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Background Thiazole and thiosemicarbazone derivatives are known to have potential anticancer activity with a mechanism of action related to inhibition of matrix metallo-proteinases, kinases and anti-apoptotic BCL2 family proteins. Materials and methods A novel three series of 5-(1-(2-(thiazol-2-yl)hydrazono)ethyl)thiazole derivatives were prepared in a one-pot three-component reaction using 2-(2-benzylidene hydrazinyl)-4-methylthiazole as a starting precursor. MS, IR, 1H-NMR and 13C-NMR were used to elucidate the structures of the synthesized compounds. Most of the synthesized products were evaluated for their in vitro anticancer screening against HCT-116, HT-29 and HepG2 using the MTT colorimetric assay. Results The results indicated that compounds 4c, 4d and 8c showed growth inhibition activity against HCT-116 with IC50 values of 3.80 ± 0.80, 3.65 ± 0.90 and 3.16 ± 0.90 μM, respectively, compared to harmine (IC50 = 2.40 ± 0.12 μM) and cisplatin (IC50 = 5.18 ± 0.94 μM) reference drugs. Also, compounds 8c, 4d and 4c showed promising IC50 values of 3.47 ± 0.79, 4.13 ± 0.51 and 7.24 ± 0.62 μM, respectively, against the more resistant human colorectal cancer (HT-29) cell line compared with harmine (IC50 = 4.59 ± 0.67 μM) and cisplatin (IC50 = 11.68 ± 1.54 μM). On the other hand, compounds 4d, 4c, 8c and 11c were the most active (IC50 values of 2.31± 0.43, 2.94 ± 0.62, 4.57 ± 0.85 and 9.86 ± 0.78 μM, respectively) against the hepatocellular carcinoma (HepG2) cell line compared with harmine (IC50 = 2.54 ± 0.82 μM) and cisplatin (IC50 = 41 ± 0.63 μM). The study also suggested that the mechanism of the anticancer action exerted by the most active compounds (4c, 4d and 8c) inside HCT-116 cells was apoptosis through the Bcl-2 family. Conclusion Thiazole scaffolds 4c, 4d and 8c showed anticancer activities in the micromolar range and are appropriate as a candidate for cancer treatment.

The exopolysaccharide (EPS) was produced by a halophilic bacterial strain isolated from marine sediments, Porto-Elsokhna Beach, Egypt. This isolate has been defined morphologically and physiologically and has been recognized by 16S rDNA as Bacillus axarquiensis NRC G6.This strain was deposited in the Gene Bank (http://www.ncbi.nlm.nih. gov) under the accession number of KU945823. The EPS produced was fractionated by precipitation and listed the primary fraction as EPSBa3. Through FT-IR and HPLC, further work attempted to elucidate the structural function of EPSBa3. The findings showed that EPSBa3 was an acidic EPS composed of glucuronic: mannose: galacturonic: glucose and xylose, respectively, in a molar ratio of 1:1:3:3:3. The proportion of uronic acid and sulfate was 13.9% and 7% respectively. The estimated median molecular weight (Mw) and molecular number (Mn) were 1.499 X106 and 1.29 X 106g / mol. In rats, the anti-inflammatory activity of exopolysaccharide (EPSBa3) was also explored using paw edema induced by carrageenan. EPSBa3 caused important anti-inflammatory effects on the carrageenan model by 50 mg/kg orally. In catalase (CAT) and superoxide dismutase (SOD) enzymes and GSH content, the EPSBa3 enhanced declines. In addition, the content of nitric oxide (NO), lipid peroxidation (LPO) and reactive oxygen species (ROS) arising from carrageenan-induced edema were considerably reduced following therapy with EPSBa3. In addition, the findings showed that interleukin-6 (IL-6) protein expression was decreased after EPSBa3 treatment leading to alleviate paw edema. These findings stated that to avoid inflammatory diseases, EPSBa3 could be utilized as a source of natural products.

Abdelwahed R Sayed,1,2 Sobhi M Gomha,3,4 Eman A Taher,5,6 Zeinab A Muhammad,5 Hesham R El-Seedi,6,7 Hatem M Gaber,5 Mahgoub M Ahmed8 1Department of Chemistry, Faculty of Science, KFU, Hofuf, Saudi Arabia; 2Department of Chemistry, Faculty of Science, Beni-suef University, Beni-suef, Egypt; 3Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt; 4Department of Chemistry, Faculty of Science, Islamic University in Almadinah Almonawara, Almadinah Almonawara 42351, Saudi Arabia; 5Department of Pharmaceutical Chemistry, National Organization for Drug Control and Research (NODCAR), Giza 12311, Egypt; 6Chemistry Department, Faculty of Science, El-Menoufia University, Shebin El-Kom 32512, Egypt; 7Division of Pharmacognosy, Department of Medicinal Chemistry, Uppsala University, Biomedical Centre, Uppsala SE-75123, Sweden; 8Molecular Drug Evaluation Department, National Organization for Drug Control and Research (NODCAR), Giza 12311, EgyptCorrespondence: Sobhi M Gomha Tel +20 100-164-9576Fax +20 25685799Email s.m.gomha@gmail.comBackground: Thiazole and thiosemicarbazone derivatives are known to have potential anticancer activity with a mechanism of action related to inhibition of matrix metallo-proteinases, kinases and anti-apoptotic BCL2 family proteins.Materials and Methods: A novel three series of 5-(1-(2-(thiazol-2-yl)hydrazono)ethyl)thiazole derivatives were prepared in a one-pot three-component reaction using 2-(2-benzylidene hydrazinyl)-4-methylthiazole as a starting precursor. MS, IR, 1H-NMR and 13C-NMR were used to elucidate the structures of the synthesized compounds. Most of the synthesized products were evaluated for their in vitro anticancer screening against HCT-116, HT-29 and HepG2 using the MTT colorimetric assay.Results: The results indicated that compounds 4c, 4d and 8c showed growth inhibition activity against HCT-116 with IC50 values of 3.80 ± 0.80, 3.65 ± 0.90 and 3.16 ± 0.90 μM, respectively, compared to harmine (IC50 = 2.40 ± 0.12 μM) and cisplatin (IC50 = 5.18 ± 0.94 μM) reference drugs. Also, compounds 8c, 4d and 4c showed promising IC50 values of 3.47 ± 0.79, 4.13 ± 0.51 and 7.24 ± 0.62 μM, respectively, against the more resistant human colorectal cancer (HT-29) cell line compared with harmine (IC50 = 4.59 ± 0.67 μM) and cisplatin (IC50 = 11.68 ± 1.54 μM). On the other hand, compounds 4d, 4c, 8c and 11c were the most active (IC50 values of 2.31± 0.43, 2.94 ± 0.62, 4.57 ± 0.85 and 9.86 ± 0.78 μM, respectively) against the hepatocellular carcinoma (HepG2) cell line compared with harmine (IC50 = 2.54 ± 0.82 μM) and cisplatin (IC50 = 41± 0.63 μM). The study also suggested that the mechanism of the anticancer action exerted by themost active compounds ( 4c, 4d and 8c) inside HCT-116 cells was apoptosis through theBcl-2 family.Conclusion: Thiazole scaffolds 4c, 4d and 8c showed anticancer activities in themicromolar range and are appropriate as a candidate for cancer treatment.Keywords: hydrazones, hydrazonoyl halides, cyclization, harmine, HCT-116, HepG2, HT-29 &nbsp

