Synthesis of Some 2-Alkylated-5-Aminoimidazoles Related to Intermediates in Purine Nucleotide de novo and Thiamine Biosynthesis

Abstract

Routes to 2-alkylated-5-aminoimidazole nucleosides have been investigated in which the 2-substituent has up to 3 carbon atoms and capable of being interconverted into suitable oxy and 0x0 alkyl derivatives for use in enzyme inhibition and biochemical incorporation studies involving both purine nucleotide de novo and thiamine biosynthesis.     

An overview of malaria transmission from the perspective of Amazon Anopheles vectors

In the Americas, areas with a high risk of malaria transmission are mainly located in the Amazon Forest, which extends across nine countries. One keystone step to understanding the Plasmodium life cycle in Anopheles species from the Amazon Region is to obtain experimentally infected mosquito vectors. Several attempts to colonise Ano- pheles species have been conducted, but with only short-lived success or no success at all. In this review, we review the literature on malaria transmission from the perspective of its Amazon vectors. Currently, it is possible to develop experimental Plasmodium vivax infection of the colonised and field-captured vectors in laboratories located close to Amazonian endemic areas. We are also reviewing studies related to the immune response to P. vivax infection of Anopheles aquasalis, a coastal mosquito species. Finally, we discuss the importance of the modulation of Plasmodium infection by the vector microbiota and also consider the anopheline genomes. The establishment of experimental mosquito infections with Plasmodium falciparum, Plasmodium yoelii and Plasmodium berghei parasites that could provide interesting models for studying malaria in the Amazonian scenario is important. Understanding the molecular mechanisms involved in the development of the parasites in New World vectors is crucial in order to better determine the interaction process and vectorial competence.     

Lung tissue extracellular matrix-derived hydrogels protect against radiation-induced lung injury by suppressing epithelial–mesenchymal transition

This study aimed to examine whether lung tissue extracellular matrix (ECM) hydrogels have protective effects on radiation-induced lung injury (RILI). The cytocompatibility and histocompatibility were tested for the obtained ECM-derived hydrogel. Sprague–Dawley rats were randomly divided into three groups (n = 18): control group (control); rats receiving irradiation and intratracheal injection of normal saline (IR + NS); and rats receiving irradiation and intratracheal injection of lung ECM-derived hydrogel (IR + ECM). The wet/dry weight ratio was used to evaluate the congestion and edema of the lungs. Histopathological analysis of lung tissues was performed using hemotoxylin and eosin staining and Masson's trichrome staining. Immunohistochemical staining and western blot analyses were carried out to determine the expression of epithelial–mesenchymal transition (EMT)-related proteins in lung tissues (E-cadherin, α-smooth muscle actin [α-SMA], and vimentin). In addition, tumor necrosis factor-α (TNF-α), transforming growth factor-β1 (TGF-β1) and interleukin-6 (IL-6), hydroxyproline, malondialdehyde (MDA), and superoxide dismutase (SOD) levels were also evaluated. The ECM-derived hydrogels had good cytocompatibility and histocompatibility. ECM-derived hydrogel treatment improved lung histopathology injury and pulmonary edema. Higher expression of E-cadherin and lower expression of vimentin and α-SMA were found in the IR + ECM group compared with those in the IR + NS group. Hydroxyproline levels were reduced by ECM-derived hydrogel treatment compared with those in the IR + NS group. Obvious increases of TNF-α, IL-6, and TGF-β1 were identified following irradiation. Marked reductions in MDA content and increases in SOD were induced by ECM-derived hydrogel treatment in rats after radiation. ECM-derived hydrogels were shown to protect against RILI, potentially by reducing EMT, inflammation, and oxidative damage.     

Chemical characteristics and antioxidant activity of exopolysaccharide fractions from Microbacterium terregens

The Gram-positive bacterial strain isolated from soil was identified as the non-pathogenic Microbacterium terregens. The exopolysaccharide (CPS) produced from M. terregens was obtained by isopropanol precipitation (13.72 g L^?1 growth medium), The resulted exopolysaccharide was purified by chromatography on DEAE-cellulose and Sephacryl S-200 columns, when two polysaccharide fractions termed CPSI and CPSII were obtained. Structure features of CPSI and CPSII were investigated by a combination of chemical and chromatographic analyses, such as acid hydrolysis, methylation analysis, periodate oxidation–Smith degradation, HPLC, GC–MS, and IR. The results indicated that CPSI and CPSII were composed of glucose: mannose in a ratio of 2.7:1 and 3.2:1 with molecular weights 80 and 150 kDa, respectively. It has a backbone of (1 → 4)-linked β-glucose residues, which occasionally branches at O-6. The branches were composed of (1 → 4)-linked β-mannose residues. The antioxidant activity of the CPS, CPSI and CPSII was evaluated in-vitro by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay (RSA). CPSI fraction showed the highest antioxidant activity among the three fractions, with an IC₅₀ value of 230 μg mL^?1. The effect of molecular weight of the polysaccharide on the improvement of the antioxidant potential seems to be significant.     

