)/poly(vinyl) pyrrolidone (PVP) doped with different weight ratios from benzoxazinone derivative (BZ) were prepared by casting solution technique. The optical absorption was recorded at room temperature in the wavelength range of 190–1100 nm. Tauc's plots revealed direct allowed transition with optical band gap, Eopt, of 5.20 eV for blend film. Under addition of benzoxazinone, the optical energy value decreased until 2.60 eV for 12 wt% BZ blend system. Optical parameters such as refractive index, dielectric constant, dielectric loss and color constants were determined. Benzoxazinone molecules have a significant effect on optical parameters.

3-Chloro-3-chlorosulfenyl-4���-methylspiro[chroman-2,1���-cyclohexane]-4-one (4) was prepared from the reaction of spiro 4���-methylcyclohexan-1���,2-chroman-4-one (3) with thionyl chloride according to reported method. Furthermore, treatment of compound 4 with potassium iodide gave 1,2-bis (3-chloro-4���-methylspirochroman-2,1���-cyclohexyl-4-one)disulfane (6) in addition to 4,4���-dimethyltrispiro[cyclohexane-1,2���-chroman-3���,2���-2H-chromeno[3,4-e][1,3,4]-oxadithiin-5���,1���-cyclohexan]-4���-one (5). The formation of compound 5 could be presumably explained via the formation of unstable intermediate oxo-thioketone A. The formation of the latter intermediate A was confirmed chemically through the thermal reaction of compound 5, or compound 6 with 1,3-homodiene such as: 1,3-cyclohexadiene, isoprene, and 2,3-dimethyl-1,3-butadiene to afford the products 7���9, respectively. The chemical structures of the newly prepared compounds were confirmed by spectroscopic methods (IR, 1H & 13C NMR, and MS). The synthesized compounds were evaluated against lung (A549), prostate (PC3), pancreatic (PACA2), and breast (MDA) cancer cell lines. Compound 3 exhibited prominent cytotoxicity against A549, PC3, and PACA2 cancer cell lines with IC50 values from 12.4 to 16.1 ��M, which was comparable or superior to the reference drug (Doxorubicin). Compounds 7���9 showed better cytotoxicity against breast (MDA) cancer cell line than the reference drug (Doxorubicin).

Alzheimer's disease (AD) is one of the most prevalent neurodegenerative disorders which affects the hippocampus and cortical neurons leading to impairment of cognitive ability. Treatment of AD depends mainly on acetylcholinesterase inhibitors, however, a novel therapeutic approach is introduced based on the maintenance of neuronal viability and functionality exerted through neurotrophic factors. In the current study, Ulmus pumila L. leaves alcoholic extract was investigated for its neuroprotective activity in AlCl3-induced AD in rats. Rats were orally treated with AlCl3 (17 mg/kg) for 4 weeks followed by U. pumila extract (150 mg/kg b.wt.) for another 6 weeks. Treatment of neuro-intoxicated rats with U. pumila extract resulted in a significant regulation in neurotrophic factors; brain derived neurotrophic factor and transforming growth factor-β and pro-inflammatory cytokine; TNF. It also induced an elevation in serum levels of monoamine neurotransmitters; norepinephrine, dopamine and serotonin and a decline in brain acetlycholinesterase activity. U. pumila extract also showed potent antioxidant activity as indicated by the declined malondialdehyde and elevated reduced glutathione, catalase and super oxide dismutase levels in AD rats‘ brains. Histological improvement was detected in the cerebral cortex, the hippocampus and striatum of the treated rats. The phytochemical analysis of U. pumila extract revealed high contents of flavonoids and phenolics and the major compounds were isolated and chemically characterized. Additionally, U. pumila extract and the isolated compounds exerted a prominent activity in in-vitro acetylcholinesterase inhibition assay with kaempferol-3-O-β-glucoside being the most potent compound showing IC50 of 29.03 ± 0.0155 μM. A molecular docking study indicated high affinity of kaempferol-3-O-β-robinobioside on acetylcholine esterase binding site with estimated binding free energy of –8.26 kcal/mol.

This overall process deals with evaluating the performance of silver nanoparticles, synthesized from sodium caseinate (SC) as green biological active agent, in comparison with widely produced from carboxymethyl cellulose, other carbohydrates (oxidized nanocellulose fibres (OC) and starch (St)). The TGA, FTIR and TEM, as well as its antimicrobial activities toward pathogenic Gram-positive and Gram-negative bacteria in addition to the yeast strain Candida albicans NRRL Y-477 were examined. In addition, with regard to their anti-tumour activity, the evaluation was studied via many cancer cell lines against RPE1 (normal retina cell line). The results revealed that the SC–Ag(I) and CMC–Ag(I) complexes were formed in six- and five-membered chelate rings, respectively, as nanoparticles, while linear chelation structure was formed in case of OC–Ag(I) and St–Ag(I) complexes. The complexation of SC with Ag(I) ions was recommended as promising stable and antimicrobial agent, with lower free Ag(I) ions and particle size than other Ag-complexes. Moreover, it provided anti-tumour activity of most tested cell lines ( in vitro ), with the following sequence HCT116 > PC3 > HePG 2 > MCF-7 > A549 with IC 50 and IC 90 values of 25.8 and 54.73 µg ml −1 , 45.1 and 66.7 µg ml −1 , 64.3 and 110.7 µgml −1 , 71.4 and 114.8 µgml −1 and 80.1 and 127.7 µgml −1 , respectively. The promising effect of SC–Ag complex was also clear from its selective index versus RPE1 (normal retina cell line).

