Flavonols and 4-thioflavonols as potential acetylcholinesterase and butyrylcholinesterase inhibitors: Synthesis,structure-activity relationship and molecular docking studies

To explore new scaffolds for the treat of Alzheimer’s disease appears to be an inspiring goal. In this context, a series of varyingly substituted flavonols and 4-thioflavonols have been designed and synthesized efficiently. All the newly synthesized compounds were characterized unambiguously by common spectroscopic techniques (IR, ¹H-, ¹³C NMR) and mass spectrometry (EI-MS). All the derivatives (1–24) were evaluated in vitro for their inhibitory potential against cholinesterase enzymes. The results exhibited that these derivatives were potent selective inhibitors of acetylcholinesterase (AChE), except the compound 11 which was selective inhibitor of butyrylcholinesterase (BChE), with varying degree of IC₅₀ values. Remarkably, the compounds 20 and 23 have been found the most potent almost dual inhibitors of AChE and BChE amongst the series with IC₅₀ values even less than the standard drug. The experimental results in silico were further validated by molecular docking studies in order to find their binding modes with the active pockets of AChE and BChE enzymes.     

Inhibition of deleterious chronic wound enzymes with plant polyphenols

The chronic wound environment is characterized by high concentrations of reactive oxygen species (ROS) and elevated levels of myeloperoxidase (MPO) and collagenases, together impairing the healing process. Therefore, the management of chronic wounds at a molecular level requires the synergistic use of antioxidants, MPO and collagenase inhibitors to simultaneously target multiple factors from wound pathogenesis. In this study, a polyphenolic extract from Hamamelis virginiana plant, rich in condensed and hydrolysable oligomeric tannins, was evaluated as an inhibitor of MPO and collagenase. In addition to efficient scavengers of radical and non-radical reactive species, H. virginiana polyphenols were found to act as substrates in the MPO peroxidase cycle, preventing the accumulation of ROS in the chronic wound site. Furthermore, it was also found that the plant exerts an irreversible inhibitory effect on collagenase activity (IC₅₀ = 75 ± 10 μg/mL).     

Synthesis, characterization and photophysical properties of mixed ligand tris(polypyridyl)chromium(III) complexes, [Cr(phen)2L]

A series of new heteroleptic, tris(polypyridyl)chromium(III) complexes, [Cr(phen)₂L]³⁺ (L = substituted phenanthrolines or bipyridines), has been prepared and characterized, and their photophyical properties in a number of solvents have been investigated. X-ray crystallography measurements confirmed that the cationic (3+) units contain only one ligand L plus two phenanthroline ligands. Electrochemical and photophysical data showed that both ground state potentials and lifetime decays are sensitive to ligand structure and the nature of the solvent with the exception of compounds containing L = 5-amino-1,10-phenanthroline (aphen) and 2,2′-bipyrimidine (bpm). Addition of electron-donating groups in the ligand structure shifts redox potentials to more negative values than those observed for the parent compound, [Cr(phen)₃]³⁺. Emission decays show a complex dependence with the solvent. The longest lifetime was observed for [Cr(phen)₂(dip)]³⁺ (dip = 4,7-diphenylphenanthroline) in air-free aqueous solutions, τ = 273 μs. Solvent effects are explained in terms of the affinity of hydrophobic complexes for non-polar solvent molecules and the solvent microstructure surrounding chromium units.     

Bioavailability of two organic forms of zinc in comparison to zinc sulphate for weaning pigs fed a diet composed mainly of wheat,barley and soybean meal