Histopathology and cytotoxicity as biomarkers in treated rats with cadmium and some therapeutic agents

The present study aimed to investigate the protective role of ascorbic acid (vitamin C) and zinc (Zn) against cadmium (Cd) induced histopathological changes in tissues of liver, kidney, lung and testis of rats as well as chromosomal aberrations. For this purpose, 60 male albino rats were divided into six groups; each group contained 10 animals. The first group served as control and was given only distilled water. The second and third groups received distilled water supplemented with 2 g ascorbic acid/l and 500 mg Zn/l, respectively. The fourth group received a daily oral dose containing 3 mg Cd/kg b.w. (1/30 LD₅₀). The fifth group received Cd + ascorbic acid (3 mg Cd/kg b.w. + 2 g ascorbic acid/l), while the sixth group received Cd + Zn (3 mg Cd/kg b.w. +500 mg Zn/l). The treatment in all groups lasted for 90 consecutive days. Rats exposed to cadmium showed severe histopathological changes in the liver, kidney, lung and testicular tissues as well as chromosomal aberrations such as: break, ring, centromeric separation and polyploidy. Co-treatment with zinc partially improved the histopathological changes and chromosomal aberrations while co-treatment with vitamin C exhibited a more protective role and markedly reduced tissues damage induced by Cd.     

Neural networks in intestinal immunoregulation

Key physiological functions of the intestine are governed by nerves and neurotransmitters. This complex control relies on two neuronal systems: an extrinsic innervation supplied by the two branches of the autonomic nervous system and an intrinsic innervation provided by the enteric nervous system. As a result of constant exposure to commensal and pathogenic microflora, the intestine developed a tightly regulated immune system. In this review, we cover the current knowledge on the interactions between the gut innervation and the intestinal immune system. The relations between extrinsic and intrinsic neuronal inputs are highlighted with regards to the intestinal immune response. Moreover, we discuss the latest findings on mechanisms underlying inflammatory neural reflexes and examine their relevance in the context of the intestinal inflammation. Finally, we discuss some of the recent data on the identification of the gut microbiota as an emerging player influencing the brain function.     

Biocides formulation of essential oils having antimicrobial activity

Essential oils of fennel, peppermint, caraway, eucalyptus, geranium and lemon were tested for their antimicrobial activities against some plant pathogenic micro-organisms (Fusarium oxysporum, Alternaria alternate, Penicilium italicum Penicilium digitatum and Botyritus cinerea). Essential oils of fennel, peppermint, caraway were selected as an active ingredient for the formulation of biocides due to their efficiency in controlling the tested micro-organisms. Successful emulsifiable concentrates (biocides) were prepared from these oils using different emulsifiers (Emulgator B.L.M. Tween20 and Tween80) and different fixed oils (sesame, olive, cotton and soybean oils). Physico-chemical properties of the formulated biocide (spontaneous emulsification, emulsion stability test, cold stability and heat stability tests as well as viscosity, surface tension and pH) were measured. The prepared biocides were ready to be tested for application in a future work as a safe pesticide against different pathogens.     

Protocol of a prospective study on the diagnostic value of transcranial duplex scanning of the substantia nigra in patients with parkinsonian symptoms

Background  

Parkinson's disease (PD) is the second most common neurodegenerative disorder. As there is no definitive diagnostic test, its diagnosis is based on clinical criteria. Recently transcranial duplex scanning (TCD) of the substantia nigra in the brainstem has been proposed as an instrument to diagnose PD. We and others have found that TCD scanning of substantia nigra duplex is a relatively accurate diagnostic instrument in patients with parkinsonian symptoms. However, all studies on TCD so far have involved well-defined, later-stage PD patients, which will obviously lead to an overestimate of the diagnostic accuracy of TCD.     

Sorption and desorption of copper by and from clay minerals

Summary The sorption of Cu by different clay minerals from dilute CuSO₄ solutions was studied as a function of pH. It was found that Cu sorption increased with increasing the equilibrium pH. The low sorption at low pH values was attributed to the competition effect of H⁺ ions and the release of octahedral Mg, Fe and Al from the 2: 1 minerals in acid solutions. The higher sorption of copper at higher pH values was related to the absence of H⁺ ions and to the increase in the pH-dependent negative charge in kaolinite and gibbsite.The desorption of copper using solutions of 1 N NaCl at different pH values indicated that kaolinite and montmorillonite released large amounts of their adsorbed Cu even at high pH values. Vermiculite, on the other hand, exhibited a strong retention of Cu against extraction with NaCl. Oven-drying had no significant effect on the desorption characteristics of the Cu-saturated clays.The Ca-Cu exchange isotherms on montmorillonite were studied at two different pH values. The isotherms indicated a preference of Ca at the lower pH (pH 3.5), with K = 0.931 and G = +41.0 cal./mole. At the higher pH (5.2) the isotherms indicated a preference of Cu with K = 1.282 and G = –141.0 cal./mole. The difference was attributed to the competition of H⁺ at low pH.