The electrical and optical properties of superalkali (OLi3) and superhalogen (MgF3) doped boron nitride nanocage are investigated. Superalkali and superhalogen are doped physically and substitutionally with boron nitride and its geometrical and optoelectronic properties are analyzed and compared systematically. In the doped nanocage of boron nitride, the linear optical polarizability and nonlinear optical hyperpolarizability increases to a greater extent. The increasing trend of the hyperpolarizability in the nanocage of metal-doped boron nitride depends on the atomicity of superhalogen and superalkali metal. The energy bandgap of HOMO-LUMO also decreases due to the injection of new energy levels in all the doped compounds of boron nitride near the Fermi level. Among different combinations, MgF3 and OLi3 doped with B12N10 found the most reliable combination with enhanced linear and nonlinear optical polarizability. The current clue gives wide applications for boron nitride nanocage in electrical instruments and devices that play an important role in the designing of efficient nonlinear optical materials.

Nitrogen doped graphene modified WO3 nanocomposites were synthesized through an effective methodology. The prepared photocatalysts were employed as active candidates for degradation of highly toxic organics i.e., 2, 4 dichloro phenol (2, 4-DCP) and methyl orange (MO). XRD profile of N-graphene showed complete reduction of GO into N-graphene. All diffraction peaks of WO3 along with N-graphene indicated monoclinic phase of WO3. SEM and TEM images of 3.0% N-graphene/WO3 have demonstrated the mixed morphology of irregular massive rod like blocks and round shaped particles of WO3 distributed on cracked sheets of N-graphene. Nitrogen defects in graphene altered zero band gap semi-metallic graphene to semiconducting material and increased the absorption edge of N-graphene/WO3 nanocomposites towards visible region as studied in DRS analysis. FTIR and Raman studies showed the strong connection between N-graphene and WO3 by making W − O − C surface linkage. The noticeable reduction in PL emission peaks of 3.0% N-graphene/WO3 indicated obvious separation of photo induced charge carriers. The study of radical scavengers suggested that holes (h+) and •OH are the main elements for the decontamination of both MO and 2, 4-DCP. XPS analysis shows all possible C − N bonding configurations in 3.0% N-graphene/WO3. 3.0% N-graphene/WO3 composite showed the maximum photo degradation of MO ( ~ 94.0%) and 2, 4-DCP ( ~ 81.0%). The synergism between N-graphene and WO3 results into more sporty sites on catalyst and restoring of sp2 structural defects in N-graphene lattice improve the transportation of charge carriers during photocatalysis. This work provides innovative strategies for designing the N-graphene/semiconductor nanosystems with enhanced photocatalytic phenomena in the environmental cleanup remedies.

Hydroxyethyl cellulose (HEC) film has been prepared by casting technique. The prepared sample has been treated with nitrogen plasma at different exposure times. The optical absorption was recorded at room temperature in the wavelength range of 200-800 nm. Absorbance fitting procedure curves revealed a direct allowed transition with optical band gap, Eopt, of 4.9 eV for pristine film, and this value decreases to 4.30 eV for 20 min plasma treatment time. The band tail values (Ee) were found to be increased under plasma time treatment from 1.74 eV in case of the pristine film to 2.20 eV for 20 min. The dispersion of refractive index and complex dielectric constants under plasma treatment was also studied. Variation of color parameters under effect of the plasma treatment is analyzed in the framework of CIE L*U*V* color space.

Acute kidney injury (AKI) is a complex clinical condition associated with significant morbidity and mortality and lacking effective management. Ischemia-reperfusion injury (IRI) remains one of the leading causes of AKI in native and transplanted kidneys. The aim of this study was to evaluate the efficacy of adipose-derived mesenchymal stem cells (ADSCs) in the prevention of renal IRI in rats. The study was conducted on male Sprague-Dawley rats (n=72) weighing 250–300 g. Rats were randomly assigned to three main groups: i) Sham-operated control group (n=24); ii) positive control group, in which rats were subjected to IRI and were administered culture media following 4 h of IRI (n=24); and iii) ADSC group (n=24), in which rats were administered 1×106 ADSCs via the tail vein following 4 h of IRI. Each main group was further divided according to the timing after IRI into four equal-sized subgroups. Renal function was tested via the measurement of serum creatinine levels and creatinine clearance. In addition, malondialdehyde (MDA) levels were determined in serum and renal tissue homogenate as an indicator of oxidative stress. Histopathological changes were analyzed in different regions of the kidney, namely the cortex, outer stripe of the outer medulla (OSOM), inner stripe of the outer medulla (ISOM) and inner medulla. In each region, the scoring system considered active injury changes, regenerative changes and chronic changes. The ADSCs were assessed and their differentiation capability was verified. IRI resulted in a significant increase in serum creatinine, serum and tissue MDA levels and a significant reduction in creatinine clearance compared with those in sham-operated rats,. These changes were attenuated by the use of ADSCs. The prominent histopathological changes in the cortex, ISOM and OSOM were reflected in the injury score, which was significantly evident in the positive control group. The use of ADSCs was associated with significantly lowered injury scores at days 1 and 3; however, no significant effect was observed on day 7. These results indicate that the use of ADSCs ameliorates renal injury and dysfunction associated with IRI in rats.

A novel series of 5-nitro-1H-benzimidazole derivatives substituted at position 1 by heterocyclic rings was synthesized. Cytotoxicity and antiviral activity of the new compounds were tested. Compound 3 was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound 3 showed no activity against human liver carcinoma Hep G-2 cell line. Compounds 9 and 17b (E) showed potency near to doxorubicin against the four cell lines. The acute toxicity of compound 9 on liver cancer induced in rats was determined in vivo. Interestingly, it showed restoration activity of liver function and pathology towards normal as compared to the cancer-bearing rats induced by DENA. Compounds 17a (Z), 17b (E) and 18a (Z) were the most promising compounds for their antiviral activity against rotavirus Wa strain.

