Synthesis,structure-activity relationship and molecular docking studies of 3-O-flavonol glycosides as cholinesterase inhibitors

The prime objective of this research work is to prepare readily soluble synthetic analogues of naturally occurring 3-O-flavonol glycosides and then investigate the influence of various substituents on biological properties of synthetic compounds. In this context, a series of varyingly substituted 3-O-flavonol glycosides have been designed, synthesized and characterized efficiently. The structures of synthetic molecules were unambiguously corroborated by IR, ¹H, ¹³C NMR and ESI-MS spectroscopic techniques. The structure of compound 22 was also analyzed by X-ray diffraction analysis. All the synthetic compounds (21–30) were evaluated for in vitro inhibitory potential against cholinesterase enzymes. The results displayed that most of the derivatives were potent inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with varying degree of IC₅₀ values. The experimental results were further encouraged by molecular docking studies in order to explore their binding behavior with the active pocket of AChE and BChE enzymes. The experimental and theoretical results are in parallel with one another.     

Protective effect of Spirulina platensis against cell damage and apoptosis in hepatic tissue caused by high fat diet

Spirulina platensis is a microalga that may be a source of antioxidants that can reduce body fat deposition. Consumption of a high fat diet produces elevated blood lipid levels, inflammation and apoptosis. We investigated the possible effects of S. platensis on the blood lipid profile, and liver inflammation and apoptosis in rats fed a high fat diet. Sixty-four young male rats were divided into eight equal groups. The control group was fed a basic diet. The experimental groups were fed a diet for 60 days that was prepared by mixing variable amounts of 43% vegetable oil and 10% cholesterol with or without 3% S. platensis mixed with the basal diet. Blood and liver tissue samples were collected from each animal. Serum samples were used to analyze lipid parameters, total antioxidant status and total oxidant status. iNOS and eNOS were determined by immunohistochemistry. TUNEL staining was used to detect apoptosis to investigate a possible connection between inflammation and apoptosis in the liver tissue. The relations between fat deposition and liver degeneration were assessed by Sirius red staining and alpha-smooth muscle actin immunostaining. S. platensis reduced serum HDL-C, LDL-C and triglyceride, increased HDL-C levels in rats fed a high fat diet to near control levels, and reduced iNOS levels and increased eNOS levels in the liver tissue compared to vegetable oil and cholesterol treated groups. The apoptotic index was reduced in the groups that were fed a high fat or a basic diet when supplemented with S. platensis.     

Sucrose-enhanced biosynthesis of medicinally important antioxidant secondary metabolites in cell suspension cultures of <Emphasis Type="Italic">Artemisia absinthium</Emphasis> L.

Natural products are gaining tremendous importance in pharmaceutical industry and attention has been focused on the applications of in vitro technologies to enhance yield and productivity of such products. In this study, we investigated the accumulation of biomass and antioxidant secondary metabolites in response to different carbohydrate sources (sucrose, maltose, fructose and glucose) and sucrose concentrations (1, 3, 5, 7 and 9 %). Moreover, the effects of 3 % repeated sucrose feeding (day-12, -18 and -24) were also investigated. The results showed the superiority of disaccharides over monosaccharides for maximum biomass and secondary metabolites accumulation. Comparable profiles for maximum biomass were observed in response to sucrose and maltose and initial sucrose concentrations of 3 and 5 %. Maximum total phenolic and total flavonoid contents were displayed by cultures treated with sucrose and maltose; however, initial sucrose concentrations of 5 and 7 % were optimum for both classes of metabolites, respectively. Following 3 % extra sucrose feeding, cultures fed on day-24 (late-log phase) showed higher biomass, total phenolic and total flavonoid contents as compared to control cultures. Highest antioxidant activity was exhibited by maltose-treated cultures. Moreover, sucrose-treated cultures displayed positive correlation of antioxidant activity with total phenolics and total flavonoids production. This work describes the stimulatory role of disaccharides and sucrose feeding strategy for higher accumulation of phenolics and flavonoids, which could be potentially scaled up to bioreactor level for the bulk production of these metabolites in suspension cultures of A. absinthium.     

Characterization ofAzospirillum and related diazotrophs associated with roots of plants growing in saline soils

Diazotrophs, especially of genusAzospirillum were readily isolated from roots of many plants using semi-solid nitrogen free malate medium (NFM). These isolates formed fine, white sub-surface pellicle in nitrogen-free malate medium within 24h, which gradually moved to the surface, and exhibited high acetylene reduction rates. Using selected cultural and biochemical tests, most of the isolates were identified asAzospirillum brasilense. Four isolates from Kallar grass root surface and one isolate fromAtriplex root interior formed phenotypically a homogenous group. It shared many characteristics with the species of genusAzospirillum except shape. All the biochemical tests performed, categorized them withA. brasilense. However, the shape and the protein profile on SDS polyacrylamide gel electrophoretograms suggested that the group of these five isolates is clearly distinct and differs widely from all the type strains, belonging to various genera.

