Reactions of 3-(1-arylhydrazono-L-threo-2,3,4-trihydroxybutyl)-1-methyl-2-Quinoxalinones

The 1-methyl derivatives (3 and 4) of 3-(1-phenyl- (1) and 3-(1-p-bromophenylhydrazono-L-threo-2,3,4-trihydroxybutyl)-2-quinoxalinone (2) were prepared by methylation. Periodate oxidation of 3 gave 1-methyl-3-[1-(phenylhydrazono)glyoxal-1-yl]-2-quinoxalinone (5), which, on reduction with sodium borohydride, gave the corresponding 3-[2-hydroxy-1-(phenylhydrazono)ethyl] derivative (8). Reaction of 5 with hydroxylamine or benzoylhydrazine gave the corresponding 2-oxime (6) and 2-(benzoylhydrazone) (7), respectively. Acetic anhydride causes one molecule of 3 or 4 to undergo elimination of two molecules of water, with simultaneous acetylation and ring closure to afford pyrazoles 9 and 10, respectively. Pyrolysis of the triacetate of 3 led to the elimination of acetic acid from the sugar and the hydrazone residue, to give the 3-[5-(acetoxymethyl)-1-phenylpyrazol-3-yl] derivatives (9). Acetic acid was found to effect the same rearrangement, but without acetylation, of 1, 2, and 3 to give the 3-[5-(hydroxymethyl)] derivatives 11, 12, and 13, respectively. The structure of these pyrazoles was confirmed by a series of reactions, including methylation and acetylation. The n.m.r. and i.r. spectra of the compounds were investigated.     

The use of Opalina sudafricana in a biological test for diagnosing disordered metabolism of tryptophan in human subjects

Injections of urine of patients with bladder cancer linked with bilharziasis, simple urinary bilharziasis, ascariasis or ancylostomiasis, induced cyst formation found in Opalina sudafricana when injected into its host Bufo regularis. It is suggested that the carcinogenic tryptophan metabolites present in the injected urine reach the parasites in the recta of the experimental toads and stimulate them to divide mitotically to form small forms which eventually encyst. This test may be of a diagnostic help in detecting any abnormality in tryptophan metabolism in some human patients.     

Intake and digestibility in sheep fed on alkali-treated straw and concentrates,as complete diets or separate feeds

Twelve mature wethers were used in an experiment of change-over design to determine the effect of complete diet feeding on intake and digestibility of diets based on alkalitreated straw and a concentrate containing rolled barley and extracted soya bean meal. Two diets were used: D₁ with a 50:50, and D₂ with a 75:25 ratio of straw:concentrates on a dry matter basis. The straw and concentrates of each diet were given either separately (S) or as a complete diet (C). Complete diets gave a slightly, but not significantly higher intake (C, 86.5) and S, 82.5 g dry matter /kg W^0.75 per day). The separate method gave a significantly higher digestibility coefficient for dry matter (C, 62.2 and S, 65.5; P < 0.05) and for crude fibre (C, 57.2 and S, 62.5; P < 0.01). Water intake increased by 42.7 ml g^?1 Na derived from NaOH. There were no significant interactions between the method of feeding and the type of diet in intake and digestibility of the diets or in the intake of water.     

Enzymatic Engineering of Polysialic Acid on Cells in Vitro and in Vivo Using a Purified Bacterial Polysialyltransferase

In vertebrates, polysialic acid (PSA) is typically added to the neural cell adhesion molecule (NCAM) in the Golgi by PST or STX polysialyltransferase. PSA promotes plasticity, and its enhanced expression by viral delivery of the PST or STX gene has been shown to promote cellular processes that are useful for repair of the injured adult nervous system. Here we demonstrate a new strategy for PSA induction on cells involving addition of a purified polysialyltransferase from Neisseria meningitidis (PST_Nm) to the extracellular environment. In the presence of its donor substrate (CMP-Neu5Ac), PST_Nm synthesized PSA directly on surfaces of various cell types in culture, including Chinese hamster ovary cells, chicken DF1 fibroblasts, primary rat Schwann cells, and mouse embryonic stem cells. Similarly, injection of PST_Nm and donor in vivo was able to produce PSA in different adult brain regions, including the cerebral cortex, striatum, and spinal cord. PSA synthesis by PST_Nm requires the presence of the donor CMP-Neu5Ac, and the product could be degraded by the PSA-specific endoneuraminidase-N. Although PST_Nm was able to add PSA to NCAM, most of its product was attached to other cell surface proteins. Nevertheless, the PST_Nm-induced PSA displayed the ability to attenuate cell adhesion, promote neurite outgrowth, and enhance cell migration as has been reported for endogenous PSA-NCAM. Polysialylation by PST_Nm occurred in vivo in less than 2.5 h, persisted in tissues, and then decreased within a few weeks. Together these characteristics suggest that a PST_Nm-based approach may provide a valuable alternative to PST gene therapy.     

Profiling the Lipophilic Fractions of Pithecellobium dulce Bark and Leaves Using GC/MS and Evaluation of Their Antioxidant,Antimicrobial and Cytotoxic Activities

Pithecellobium dulce has been used in traditional medicine to treat various ailments owing to its restorative properties. The biological activities and chemical profiles of the lipophilic fraction of P. dulce bark and leaves were assessed herein. Fatty acid methyl esters (FAME) and unsaponifiable matter (USM) were prepared and analyzed by GC/MS. A total of 40 compounds were identified in the bark saponifiable fraction, whereas 9 compounds were annotated in the leaves. Palmitic acid methyl ester was the major compound identified accounting for 41.48 % of the bark and 19.03 % of the leaves composition. Besides, linolenic acid methyl ester (22.40 %) and linoleic acid (12.69 %) were annotated in the leaves saponifiable fraction. A total of 63 compounds were detected in the bark USM and 4 compounds were identified in the leaves. Phytol represented the major component in the leaves (52.57 %) followed by lupeol (20.68 %) and lupenone (8.60 %). Meanwhile, n‐dodecane dominated in the bark USM accounting for 24.69 % of the total composition. The leaves and bark lipophilic fractions revealed moderate antioxidant and antibacterial activities. Both extracts showed no antifungal activity. No cytotoxicity was observed for both lipophilic fractions. P. dulce offers a good source of antioxidant compounds that can be introduced to food and pharmaceutical industry.     

Investigations of the kinetic energy parameters of irradiated (La)‐doped phosphate glass

The current study characterizes and analyzes glow curves obtained from phosphate glass doped with different concentrations of lanthanum. Kinetic parameters of the glow curves obtained from beta‐irradiated phosphate glass samples doped with lanthanum were determined using a newly designed deconvoluted software. The obtained results from the analyses indicated that the glow curves of the phosphate glass samples were composed of five overlapping peaks. The activation energies of the five electron traps were located between 0.622 and 1.133 eV. The obtained kinetic parameters were evaluated using the designed software and another two methods and all revealed good agreement. The first three traps displayed non‐first‐order behaviour, while the two deep traps obeyed nearly first‐order kinetics.