Hydroxyethyl cellulose and cobalt chloride are used as precursor materials for the synthesis of cobalt oxide (Co3O4) nanoparticles. A composite system from polymer and metal chloride is prepared via casting technique. The thermal decomposition of the composite is studied using thermogravimetric technique. Calcination of the composite system at 350°C resulted in the formation of Co3O4 nanoparticles. X-ray diffraction analysis reveals the presence of crystalline Co3O4 with an average particle size of around 15 nm. The bonding nature and morphology of nanosized Co3O4 are examined using transmission electron microscopy and infrared spectroscopy. The Tauc's plot indicates the energy band gap for direct allowed transition as 3.2 eV and 1.4 eV. POLYM. COMPOS., 2015. © 2015 Society of Plastics Engineers

A series of thiazole, pyridine and benzylidene derivatives derived from thiophene scaffold have been synthesized. The antitumor evaluation of the newly synthesized products against four cancer cell lines, namely breast carcinoma (MCF-7), liver carcinoma (HepG2), colon carcinoma (HCT-116) and prostate carcinoma (PC3), indicated that the thiazole derivative 11b showed remarkable activity against all cell lines with LC50 values of 18.3, 2.5, 7.5 and 7.6 µM, respectively. Cytotoxicity toward normal cell lines was also investigated and indicated that compound 21c displayed remarkable potency against PC3 with LC50 values of 7.1 µM and showed weak inhibition of normal cell lines at (GI %) of 41.2 % and thus could be considered as an important lead compound for potential application in anticancer chemotherapy. Brine shrimp lethality assay of the most active compounds was carried out to detect possible cytotoxicity effects and indicated that highly active compound, 21c, is not harmful. The X-ray crystallographic analysis of compounds 3 and 11b was obtained thus establishing with certainty the proposed structures in this work. The synthesized compounds were also screened for their free radical scavenging activity. Hydrazino–thiazole derivatives 15 and 16 showed remarkable antioxidant activity with IC50 values of 60.9 and 61.9 μg ml−1, respectively.

Silver nanoparticles (Ag NPs) were synthesized by chemical reduction of silver salt (AgNO3) through sodium borohydride. The characteristic surface plasmon resonance band located at around 400nm in the UV-Visible absorption spectrum confirmed the formation of Ag nanoparticles. Polyvinyl alcohol-silver (PVA-Ag) nanocomposite films were prepared by the casting technique. The morphology and interaction of PVA with Ag NPs were examined by transmission electron microscopy and FTIR spectroscopy. Optical studies show that PVA exhibited indirect allowed optical transition with optical energy gap of 4.8eV, which reduced to 4.45eV under addition of Ag NPs. Optical parameters such as refractive index, complex dielectric constant and their dispersions have been analyzed using Wemple and DiDomenco model. Color properties of the nanocomposites are discussed in the framework of CIE L(∗)u(∗)v(∗) color space. The antimicrobial activity of the nanocomposite samples was tested against Gram positive bacteria (Staphylococcus aureus NCTC 7447 &Bacillus subtillis NCIB 3610), Gram negative bacteria (Escherichia coli, NTC10416 &Pseudomonas aeruginosa NCIB 9016) and fungi (Aspergillus niger Ferm - BAM C-21) using the agar diffusion technique. The antimicrobial study showed that PVA has moderate antibacterial activity against B. subtillis and the 0.04wt% Ag NPs composite sample effect was strong against S. aureus.

Casting solution method has been used to prepare Polyvinyl alcohol (PVA) film. The prepared film has been irradiated with a laser beam of 6 ns Q-switched Nd:YAG laser (Lotus II) operating at 10 Hz and fourth harmonic wavelength, 266 nm, at different irradiation times. Optical absorbance of the irradiated sample was studied in the wavelength region between 200 and 800 nm. The absorption peak shift of 272 nm towards the longer wavelengths region and the increase of absorption as the irradiation time increases, are related to the increase in crosslinking network. The fitting technique of the absorbance revealed an indirect allowed transition with optical energy gap of 4.22 eV for the pristine PVA sample, and 2.85 eV after 2 h of laser irradiation. The index of refraction and the dielectric function showed dispersion in the studied wavelength range. The analysis of color parameters of PVA showed an observable change after laser irradiation.

The ability of eight flavonoids to react with the biologically relevant reactive nitrogen species, nitric oxide, peroxynitrite, and nitrous acid were investigated in vitro, for the first time. All the investigated flavonoids were found to be potent reactive nitrogen and oxygen species scavengers and resulted in a significant inhibition of 3-nitrotyrosine (3-NT) formation in a dose-dependent manner. All the IC50s were found at the μM level. The results reveal that, the presence of C5–OH and C4’–OH, in the flavonoid skeleton, enhanced the anti-nitrosative activity. The absence of the C2=C3 double bond and/or C4-carbonyl group resulted in slight decrease of the anti-nitrosative activity. However, the presence of C6- and/or C3’-methoxy groups together with C4’–OH dramatically decrease the inhibition capacity. Especially the free hydroxyl groups at 3’ and 4’ of the catechol containing ring B flavonoids as well as both hydroxyl groups at C3 and C5 are necessary for better antioxidant activity. The absence of both C3–OH and/or C3’–OH groups resulted in a remarkable decrease in the antioxidant activity. The cytotoxicity results indicate that the investigated flavonoids are safe to be used up to a concentration of 100 μM and may be utilized as promising sources of therapeutics.

