Effect of drugs on brain acetylcholine level in Gerbillus pyramidum

1. The quantitative estimation of total acetylcholine content in the whole brain tissue in normal Egyptian gerbil Gerbillus pyramidum, gives an average of 1.43 +/- 0.06 micrograms of acetylcholine chloride/g fresh brain tissue. 2. The brain acetylcholine level in Gerbillus pyramidum was generally found to vary with the changes induced in the brain activity by drugs. 3. Depressants caused a increase and convulsants a decrease in total brain acetylcholine level. 4. Phenytoin depressed the brain activity but lowered brain acetylcholine level.     

Synthesis of novel estrone analogs by incorporation of thiophenols via conjugate addition to an enone side chain

Functionalized estrogen analogs have received interest due to their unique and differing biological activity compared to their parent compounds. The synthesis of a new class of 3-methoxyestrone analogs functionalized at the C17 position possessing both alkyl and aryl substituted α,β-unsaturated ketones is described, along with their thiophenol conjugate addition products.     

Genetic variability of the tropical grasshopper Poecilocerus bufonius in Saudi Arabia

Electrophoresis for SDS-proteins and isoenzymes was applied to investigate the genetic variability within the tropical grasshopper Poecilocerus bufonius, which inhabits Saudi Arabia. Samples were selected from different localities that are encompassing the Sarawat Mountains in the west and An-Nafud desert in the north and middle. A range of 2 to 14 protein bands were recorded in the studied samples as measured by SDS-polyacrylamide gel electrophoresis, from which only two were common. The maximum number of protein bands has been recorded in the samples from the west and the minimum number has been recorded in the samples from the north and middle. Six arbitrary chosen enzymes were examined by native-polyacrylamide gel electrophoresis. They were peroxidase (Px), aldehyde oxidase (Ao), acid phosphatase (Acph), alcohol dehydrogenase (Adh), á and â ePsterase (Est). Fourteen presumptive gene loci and 26 polymorphic alleles have been recorded with the highest number of alleles in Taif and minimum number of alleles in Qassim. Adh, Px and Acph have not been recorded in samples from the localities of An-Nafud desert. The samples from Taif (Sarawat Mountains) were more genetically variable than the samples from other localities. Most of alleles were monomeric but only the Px-1 showed trimeric alleles in samples from Taif.     

Palaeolimnological responses of nine North African lakes in the CASSARINA Project to recent environmental changes and human impact detected by plant macrofossil, pollen, and faunal analyses

This paper presents multi-proxy palaeolimnological analyses from recent sediments in the nine CASSARINA lakes in northernmost Africa, three from each of Morocco, Tunisia, and Egypt. The lakes are diverse, ranging from hypersaline to brackish lagoons and fresh-water lakes from high to low conductivity and pH. The macrofossils analysed include fruits, seeds, and vegetative remains of plants, lagoon and fresh-water Mollusca, a range of other aquatic animals, and from one site in each country, Ostracoda and Foraminifera. The diverse macrofossils are multi-proxy indicators of environmental change, and demonstrate changes in response to human activities in the catchments of all the lakes. The three Egyptian Nile Delta lakes have received massive inputs of fresh-water due to modifications of the flow of the R. Nile culminating in the Aswan High Dam built in 1964. Elsewhere, water withdrawal is frequently a serious threat. One lake with high biodiversity in Morocco has been drained and cultivated, and a rare acid-water lake in Tunisia is in danger of drying up. The internationally famous Garaet El Ichkeul in Tunisia, which was so important for birds, has become permanently saline with a loss of diversity. All the lakes are affected by agricultural and/or urban run-off and are experiencing changes as a result of human activities. Several are in a marginally sustainable condition, whereas others are permanently damaged.     

