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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.

International audience; The Coulomb excitation of Ru102 was performed with beams of C12 and O16 ions. The beam particles scattered at forward angles were momentum analyzed with a magnetic spectrograph. The resolution achieved enabled the populations of the 21+ state, the unresolved 22+/41+, and 24+/31−, doublets of states, and the 32− state to be determined as a function of the scattering angle. These populations are compared with gosia calculations, yielding B(E2;21+→01+)=41.5±2.3 W.u., B(E2;22+→01+)=1.75±0.11 W.u., B(E3;31−→01+)=31.5±3.5 W.u., and B(E3;32−→01+)=6.8±0.5 W.u. The B(E3;31−→01+) value is significantly larger than previously measured. The weakly populated 23+ state, presumed to be a member of the band built on the 02+ state, was observed clearly for a single angle only, and a fit to its population results in B(E2;23+→01+)=0.053±0.011 W.u. Using the known γ-ray branching ratios for the 23+ level, the B(E2;23+→02+) value is calculated to be 18±4 W.u., substantially less than the B(E2;21+→01+). This suggests that the deformation of the 02+ state is lower than that of the 01+ state. The results are compared with beyond-mean-field calculations with the Gogny-D1S interaction using the symmetry-conserving configuration-mixing method.

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.

More than 20 000 infants and children have a cardiac arrest per year in the United States. In 2015, emergency medical service���documented out-of-hospital cardiac arrest (OHCA) occurred in more than 7000 infants and children.

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.