Background and objectives Hyperlipidemia has been embroiled in atherosclerosis, which is the primary factor of heart disease and stroke. An important aim in the pivotal restrain of atherosclerosis awaits an affordable and safe drug that will fundamentally confirm to have a great effect where treatment is decisive. Humans have been served by a variety of drugs extracted from a natural source, and the most of these cures were provided by higher plants. Materials and methods The aim of this study is to investigate and assess the hypolipidemic effect of Euphorbia lathyris L. extracts on high-fat diet-induced hyperlipidemia in rats, and it shows a scientific proof for expansion of E. lathyris L. as a prospect naturalistic oral hypolipidemic drug. Rats were administrated orally with cholesterol in a dose of 100 mg/1 ml olive oil/1 kg five times a week for 12 consecutive weeks. This was accomplished by assessing the activities of particular biochemical parameters associated with liver functions in tissue of high-fat-diet group when compared with those of control one. Liver function tests, included aspartate aminotransferases; alanine and alkaline phosphatases; antioxidants and oxidative stress biomarkers, such as glutathione, catalase, and glutathione-S-transferase; total antioxidant capacity; nitric oxide; and lipid peroxide. In addition, lipid profile (cholesterol, total lipid, high-density lipoprotein-cholesterol, and triglyceride) were also evaluated. Moreover, histological examination of liver, heart, and kidney was done to prove the biochemical outcomes. Results and conclusion The present findings strongly clarify defects in all biochemical measurements, such as increase in the malondialdehyde level and liver function enzyme activities. However, reductions in enzymatic and nonenzymatic antioxidant in liver of hyperlipidemic rats were marked. On the contrary, treatment of hyperlipidemic rats with low and high dose of methanol and petroleum ether extract of E. lathyris natural product proved to have ameliorating effects in all biochemical parameters under investigation. The previous biochemical observations were also accompanied by histopathological examinations of the heart, liver, and kidney sections, which showed significant recovery of hepatocytes and amelioration in histological architectures of heart and kidney. It could be concluded that the two extracts of E. lathyris showed improvement in liver function enzyme activities, oxidant–antioxidant biomarkers, and lipid profile activities in liver of high-fat-diet rats.

In this study, poly(vinyl alcohol) (PVA) films doped with thorium nitrate hydrate [Th(NO3)4] have been prepared using casting technique. The optical absorption spectra were recorded at room temperature in the wavelength range 200–800 nm. From the absorption edge studies, the values of the Urbach energy (Eu) have been evaluated. These energy values vary slightly with composition, indicating that the model based on electronic transitions between localized states is not preferable. Optical parameters such as refractive index and complex dielectric constant have been determined. The dispersion of the refractive index is discussed in terms of the single-oscillator Wemple-DiDomenico model. Color properties of the prepared samples were discussed in the framework of CIE L*u*v* color space. POLYM. COMPOS., 35:1786–1791, 2014. © 2013 Society of Plastics Engineers

Several new 2,6-bis(substituted)pyridine ligands and 2,6-bis(substituted)pyridine Ag(I) nitrate complexes were synthesized and characterized spectroscopically. The newly synthesized ligands include pyridine-2,6-bis(3-oxopropanenitrile) (1), pyridine-2,6-bis(2-cyano-N-phenyl-3-oxopropanethioamide) (2), and pyridine-2,6-bis((E)-2-(2-phenylhydrazono)-3-oxopropanenitrile) (3). The newly synthesized ligands and silver(I) complexes were evaluated for their in vitro anticancer activity against four human cancer cell lines including hepatocellular carcinoma (HePG2), lung adenocarcinoma (A549), colon carcinoma (HT29), and breast adenocarcinoma (MCF7). Most of the newly synthesized silver(I) complexes exhibited better activity than the ligands, and the results have been compared with doxorubicin as a reference drug.

Two new flavonoid compounds were isolated from Astragalus bombycinus Boiss. and identified as quercetin-3,7-di-O-β-glucopyranoside 4'-O-α-rhamnopyranoside and 5,2',4'-trihydroxy-flavone-8-C-α-arabinopyranoside-7-O-β-glucopyranoside. In addition, apigenin, apigenin-7-O-β-glucopyranoside, apigenin 7-O-gentobioside, luteolin, luteolin-7-O-β-glucopyranoside, quercetin-3,7-di-O-β-glucopyranoside, quercetin-3-O-β-glucopyranoside-7-O-α-rhamnopyranoside and daidzein were also isolated and identified. The structure elucidation of the isolated compounds was performed by chromatographic, chemical and spectroscopic methods. Antioxidant and cytotoxic activities were also determined for the four consecutive extracts of the plant.

1.1.Background:Mesenchymal stem cells (MSCs) have generated a great deal of excitement and promise as a potential source of all types of cells for cell-based therapeutic strategies. The reparative role of MSCs may be multifunctional and include the secretion of anti-inflammatory cytokines like TGFβ1 to limit apoptosis and dampen the inflammatory response. There are reports suggesting that antioxidants such as N N'-diphenyl-1, 4-phenylenediamine (DPPD) inhibit interstitial fibrosis induced by cisplatin. It inhibits lipid peroxidation and nephrotoxicity induced by cisplatin, where antioxidants make trapping for free radicals. 1.2.Aim:We aimed to investigate the inhibitory potential of either stem cells or DPPD on renal fibrosis in cisplatin induced tubulointerstitial fibrosis rat model. 1.3.Materials and methods:This study was carried on 40 male Sprague-Dawley rats (body weight 170 - 220 g). Rats were divided into 4 groups as follow: Control group, received intravenous saline. Cisplatin group, received cisplatin (6 mg/kg, i.p). DPPD group, received cisplatin (6 mg/kg, i.p) at the start of experiments and three days after cisplatin administration, rats were given DPPD (0.5 g/kg, i.p) every two days. MSCs group, received cisplatin (6 mg/kg, i.p) at the start of experiments and three days after cisplatin administration, rats were given MSCs (1 ×106, i.v) single dose. 14 days after cisplatin (or saline) administration, blood samples were obtained and kidneys were removed for biochemical, histopathology and immunohistochemical markers investigations. 1.4.Results:In addition to the significant rise in urea and creatinine, cisplatin group showed atrophied glomeruli with tubular cells vacuolization and increased collagen deposition. Alpha smooth muscle actin (α-SMA) and fibroblast proliferation marker Ki-67 were found to be increased in renal tissue. Lipid peroxidation and collagen formation markers showed significant elevation. Both MSCs and antioxidant ameliorated cisplatin-induced nephrotoxicity to a great extent and showed marvelous anti-fibrotic effect as evidenced by histopathological, immunohistochemical and biochemical assessments. 1.5.Conclusion:Both MSCs and antioxidant (DPPD) were found to have potent potentials to inhibit tubulointerstitial fibrosis in cisplatin induced nephrotoxicity rat model.