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Résumé It est apparu facile d'isoler des diazotrophes, principalement du genreAzospirllium à partir de racines de nombreuses plantes et utilisant un milieu malate semisolide exempt d'azote (NFM). Ces isolats forment une pellicule fine et blanche sous la surface dans le milieu malate exempt d'azote, endéans les24h. Ces pellicules ae déplacent progressivement vers la surface et exhibent des vitesses élevées de production d'acétylène. L'emploi de tests de culture sélective ou biochimique, a permis d'identifier la plupart des isolats commeAzospirillum brasilense. Quatre isolats à partir de la surface des racines d'herbe Kallar et un isolat à partir de l'intérieur d'une racine d'Atriplex forment an groupe homogène sur le plan phénotypique. Celui-ci partage de nombreuses caractéristiques avec les espèces du genreAzospirillum excepté la forme. Tous les tests biochimiques exécutés les rangent avecA. brasilense. Toutefois, leur forme ainsi que le profil protéique sur un électrophérogramme sur gel de polyacrylamide-SDS suggèrent que le groupe de cinq isolats est nettement distinct et diffère largement de toutes les souches types, appartenant à de nombreux genres.

     

Joint mode selection and user association in D2D enabled multitier C-RAN

Cluster Computing - The device-to-device D-2-D Communication empowered Cloud Radio Access Network (CRAN) which is examined to be auspicious system model, gives energy efficiency and high data rate....     

Molecular and enzymatic characterizations of novel bifunctional 3beta-hydroxysteroid dehydrogenases/C-4 decarboxylases from Arabidopsis thaliana

We have isolated two cDNAs from Arabidopsis thaliana encoding bifunctional 3beta-hydroxysteroid dehydrogenase/C-4 decarboxylases (3betaHSD/D) involved in sterol synthesis, termed At3betaHSD/D1 and At3betaHSD/D2. Transformation of the yeast ergosterol auxotroph erg26 mutant, which lacks 3betaHSD/D activity, with the At3betaHSD/D1 isoform or with At3betaHSD/D2 isoform containing a C-terminal At3betaHSD/D1 endoplasmic reticulum-retrieval sequence restored growth and ergosterol synthesis in erg26. An in vitro enzymatic assay revealed high 3betaHSD/D activity for both isoenzymes in the corresponding microsomal extracts. The two At3betaHSD/D isoenzymes showed similar substrate specificities that required free 3beta-hydroxyl and C-4-carboxyl groups but were quite tolerant in terms of variations of the sterol nucleus and side chain structures. Data obtained with 4alpha-carboxy-cholest-7-en-3beta-ol and its 3alpha-deuterated analog revealed that 3alpha-hydrogen-carbon bond cleavage is not the rate-limiting step of the reaction. In planta reduction on the expression of the 3betaHSD/D gene as a consequence of VIGS-mediated gene silencing in Nicotiana benthamiana led to a substantial accumulation of 3beta-hydroxy-4beta,14-dimethyl-5alpha-ergosta-9beta,19-cyclo-24(24(1))-en-4alpha-carboxylic acid, consistent with a decrease in 3betaHSD/D activity. These two novel oxidative decarboxylases constitute the first molecularly and functionally characterized HSDs from a short chain dehydrogenase/reductase family in plants.     

Upper Cretaceous rudist biostratigraphy of the Bey Da?lar? Carbonate Platform, Western Taurides, SW Turkey

The Upper Cretaceous (Middle Cenomanian-Coniacian) successions of the Bey Da?lar? Carbonate Platform (Western Taurides, SW Turkey) are represented by rudist-bearing shallow-water limestones. Four rudist lithosomes are distinguished for the first time from the Eastern, Northern and Southern Areas of the Bey Da?lar? Autochthon. The oldest rudist assemblages dominated by caprinids are observed in the Eastern (Katran Da?) Area (caprinid lithosomes) and suggest a Middle-Late Cenomanian age. The uppermost part of the platform carbonates in the Northern Area is characterized by an association of hippuritid and radiolitid rudist bivalves dominated by Vaccinites praegiganteus (Toucas) (hippuritid lithosomes). The rudist fauna indicates the Late Turonian age, which is confirmed by the previously obtained ⁸⁷Sr/⁸⁶Sr values of well-preserved low-Mg calcite of Vaccinites praegiganteus (Toucas) shells. The rudist associations of the Southern (Susuzda?) Area are represented by two rudist formations. The lower lithosomes are mainly made up of hippuritids and radiolitids (hippuritid-radiolitid lithosomes). The stratigraphical distributions of the species of the assemblage indicate a Santonian-Early Campanian age. The rudist associations of the upper lithosomes are dominated by species of Joufia and Gorjanovicia (Joufia-Gorjanovicia lithosomes), which suggest a Late Campanian-Maastrichtian age. Identification of the rudist lithosomes yields information on the palaeobiogeographic distribution of the rudist species in the eastern Mediterranean region and also on the biostratigraphic frame of the Upper Cretaceous successions of the Bey Da?lar? Carbonate Platform.