The present study investigated the effect of rutin on acrylamide (ACR) toxicity was evaluated in experimental animal rats. The rats were feeding on basal diet and received oral 20 mg/kg b.w of acrylamide with 100, 50 and 25 mg/kg w.t of rutin; others were received the acrylamide concentrations only. The present results showed that 8-hydroxydeoxy guanidine (8-OHdG), protein carbonyl (PC), reactive oxygen species (ROS), glutathione peroxidase (GPx), tumor necrosis factor- (TNF-α), nitric oxide (NO) myeloperoxidase (MPO), caspase-3, bax, P53 and cytochrome-C in liver tissues were increased in rats-treated with acrylamide. This effect of acrylamide was attenuated by rutin. In conclusion, rutin ameliorates hepatotoxicity induced by acrylamide in male albino rats. It can be recommend the use of rutin to mitigate the acrylamide concentration in food products.

Gravity currents are complex phenomena that occur in estuaries, and the complexity of these phenomena is even higher for tideless estuaries. To improve the process of understanding such phenomena, the three-dimensional TELEMAC3D modelling system was used to model the Nile estuary as an example of tideless estuaries. The nonhydrostatic simulation and the use of a complex turbulence model were necessary. The current mean flow conditions were modelled first; the results were then compared with three scenarios of sea level rise to study its impact. According to the model results, the salt wedge was not stagnant but fluctuated in cycle-like variations; the fluctuations were higher at the surface and smaller near the bottom, and at the end of the salt wedge, no fluctuations were noticed. The salt concentration and hence the density differs significantly throughout the salt wedge in the longitudinal direction as well as in the vertical direction. Changes in density in the lateral direction were also noticed; greater concentrations were at greater water depths for the same transverse section. The sea level rise caused greater saltwater intrusion inside the Nile and the greater the sea level rise, the more the intrusion increased. To maintain the current saltwater intrusion length without any increase, discharging additional water from the Edfina Barrage (the last barrage on Rosetta branch) could be used as a direct mitigation option; however, doing so, could have negative consequences on the water budget of the country.

The efficacy of the Insect growth regulator (IG R) teflubenzuron (Nomolt 50 ULV) was evaluated against desert locust (DL) nymphs (3rd and 4th instars) during two seasons (2008 and 2009). All experiments were carried out under semi-field conditions, on irrigated plots planted with millet, and large cages (2x2x1m) and bomas (2x6x1m) were erected to enclose the test insects. The IGR was applied by means of a battery driven hand held (Micro ULVA) sprayer either as direct spray on the nymphs or as a simulated barrier treatment. The impact of the IGR on the feeding rate of the nymphs was investigated as well. The IGR was tested at the recommended dose (450ml/ha), and at fractional doses (225, 112.5 and 56.25ml/ha) in combination with Metarhizium anisopliae (Green Muscle®) at 50g/ha and the pheromone Phenyl Aceto Nitrile (PAN) 98% at 10ml/ha. Diesel was used as a dilutant in all formulations. Nomolt 450 m/ha resulted in 100% nymphal mortality in 20 days after treatment. The fractional doses of the IGR combined with the pheromone PAN, proved to be effective in the manipulation of nymphs, 100% mortality was obtained in 21, 20 and 21 days after treatment, in both seasons of the study. The fractional doses of the IGR combined with Metarhizium GM resulted in 100% mortality within 14 days of the treatment. Tests in bomas using barrier treatment in the 1 st season of the study revealed that the recommended dose of Nomolt applied on the nymphs resulted in 72.5, 88.5, 89 and 53% mortality after the 1 st , 6 th , 12 th and 24 th day after treatment respectively. Percentage mortality of 78.5, 68.5, 74 and 61.5 were achieved in the 2 nd season. The Nomolt either alone or in combined with PAN and GM revealed a clear negative impact on the feeding rate of nymphs.

The Second International Symposium on Flash Floods in Wadi Systems: 25-27 October 2016. Technische Universität Berlin, Campus El Gouna, Egypt.