Natural rubber (NR)-barium ferrite (BaF) composites (RFCs) have been prepared. Structural features of the composites were characterized by Infrared spectroscopy and scanning electron microscope (SEM). Differential scanning calorimetry (DSC) analysis showed that there is small variation of glass transition temperature (≈ –1℃). The activation energy of glass transition was calculated by Kissinger method and has values between (53-110 kJ/mol). Thermodynamic parameters such as activated entropy, enthalpy and Gibbs free energy were calculated for glass transition also. Thermogravimetric analysis TG and its derivative DTG showed one stage thermal decomposition between 300℃-400℃ with weight loss between (19.47%-52.13%). Increasing barium ferrite loading will increase the thermal stability of natural rubber. The kinetic parameters such as activation energy, entropy, enthalpy and Gibbs free energy for composites in the decomposition region were calculated and analyzed using Coats-Redfern technique.

This study is a continuation of our previous work in which a bioassay screening of 346 methanol extracts from 281 Egyptian plant species was carried out for in vitro schistosomicidal activity.Another 309 methanol extracts from 278 plant species were subjected to the bioassay screening using the same technique on viable Schistosoma mansoni Sambon (Schistosomatidae) mature worms in specialized culture medium (Roswell Park Memorial Institute medium 1640) in a trial to discover a source for a schistosomiasis drug from Egyptian flora.The methanol plant extracts were tested in vitro against viable S. mansoni mature worms in culture medium. Viability of worms was examined after exposure to 100 μg/ml of the extract in the medium for 24 h. Negative (dimethyl sulfoxide) and positive (praziquantel) controls were simultaneously used. Extracts showing schistosomicidal activity were further subjected to determination of their (Lethal concentration) LC₅₀ and LC₉₀ values.Confirmed in vitro antischistosomal activity was found in 42 extracts. Of these, 14 plant species possessed considerably high antischistosomal activity (LC₅₀ ≤ 15 µg/ml), viz. Callistemon viminalis (Soland. Ex Gaertn) Cheel, C. rigidus R.Br., C. speciosus (Sims.) DC, C. citrinus Stapf, Eucalyptus citriodora Hook, E. rostrata Dehnh., Eugenia edulis Vell, E. javanica Lam syn. Syzygium samarangense (Blume) Merril, Melaleuca leucadendron (L.) L., M. stypheloides Sm. (all belong to Myrtaceae), Cryptostegia grandiflora R.Br. (Asclepiadaceae), Zilla spinosa (L.) Prantl (Cruciferae), Ficus trijuja L. (Moraceae) and Fagonia mollis Delile (Zygophylacae).These species may represent additional natural sources of bioactive material that deserve further investigation for drug discovery against schistosomiasis.

Films with different compositions of polyvinyl alcohol (PVA) and carboxymethyl cellulose (CMC) blends have been prepared using the casting method. Differential scanning calorimetery (DSC), thermogravimetric analysis (TGA) and dielectric spectroscopy of all compositions have been investigated. It was found that PVA and CMC are compatible in the studied range of composition. With increasing CMC content, the thermal stability of PVA increases. Based on DSC and TGA data, the activation energies of all the investigated samples were calculated. The absorption edge ( E a ) was also determined from Ultraviolet–visible (UV–vis) spectra. Dielectric permittivity, loss tangent and ac conductivity of all samples were studied as functions of temperature and frequency. The results show that the dielectric dispersion consists of both dipolar and interfacial polarization. The frequency dependence of the ac conductivity indicates that the correlated barrier hopping (CBH) is the most suitable mechanism for conduction. The polaron binding energy ( U M ) was determined. Results of the present system are compared with those of similar materials.

Polyvinyl alcohol (PVA) films doped with europium chloride (EuCl 3 ) have been prepared by casting from their aqueous solutions. The phase transitions and thermal decomposition behavior of the prepared samples were investigated by thermal analysis and the interactions between the host PVA and Eu 3+ were examined by FTIR spectroscopy. The optical absorption was recorded at room temperature in the range of 190–1000 nm. From the absorption edge studies, the values of the Urbach energy ( E e ) were found to be 0.56 eV in case of the pure polymer; however, its value increased to be in the range of 1.21–1.75 eV. These energy values indicate that the model based on electronic transitions between localized states is not preferable and transitions are made between band tails. Optical parameters such as refractive index and complex dielectric constant have been determined. The dispersion of the refractive index is discussed in terms of the single-oscillator Wemple-DiDomenico model. Color properties of the prepared samples are discussed in the framework of CIE L ⁎ u * v * color space. The prepared samples have been used as catalysts in the photocatalytic degradation of p -nitrophenol (PNP) in aqueous solution under UV light irradiation using H 2 O 2 as oxidizing agent. The catalytic activity of the Eu-polymer towards the photodegradation of PNP greatly increased after doping with Eu 3+ ions. The highest catalytic activity was noticed at the optimum pH value of 5.5.

