Unorthodox synthesis, biological activity and DFT studies of novel and multifunctionalized naphthoxocine derivatives

A new promising protocol has been developed for the synthesis of scarce oxocine derivatives 3a–e and 6 through addition of amine-based nucleophiles such as hydroxylamine hydrochloride, primary amine and hydrazide to chromonylidene benzothiazol-2-ylacetonitrile 2 in refluxing dioxane under metal free reaction conditions in moderate to good yields. Other nitrogen nucleophiles such as piperidine, hydrazine and thiosemicarbazide failed to afford the corresponding oxocinols, and instead pyridine derivatives 7, 8 and 10 were obtained exclusively. Predictive study for the biological activities using PASS (prediction of activity spectra for biologically active substances) online software showed optimistic activities for oxocinols 3a–e in the treatment of cancer, influenza A and microbial infections. Additionally, DFT studies of oxocine derivatives 3a–e and 6 indicated the presence of required thermodynamics parameters for the application in dye-sensitized solar cells (DSSCs)

CHEMICAL COMPOSITION, CYTOTOXIC ACTIVITY AND ANTIMICROBIAL ACTIVITY OF ESSENTIAL OILS OF LEAVES AND BERRIES OF JUNIPERUS PHOENICEA L. GROWN IN EGYPT.

Hydrodistillation of berries and leaves of Juniperus phoenicea grown in Sinai yielded volatile oils in the yield of 0.36 and 1.96%, respectively. Using gas chromatography/mass spectrometry technique, fifty eight compounds were identified in berry oil representing 99.2% of the oil composition. -Pinene was the major compound in berry oil (39.30%) followed by sabinene (24.29%). Berry oil composed mainly of monoterpenoids which amounted to 90.53%, of which 72.85% was monoterpene hydrocarbons. The sesquiterpenoids accounted for about 8% of the total oil composition. Leaf oil was composed of about 66 compounds representing 99.16% of the total composition of the oil. -Pinene was the major constituent of leaf oil at concentration of 38.22%, followed by -cedrol (31.23%). The monoterpene hydrocarbon was the predominant chemical group (41.29%) followed by the oxygenated sesquiterpenes (32.21%). Both oils showed very high cytotoxic activities against all cell line tested. They showed equal activities against brain (0.6 g//ml) and cervix (5.0 g//ml) human cell lines, while berry oil was slightly more active than leaf oil against lung (0.6 and 0.7 /ml, respectively), liver (0.7 and 0.9 g//ml, respectively) and breast human cell lines (0.8 and 1.g//ml, respectively). The antimicrobial activity and minimum inhibitory concentration (MIC) of leaf and berry oils were also determined. The oils showed high activity against most of the tested strains

Synthesis of novel naphthalene-heterocycle hybrids with potent antitumor, anti-inflammatory and antituberculosis activities

Multitarget-directed drugs (hybrid drugs) constitute an efficient avenue for the treatment of multifactorial diseases. In this work, novel naphthalene hybrids with different heterocyclic scaffolds such as nicotinonitrile, pyran, pyranopyrazole, pyrazole, pyrazolopyridine, and azepine were efficiently synthesized via tandem reactions of 3-formyl-4H-benzo[h]chromen-4-one 1 with different nucleophilic reagents. Analysis of these hybrids using PASS online software indicated different predicted biological activities such as anticancer, antimicrobial, antiviral, antiprotozoal, anti-inflammatory, etc. By focusing on antitumor, anti-inflammatory, and antituberculosis activities, many compounds revealed remarkable activities. While 3c, 3e, and 3h were more potent than doxorubicin in the case of HepG-2 cell lines, 3a–e, 3i, 6, 8, 10, 11, and 12b were more potent in the case of MCF-7. Moreover, compounds 3c, 3h, 8, 10, 3d, and 12b manifested superior activity and COX-2 selectivity to the reference anti-inflammatory Celecoxib. Regarding antituberculosis activity, 3c, 3d, and 3i were found to be the most promising with MIC less than 1 mg mL–1. The molecular docking studies showed strong polar and hydrophobic interactions with the novel naphthalene-heterocycle hybrids that were compatible with experimental evaluations to a great extent

Medullary sponge kidney presenting in a neonate with distal renal tubular acidosis and failure to thrive: a case report