Identification of Yeast Strains Isolated from Agricultural Soils for Releasing Potassium-bearing Minerals

Thirty-five yeast strains were isolated from soil samples that were collected from different locations in Upper Egypt. The purified isolates were screened for the release potassium from mica on Aleksandrov agar medium. Two yeast isolates (KSY-29 and KSY-33) showed an ability to solubilize potassium by inducing clear zones around their colonies. They were identified as Pichia anomala and Rhodotorula glutinis, respectively, based on PCR analysis of the ITSI-26S region that was amplified by NL1/NL4 species-specific primers. The amount of K released from muscovite mica in the broth culture of the yeast isolates was measured after 5, 10, 15 and 20 days of the incubation at 25°C. Both yeast isolates were very effective in releasing K of muscovite in broth culture, recording 8.11–13.21 μg/ml that were released from muscovite mica after 20 days of incubation. The inoculation of maize (Zea maize) plants with these yeast isolates under different K levels (25, 50 and 100% of recommended dose of potassium, RDK) as potassium sulfate was tested on growth and K uptake by these plants in the greenhouse. Significant increases (p < 0.05) in plant height, root and shoot dry weights as well as K uptakes by shoots and roots maize plants occurred through the inoculation with KSY-29 or KSY-33 isolates.     

Discovery of novel glycerolated quinazolinones from Streptomyces sp. MBT27

Actinobacteria are a major source of novel bioactive natural products. A challenge in the screening of these microorganisms lies in finding the favorable growth conditions for secondary metabolite production and dereplication of known molecules. Here, we report that Streptomyces sp. MBT27 produces 4-quinazolinone alkaloids in response to elevated levels of glycerol, whereby quinazolinones A (1) and B (2) form a new sub-class of this interesting family of natural products. Global Natural Product Social molecular networking (GNPS) resulted in a quinazolinone-related network that included anthranilic acid (3), anthranilamide (4), 4(3H)-quinazolinone (5), and 2,2-dimethyl-1,2-dihydroquinazolin-4(3H)-one (6). Actinomycins D (7) and X2 (8) were also identified in the extracts of Streptomyces sp. MBT27. The induction of quinazolinone production by glycerol combined with biosynthetic insights provide evidence that glycerol is integrated into the chemical scaffold. The unprecedented 1,4-dioxepane ring, that is spiro-fused into the quinazolinone backbone, is most likely formed by intermolecular etherification of two units of glycerol. Our work underlines the importance of varying the growth conditions for the discovery of novel natural products and for understanding their biosynthesis.

     

Comparative Study to Investigate the Effect of Meloxicam or Minocycline HCl In Situ Gel System on Local Treatment of Periodontal Pockets

In situ gelling formulations allow easy application to the target area. Gelation is induced by physiological stimuli at the site of application where the formula attains semisolid properties and exerts sustained drug release. In situ gelling formulations containing either 3% meloxicam (Mx) or 2% minocycline HCl (MH) were prepared for local application into the periodontal pockets. Gel formulations were based on the thermosensitive Pluronic^® (Pl) and the pH-sensitive Carbopol^® (C) polymers. C gels were prepared in combination with HPMC (H) to decrease its acidity. The total percent drug released from Pl formulae was 21.72% after 1 week for Mx and 85% after 3 days for MH. Their release kinetics data indicated anomalous non-Fickian behavior that could be controlled by both diffusion and chain relaxation. Addition of MH to C/H gels (1:2.5) resulted in liquefaction, followed by drug precipitation. Regarding C/H gel containing Mx, it showed a prolonged release rate up to 7 days with an initial burst effect; the kinetics data revealed Fickian-diffusion mechanism. The in vitro antibacterial activity studies for MH gel in Pl revealed that the drug released exceeded the minimum inhibitory concentration (MIC) of MH against Staphylococcus aureus ATCC 6538; placebo gel showed no effect on the microorganism. Clinical evaluation of Pl gels containing either Mx or MH showed significant improvement in chronic periodontitis patients, manifested by decrease in pocket depth and gingival index and increase in bone density.