2,7-di-tert-butylpyrene was oxidized to 2,7-di-tert-butylpyrene-4,5,9,10-tetraone. The latter through condensation reactions with vicinal diamine such as 4,5-diaminophthalonitrile produced heterocyclic monomer, 2,7-di-tert-butyl pyrene[4,5][9,10]bisquinoxaline-6,7-dinitrile, which was cyclo-tetramerized to the corresponding tetra[2,3-(1,4-diaza-6,6-di-tert-butylphenanthreno)[4,5]phthalocyanine]-based network polymer (2H-Pc), and tetra [2,3-(1,4-diaza-6,6-di-tert-butylphenanthreno)[4,5]phthalo-cyaninato metal II-based network polymers (M-Pc, M= Co, Ni, Zn, or Cu). Elemental analytical results, IR and NMR spectral data of the new prepared molecules are consistent with their assigned formulations. Molecular masses and metal contents of the synthesized polymers proved to be of high molecular masses which confirm the efficiency of tetramerization polymerization and complexation reactions. The dielectric constant (e′) and dielectric loss tangent (tan δ) were studied as a function of temperature and frequency. The detailed analysis of the results showed that the dielectric dispersion consists of both dipolar and interfacial polarization. Measurements of ac conductivity as a function of frequency at different temperatures revealed that the nonoverlapping small polaron tunneling is the most suitable mechanism for ac conduction behavior. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012

Cast thin films of polyvinyl alcohol/glycogen blends of different compositions have been prepared and subjected to the electrical measurements of both current–time and current–voltage characteristics as well as d.c. conductivity as a function of temperature. The conduction mechanisms operative in the films at different temperature and voltage ranges are estimated from the behavior of log I versus V1/2 plots. For individual polymers, the conduction mechanism appears to be essentially a Poole–Frenkel type. On blending, at lower temperature the charge conduction is through the Schottky emission while at higher temperature the charge conduction mechanism is Poole–Frenkel. In addition, the deviation of the plots at lower voltages indicates the existence of space charge contribution in conduction mechanism. The obtained results made it possible to determine several conduction parameters including activation energy, carrier mobility, and carrier concentration. POLYM. COMPOS., 2009. © 2008 Society of Plastics Engineers

The transient currents, I–V characteristics and dc electrical conductivity of 70/30 (wt/wt.%) polyvinyl alcohol (PVA)/glycogen undoped and doped with eosin films have been studied under different conditions before and after irradiation by γ-doses in the range 5–100 kGy. The conduction mechanisms operative in the films at different temperature and γ-irradiation ranges are estimated from the behaviour of Log I versus V1/2 plots. The results show that both temperature and γ-irradiation affects the type of electronic transport mechanism for undoped blend sample. On doping with eosin, there is only considerable influence on the type of conduction with varying temperature but γ-doses have no significant effect. The dc conductivity for blend sample doped with eosin is found to increase by 1–2 orders of magnitude compared to the undoped sample at both different temperatures and γ-doses. The values of mobility and charge carrier concentration for all samples under investigation were found to vary from (0.26–2.22) × 10− 4m2V− 1 s− 1 and (0.52–76.20) × 1024 m− 3 respectively.

The dielectric relaxation spectra of various poly(vinyl alcohol) (PVA)/glycogen blends and irradiated blend samples with 70 wt % PVA content that were undoped and doped with eosin were measured in extended temperature (30–160°C) and frequency (1 kHz to 1 MHz) ranges. Dielectric relaxation spectroscopy separates different molecular groups of a repeating unit of a polymer with respect to the rate of its orientation dynamics. In the high-temperature range (>100°C), the σ relaxation, which is associated with the hopping motion of ions in the disordered structure of the biopolymeric material, can be measured. The electric dipole moment and the activation energy of the glass-transition temperature relaxation process were calculated. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2008

Differential scanning calorimetry (DSC), thermogravimetry analysis (TGA), UV/visible spectra and colour detection of pristine and γ-irradiated undoped and eosin-doped 70/30 (wt/wt%) PVA/glycogen has been measured. The kinetic parameters such as the activation energy, entropy, enthalpy and free energy for all investigated samples were determined using Coats–Redfern relation. The shift of T g position towards lower temperatures with increasing γ-doses reflect that the degradation process is the predominant one. The values of absorbance and optical parameters in UV/visible range for γ-irradiated blend sample doped with eosin showed no significant variation with increasing γ-doses. This reflects that the addition of eosin to 70/30 (wt/wt%) PVA/glycogen makes it more resistant to γ-radiolysis. The calculated colour parameters such as L ∗ , U ∗ , V ∗ , C ∗ , hue and Y e were found to be dependent on addition of eosin and γ-irradiation.

The dipolar relaxation in poly(vinyl alcohol) (PVA), sodium carboxy methyl cellulose (NaCMCs), and their blends were studied using a thermally stimulated depolarization current (TSDC) technique. The mutual effects of polarization conditions such as heating rate, poling temperature, time, and field on the properties of TSDC were investigated. Quantitative analysis of the experimental data is given in terms of dipolar and space charge polarization. A thermal sampling (TS) technique was applied to decompose the complex relaxations in individual polymers and their blend of 0.5/0.5 wt/wt into its normal distribution components. The activation energy of TS-formed electrets was determined by fitting the experimental curve to Bucci and Fieschi equations. Peak parameters such as activation energy and preexponential factor τ0 were obtained. A linear relationship between the activation energy and logarithm of the preexponential factor was found, thus confirming operation of the compensation law. In addition, by using the Eyring equation of the rate theory, the activation enthalpy ΔH≠ and the activation entropy ΔS≠ were calculated. © 2005 Wiley Periodicals, Inc. J Appl Polym Sci 95: 1342–1353, 2005