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A biochemical, theoretical and immunohistochemical study comparing the therapeutic efficacy of curcumin and taurine on T-2 toxin induced hepatotoxicity in rats

Introduction: Foodborne trichothecene T-2 Toxin, is a highly toxic metabolite produced by Fusarium species contaminating animal and human food, causing multiple organ failure and health hazards. T-2 toxins induce hepatotoxicity via oxidative stress causing hepatocytes cytotoxicity and genotoxicity. In this study, curcumin and taurine were investigated and compared as antioxidants against T-2-provoked hepatotoxicity.Methods: Wistar rats were administrated T-2 toxin sublethal oral dose (0.1 mg/kg) for 2 months, followed by curcumin (80 mg/kg) and taurine (50 mg/kg) for 3 weeks. Biochemical assessment of liver enzymes, lipid profiles, thiobarbituric acid reactive substances (TBARs), AFU, TNF-α, total glutathione, molecular docking, histological and immunohistochemical markers for anti-transforming growth factor-β1 (TGFβ1), double-strand DNA damage (H2AX), regeneration (KI67) and apoptosis (Active caspase3) were done.Results and Discussion: Compared to T-2 toxin, curcumin and taurine treatment significantly ameliorated hepatoxicity as; hemoglobin, hematocrit and glutathione, hepatic glycogen, and KI-67 immune-reactive hepatocytes were significantly increased. Although, liver enzymes, inflammation, fibrosis, TGFβ1 immunoexpressing and H2AX and active caspase 3 positive hepatocytes were significantly decreased. Noteworthy, curcumin’s therapeutic effect was superior to taurine by histomorphometry parameters. Furthermore, molecular docking of the structural influence of curcumin and taurine on the DNA sequence showed curcumin’s higher binding affinity than taurine.Conclusion: Both curcumin and taurine ameliorated T-2 induced hepatotoxicity as strong antioxidative agents with more effectiveness for curcumin

Some problems in the motion of gas bubbles

Imperial Users onl

Institutional Reform of Economic Legislation in Egypt

The relationship between institutional and economic reform has dominated the field of development research since the 1990s. However, there is unclarity on the significance of reform of institutions of legislation and representation (whether in the form of interest groups or other civil society organizations). Similarly, there is unclarity regarding the sequence of reform of such institutions. There are, for example, four unresolved contentions about institutional reform. (1) If economic reform partly means economic legislation, is it necessary to reform parliament even when economic legislation is mainly done by the executive? (2) If economic reform requires efficient allocation of resources, is it necessary to strengthen special interest groups and increase societal representation/participation, running the risk of increasing clientelistic lobbying? (3) If one is to answer both questions positively, how should the reformation of the institution of parliament and that of interest representation happen and (4) in which sequence? This study focuses on the institutional environment of economic law-making in Egypt in a decade of intensive economic reform. It highlights the phases that characterized the relationship between economic reform and economic legislation, uncovers the macro-political factors that influence the institution of legislation, and unravels the institutional weakness embedded in the informational base of legislation. The argument is that economic legislation involves an intricate process of judgement. This process of judgement may require redundant channels of information processing and opinion-making that go beyond a linear and simple expert-executive relationship. Hence, the institutional reform of parliament and of interest representation become necessary even in politico-economic systems where the executive is dominant. This study relies on analyses of parliamentary discussions of nine major economic laws between 1989 & 1997 as well as on opinion surveys and extensive interviews with parliamentarians and interest group representatives

Baker’s yeast induces apoptotic effects and histopathological changes on skin tumors in mice

The current study investigates the apoptotic effect of Baker’s yeast (Saccharomyces cerevisiae) on chemically-induced skin cancer in mice. Intra-tumoral treatment with yeast caused: increases in Ca2+ in skin homogenate, as well as modulation of the intrinsic/extrinsic pathways by downregulating Bcl-2 and FasL, upregulating Bax, and increasing the expression of cytochrome-c and caspases 9, 8, and 3. Histopathological changes were detected, including mild dysplasia, atypia, tumor regression, and absence of basaloid cell proliferation. No toxic effects were detected, as examined by histopathological, biochemical, and body weight analysis. These results show that yeast exerts anti-skin cancer activity, suggesting its possible use for treatment of human skin cancer