One pot synthesis of new cross-linked chitosan-Schiff' base: Characterization, and anti-proliferative activities.

Four novel chitosan hydrogels were successfully synthesized through the cross-linking reaction of chitosan with different concentrations of ethyl 5-(3,5-dihydroxy-1,4-dioxan-2-yl)-2-methylfuran-3-carboxylate. Their structures were confirmed by Fourier transform infrared spectroscopy (FT-IR), 13C Cross polarization magic angle spinning nuclear magnetic resonance spectroscopy (CP/MAS 13C NMR), ultraviolet-visible spectroscopy, thermogravimetric analysis (TGA, DTA), and X-ray diffraction (XRD). Cytotoxicity on hepatocellular carcinoma (HepG-2) cell line and a normal African green monkey kidney (Vero) cell line were studied using the MTT assay. The resultant hydrogels showed a good inhibitory effect comparing to the un-modified parent; the hydrogels with the lowest degree cross-linking (0.125 and 0.25 mol cross-linker per one chitosan residue) showed potent anticancer activity in the HepG2 cells with IC50 of 57.9 and 80.9 µg/ml, respectively. These results show that the newly synthesized cross-linked chitosan derivatives demonstrated more selectivity to the HepG2 than the Vero cells, indicating its potential for Investigation in the cure of hepatocellular carcinoma.

In vitro biological activities and in vivo hepatoprotective role of brown algae-isolated fucoidans.

Brown seaweeds are rich in polysaccharides, such as fucoidan (FUC) which has shown beneficial effects in several medical conditions. The aim of the present study was to assess the antioxidant, anti-inflammatory, and hepatoprotective properties of Colpomenia sinuosa- and Sargassum prismaticum-isolated FUC in vitro and in vivo. The hot acid extraction method was used to isolate FUC from C. sinuosa (FCS) and S. prismaticum (FSP) species. The antioxidant, anticancer, as well as the effect on neurotransmitter-degrading enzyme and disaccharidase activities were measured using standard protocols. Moreover, the hepatoprotective effect of two FCS doses (100 and 200 mg/kg) on paracetamol-administered rats (one dose of 1 g/kg) were evaluated by measuring blood liver function markers, hepatic pro-oxidants as malondialdehyde (MDA) and nitric oxide (NO), antioxidants as glutathione (GSH) and glutathione peroxidase (GPx), proinflammatory markers as inducible nitric oxide synthase (iNOS), interleukin 1ß (IL-1ß), tumor necrosis factor-α (TNF-α), and liver histology. The crude fucoidan yield was 15.6% and 14.8% of C. sinuosa and S. prismaticum dry weights, respectively. The antioxidant effects and cytotoxic activity on hepatic cancer cell were higher for FCS than FSP. Moreover, in vivo data showed that FCS administration at both doses significantly improved liver functions and alleviated histological alterations, hepatic inflammation, and oxidative stress following paracetamol intake. In conclusion, fucoidan exerts anti-inflammatory, antidigestive enzyme activity, antioxidant, anticancer, and hepatoprotective effects.

Synthesis and characterization of chitosan-pyrazoloquinoxaline Schiff bases for Cr (VI) removal from wastewater.

Two novel chitosan Schiff bases namely chitosan pyrazolo[3,4-b]quinoxaline Schiff base (Ch-PQ1) and chitosan phenyl-1H-pyrazolo[3,4-b]quinoxaline Schiff base (Ch-PQ2) were synthesized as a modification of chitosan in order to increase its ability in heavy metal removal from wastewater. Their structures were characterized by FT-IR spectroscopy, TGA analysis and X-ray diffraction. They were tested for the removal of hexavalent chromium from synthetic samples. In addition pH conditions, polymer dosage, Cr (VI) initial concentration and contact time were studied as a key factor for the adsorption process. Kinetic studies of the removal process were also clarified. Furthermore, experimental equilibrium data were fitted to Langmuir and Freundlich adsorption isotherms. Both chitosan Schiff bases showed high removal efficiency, the result indicated that Cr (VI) removal using Ch-PQ1 and Ch-PQ2 was 96.4% and 98.8% respectively.