Objective: Mulberry is a nontoxic commonly eaten plant, belongs to the Morus and used in folk medicine in the remedy of dysentery, antiphlogistic, diuretic, expectorant, and antidiabetic. The purpose of this study is to evaluate the antiproliferative and radical scavenging activity of the total alcoholic and successive fractions thereof of Morus alba and Morus rubra fruits. In addition, the chemical composition of the bioactive fractions of each species was investigated. Methods: The antiproliferative potential of 8 extracts on 4 human cancer cell lines, hepatocellular carcinoma (HepG2), Caucasian breast adenocarcinoma (MCF7), prostate (PC3), and colon carcinoma (HCT116) in addition to one normal cell line namely human normal immortalized skin fibroblast cells (BJ1) were carried out. Cell viability was determined using MTT assay. The potency was compared with the reference drug doxorubicin. These extracts were also assayed for 1,1-diphenyl-2-hydrazyl free radical scavenging activities. After saponification of the n-hexane fraction, unsaponifiable matter and fatty acid methyl esters were analyzed by gas liquid chromatography (GLC). The chemical composition of the bioactive fractions was investigated using gas chromatography/mass spectrometry (GC/MS) analysis. Results: All the extracts showed significant free radical scavenging activity dose-dependently. The n -hexane and dichloromethane (DCM) fractions of M. rubra exhibited potent cytotoxic activity on almost cancer cell lines. In the same pattern, ethyl acetate (EtOAc) of M. rubra has moderate cytotoxic activity against all cell lines except HepG2. DCM fraction of M. alba possessed both radical scavenging and high potential antiproliferated activities against HCT116 and MCF7 with inhibitory concentration of 43.9 and 32.3 μg/ml, respectively, while it showed no cytotoxic effect on BJ1. GLC analysis showed the major hydrocarbons in M. alba and M. rubra were heptacosane and docosane, respectively. Sterols were similar in both species but with different ratios and cholesterol was the major one. Palmitic and margaric were the major saturated fatty acid while arachidonic was the major unsaturated fatty acid in both species. GC/MS analysis showed the main compound in DCM fraction of each Morus species was palmitic acid. Furthermore, 1,11- bis -(methoxycarbonyl-ethenyl)-10,2-dihydroxy-cycloeicosane and linolelaidic acid, methyl ester were the main compounds in the EtOAc fraction of each Morus species. Whereas, the main compounds in alcoholic extract of M. alba and M. rubra were methyl-14-methyl-pentadecanoate and 1,2- O -isopropylyidene-4-nonene-1,2,3-triol, respectively. Conclusions: The results observed remarkable biological activity of the successive fractions of M. rubra more than those of M. alba and confirmed its importance as a natural bioactive source. Morus species are good candidates to be promising as possible sources for future antitumor and antioxidants in food and pharmaceutical formulations. The strong activity partly explains the potential effects of Morus species for the treatment of cancer and degenerative diseases caused by free radicals.

Several new polysubstituted thiophene and thiadiazole derivatives incorporating a 2,6-pyridine moiety are efficiently synthesized using hitherto not reported bis(3-oxopropanethioamide) (III) as key building block.

Virtually, all studies reporting the outcomes of living kidney donation beyond the first year from donation were retrospective. In this prospective study, the outcome of 81 consecutive living kidney donors was thoroughly evaluated. Clinical, laboratory, and radiological assessments were carried out at predonation (basal), 3, 6, 12, and 24 months after donation. The mean age at time of donation was 37.8 ± 9.8 years and the majority was females (75.3%). The mean BMI increased significantly after donation (P<0.04). The mean serum creatinine levels (mg/dl) were 0.75 ± 0.14, 1.01 ± 0.22, 0.99 ± 0.21, 0.98 ± 0.20, and 0.94 ± 0.20 (P<0.0001). Likewise, the mean levels of measured creatinine clearance (mL/min) were 148.8 ± 35.7, 94.7 ± 26.6, 95.5 ± 24.6, 96.7 ± 20.2, and 101.6 ± 26.2 (P<0.0001). The mean 24 hours urinary protein excretion (gm/dL) were 0.09 ± 0.03, 0.19 ± 0.18, 0.16 ± 0.09, 0.18 ± 0.25, and 0.17 ± 0.12 (P<0.0001). There were significant increases in the means of the longitudinal and transverse diameters of the remaining kidney over time (P<0.001). Out of 42 female donors, eleven female donors have got successful postdonation pregnancies. There were no reported surgical complications, either intra- or postoperative. Long-term follow-up is necessary for all living kidney donors through local institutional and world registries. This trial is registered with ClinicalTrials.gov NCT00813579.

Surface Enhanced Raman Spectroscopy (SERS) nanosensor for ultrasensitive detection of bromate in drinking water: State-of-the-art and prospective Khaled A. Mahmoud Qatar Environment & Energy Research Institute (QEERI), kmahmoud@qf.org.qa Sergey V. Gaponenko B. I. Stepanov Institute of Physics, National Academy of Sciences of Belarus, Minsk 220072 Belarus, s.gaponenko@ifanbel.bas-net.by The advances in Surface Enhanced Raman Spectroscopy (SERS) offer highly sensitive detection methods for monitoring drinking and potable water. The main experimental obstacle is the selective evaluation of a target pollutant in presence of the other pollutants. While single molecule detection is feasible in ultra-pure solutions with the known target molecules the trace detection of common pollutants in drinking and potable water remains a serious challenge. We consider the molecular recognition as the principal approach towards reliable development of plasmonic nanosensors for trace contaminations monitoring in water at the World Health Organization (WHO) prescribed levels. The molecular recognition approach has been recently shown to offer efficient selective analysis of certain target organic molecules in complex mixtures [4]. It is based on using specific binding of an additional agent (molecular compound) to the target molecules on complex solutions with the subsequent deposition of resulting conjugates on nanoplasmonic substrates and its Raman analysis. Specific binding can be tested additionally by predetermined modification of certain vibrational modes in conjugates as compared to free molecules. Desalinated water used in many countries including Qatar contains certain contaminants which does not present in ground water. Therefore analysts in these countries face the problem to develop affordable and reliable techniques for routine analysis of these contaminants in desalinated drinking and potable water. The representative examples are bromate, chlorate, and iodate anions. Bromate is supposed to possess carcinogenic properties with respect to humans and its content should thoroughly meet the WHO recommendation. We consider possible approaches to SERS sensor for trace level of bromate detection in desalinated drinking water. Herein we present novel analytical technique to trace bromate in drinking water based on novel molecular recognition and SERS sensor with detectability level improved by many orders of the magnitude. The novel and affordable technique for bromate detection in drinking water is expected to replace existing costly and bulky devices. This technique will offer bromate nanosensor test kit(s) to be used with the existing commercial Raman spectrometer and also will open an avenue towards portable desktop or even handheld bromate detection devices. The novel approach can be potentially foreseen to bromate extraction from drinking water. [1] S. V. Gaponenko, Introduction to Nanophotonics, Cambridge University, 2010. [2] K. Kneipp, M. Moskovits, H. Kneipp (Eds.) Surface-Enhanced Raman Scattering, Springer, 2006. [3] S. V. Gaponenko, D. V. Guzatov, Chem. Phys. Lett. 2009, 477, 411-414. [4] Kh. A. Mahmoud and M. Zourob, Analyst, 2013, 138, 2712-2719. [5] Bromate in Drinking-water, World Health Organization 2005.

The versatile multifunctional unreported pyridine-2,6-bis(2-cyano-N-phenyl-3-oxopropanethioamide) (3) was prepared starting from pyridine-2,6-bis-(3-oxopropanenitrile) (1). Several new series of polysubstituted thiophenes and 1,3,4-thiadiazoles incorporating 2,6-pyridine moiety were efficiently synthesized. The newly synthesized compounds were evaluated for their in vitro anticancer activity against human cancer cell lines: hepatocellular liver carcinoma (HEPG2) and Caucasian breast adenocarcinoma (MCF-7). Some of the newly synthesized compounds exhibited better activity than doxorubicin as a reference drug.

Synthesis, antimicrobial and anti-cancer activities of some newN-ethyl,N-benzyl andN-benzoyl-3-indolyl heterocyclesA series of 1-(N-substituted-1H-indol-3-yl)-3-arylprop-2-ene-1-ones (2a, b-4a, b) were prepared and allowed to react with urea, thiourea or guanidine to give pyrimidine derivatives5a, b-13a, b. Reaction of2a, b-4a, bwith ethyl acetoacetate in the presence of a base gave cyclohexanone derivatives14a, b-16a, b. Reaction of the latter compounds with hydrazine hydrate afforded indazole derivatives17a, b-19a, b. On the other hand, reaction of2a, b-4a, bwith some hydrazine derivatives, namely hydrazine hydrate, acetyl hydrazine, phenylhydrazine and benzylhydrazine hydrochloride, led to the formation of pyrazole derivatives20a, b-31a, b. Moreover, reaction of2a, b-4a, bwith hydroxylamine hydrochloride gave isoxazole derivatives32a, b-34a, b. The newly synthesized compounds were tested for their antimicrobial activity and showed that 4-(N-ethyl-1H-indol-3-yl)-6-(p-chlorophenyl)-pyrimidine-2-amine (11b) was the most active of all the test compounds towardsCandida albicanscompared to the reference drug cycloheximide. Eighteen new compounds, namely pyrimidin-2(1H)-ones5a, b-7a, b, pyrimidin-2(1H)-thiones8a, b-10a, band pyrimidin-2-amines11a, b-13a, bderivatives, were tested for theirin vitroantiproliferative activity against HEPG2, MCF7 and HCT-116 cancer cell lines. 4-(N-ethyl-1H-indol-3-yl)-6-(p-methoxyphenyl)-pyrimidin-2-amine (11a)was found to be highly active withIC50of 0.7 μmol L-1.

In the present study, versatile multifunctional unreported triazolo[1,5-a]quinoline derivatives were prepared. Compounds 1–19 were synthesized by adopting appropriate synthetic routes and were pharmacologically evaluated for their in vitro anticancer activity against human cancer cell lines: hepatocellular liver carcinoma (HEPG2) and Caucasian breast adenocarcinoma (MCF-7), in addition to their antibacterial and antifungal activities. Compound 4 demonstrated strong inhibitory effects against breast cancer (MCF-7), whereas compounds 8 and 19 exhibited moderate activity against breast carcinoma cell line MCF-7. Compounds 16 and 19 gave moderate activity against liver carcinoma cell line HEPG2. The antimicrobial activity of the prepared compounds was tested against bacteria and fungi. Among them, the results of antimicrobial activity indicated that compounds 4, 9, 11, 13, 15, 17, 18 and 19 were the most active compounds. Compound 4 exhibited strong activity against Fusarium sp., whereas compounds 9, 11, 15, 17, 18 and 19 showed high activity against Escherichia coli. More specifically, compound 17 displayed a high inhibitory effect against Bacillus cereus, Escherichia coli and Rhizoctonia sp.

A new fl avonoid C-glycoside, kaempferol 8-C-β-galactoside, along with twelve known glycosidic fl avonoids was isolated from the aqueous methanolic extract of Solanum elaeagnifolium Cav. (Solanaceae), by conventional chromatographic methods; their structure elucidation was achieved using UV, ESI-MS, and NMR spectral analyses. Groups of six mice were administered S. elaeagnifolium extracts at 25, 50, and 75 mg/kg body weight (BW) prior to or post administration of a single dose of paracetamol (500 mg/kg BW). The extract showed signifi cant hepatoprotective and curative effects against histopathological and histochemical damage induced by paracetamol in liver. The extract also ameliorated the elevation in glutamate oxaloacetate transaminase (GOT), glutamate pyruvate transaminase (GPT), and alkaline phosphatase (ALP) levels. These fi ndings were accompanied by a nearly normal architecture of the liver in the treated groups, compared to the paracetamol control group. As a positive control, silymarin was used, an established hepatoprotective drug against paracetamol-induced liver injury. This study provides the fi rst validation of the hepatoprotective activity of S. elaeagnifolium.