Cytotoxicity influence of new chitosan composite on HEPG-2, HCT-116 and MCF-7 carcinoma cells.

Chitosan/aroylhydrazine composite were synthesized in hydrogel form in which aroylhyrazines, heteroaroylhydrazines as well as p-tolylsulphonylhydrazine embedded in the cross linked Chitosan/oxalic acid network. Their structures were characterized by (elemental analysis, FT-IR, 1H NMR, and XRD). Antimicrobial behavior and Cytotoxicity screening of the examined compounds against breast, colon and hepatocellular cancer were investigated. The obtained data revealed that the examined compounds have promising cell growth inhibitory effect on the cell lines as compared to standard. Also, some of the newly synthesized derivatives had shown better antibacterial and antifungal activities, comparing with that of the parent chitosan.

Synthesis and Characterization of Glutamic-Chitosan Hydrogel for Copper and Nickel Removal from Wastewater.

Chitosan was reacted with four concentrations (2.5, 5, 10 and 20 mmol) of glutamic acid resulting in four types of glutamic-chitosan hydrogels (GCs), the activity of the resulted compounds on the removal of copper(II) and nickel(II) from wastewater were tested. The results indicated that by increasing glutamic acid concentration from GCs-1 to GCs-4, the efficiency of removing Cu(II) and Ni(II) were decreased, which may be due to a decrease in the pore size of the hydrogels as a result of the increased degree of crosslinking.

Antioxidant and antitumor activities of new synthesized aromatic C-nucleoside derivatives.

The carbohydrazide 1 was used as the precursor for the synthesis of a number of new aromatic C-nucleosides containing 1,3,4-oxadiazole 7, [1,3,4]oxadiazolo[2,3-a]isoindole 10b and pyrazole units 18. On the other hand, the thiosemicarbazone 20 was used as the key intermediate for synthesis of 1,3,4-oxadiazole  and 1,2,4-triazole-3-thione derivatives 21 and 23. The antioxidant activities of the prepared compounds were evaluated. The carbohydrazide 1 in particular was found to have potent antioxidant and antitumor activity.

Synthesis and bioassay of a new class of furanyl-1,3,4-oxadiazole derivatives.

Tyrosinase enzyme is a monophenol monoxygenase enzyme, which plays an important role in human as a rate limiting step enzyme for different specific metabolic pathways, as well as its useful application in industry and agriculture. So this study was carried out to test the effect of newly prepared compounds containing 1,3,4-oxadiazoles with different substituted groups on tyrosinase enzyme activity, hoping to use them in the treatment of some diseases arising from tyrosinase activity disorders such as Parkinson's disease, schizophrenia, autism, attention deficit, hyperactivity disorder, and cancer.

Synthesis of new 1,3,4-thiadiazole and 1,2,3,4-oxathiadiazole derivatives from carbohydrate precursors and study of their effect on tyrosinase enzyme.

5-(1,2,3,4-Tetrahydroxybutyl)-2-methylfuran-3-carbohydrazide (2) was condensed with a variety of ketones to afford carbohydrazide derivatives 3-6. Acetylation of 3-5 afforded the acetyl derivatives 7-9, while periodate oxidation of 3-6 afforded the formyl derivatives 10-13. Acid catalyzed condensation of thiosemicarbazide or o-tolylthiosemicarbazide with the prepared aldehydes 10-12 gave thiosemicarbazone derivatives 14-19. Cyclization of the latter with acetic anhydride afforded 4,5-dihydro-1,3,4-thiadiazolyl derivatives 20-25. On the other hand, condensation of p-tosylhydrazine with the prepared aldehydes 10-12 afforded p-tosylhydrazone derivatives 26-28. Cyclization of 26-28 with acetic anhydride afforded 1,2,3,4-oxathiadiazole derivatives 29-31 respectively. Moreover, the obtained results regarding to the effect of some of the prepared compounds on tyrosinase enzyme showed that the majority of these compounds having an inhibitory effect; especially compounds 12, 16, 17, and 28.