This study was performed to compare the bioavailability of two organic zinc compounds, a zinc glycinate complex and a zinc amino acid chelate with that of zinc sulphate in growing pigs fed a basal diet composed mainly of wheat, barley and soybean meal. The experiment included 96 pigs with an average body weight of 8 kg, allotted to ten groups of nine to ten pigs each. The first group received the basal diet, containing 42 mg of native zinc per kg, without zinc supplementation over a period of five weeks. The other nine groups received the basal diet supplemented with 15, 30 or 50 mg of zinc/kg as zinc sulphate, zinc glycinate or the zinc amino acid chelate. Pigs fed the unsupplemented diet had a lower growth performance (body weight gain, feed conversion ratio) than the other nine groups. Supplementation of 15 mg zinc/kg diet (irrespective of zinc form) was sufficient to yield optimum growth performance. Plasma zinc concentration and activity of alkaline phosphatase were rising with increasing zinc supplementation levels up toa maximum reached at a supplementary level of 30 or 50 mg/kg diet for activity of alkaline phosphatase and plasma zinc concentration, respectively. The response of those parameters to zinc supplementation did, however, not differ between thethree zinc compounds considered. The apparent digestibility of zinc from the diet was also not different for the three zinc compounds. In conclusion, these findings show that the bioavailability of the two organic zinc compounds did not differ from that of zinc sulphate in growing pigs fed a diet with wheat, barley and soybean meal as major components.     

ECOPHYSIOLOGY OF TROPICAL RHODOPHYTES. I. MICROSCALE ACCLIMATION IN PIGMENTATION1,2

Microscale pigment adjustments to a tropical photosynthetically active radiation and ultraviolet (UV) environment by the intertidal turf algae Ahnfeltiopsis concinna (J. Ag.) Silva et DeCew and Laurencia mcdermidiae (J. Ag) Abbott were promoted by thalli densities that self-shade the under story portions of the same diminutive axes. Tissues of A. concinna from canopy microsites had significantly reduced levels of phycoerythrin, phycocyanin, and allophycocyanin compared to tissues from understory microsites of the same axes. Tissues of L. mcdermidiae from canopy microsites had reduced levels of only phycoerythrin compared to tissues from understory microsites. These alterations coupled with enhanced levels of carotenoid and UV-absorbing compounds in tissues from canopy compared to tissues from understory microsites indicated a pattern of remarkably sensitive photoacclimation over the ≤10-cm axes of these turf-forming rhodophytes. Microscale variation in the in vivo UV absorbance capabilities for turfs of A. concinna and L. mcdermidiae was directly related to the amount of extractable UV-absorbing compounds. An in vivo absorbance signature at ～345 nm appears to provide a method to quickly and accurately gauge the potential UV-shielding capacity of primary producers even at remarkably fine ecological scales. The capacity for highly responsive biochemical adjustments that result in marked canopy–understory distinctions coupled with a turf morphology may be crucial for macroalgal tolerance of physiological stresses associated with tropical intertidal zones. This responsive capacity allows for enhanced photoprotective mechanisms in tissues from canopy microsites while optimizing irradiance capture in deeply shaded tissues from understory microsites < 10 cm away.     

Characterization of Polar and Non‐Polar Compounds of House Edible Bird's Nest (EBN) from Johor,Malaysia

This work investigated the polar (PC: protein, amino acid and metabolite) and non‐polar (NPC: fatty acid) compounds and bioactivity characteristics of the EBN harvested from the state of Johor in Malaysia. The electrophoretic gels exhibited 15 protein bands (16–173 kD) with unique protein profile. Amino acids analysis by AccQ?Tag method revealed 18 types of amino acids in EBN. Metabolite profiling was performed using High‐Performance Liquid Chromatography coupled with Quadrupole Time‐of‐Flight Mass Spectrometer (HPLC‐QTOF/MS) technique and a total of 54 compounds belonging to different groups were detected and identified. These findings help to uncover the relation of therapeutic activity of EBN. The EBN was further extracted with AcOEt and BuOH. The AcOEt extract was fractionated into three fractions (F₁?F₃), and the high triglyceride content in F₂ was verified by gC‐FID. The three groups of fatty acids discovered in EBN are 48.43 % of poly‐unsaturated (PUFA), 25.35 % of saturated fatty acids (SFA) and 24.74 % of mono‐unsaturated fat (MUFA). This is the first time to report results ofEBN, BuOH, and AcOEt extracts and of fraction F₂ (TEBN) on their analysis for their antioxidant activities by DPPH, ABTS and catalase assay and for their paraoxonase and anti‐tyrosinase activities. The results showed that TEBN exhibited the significant bioactivity in all assays. These findings suggest that TEBN is a good source for natural bioactive compounds in promoting body vigor. Current work widened the content of EBN especially on the triglyceride and also marked the content of specific location (Johor, Malaysia) of EBN origin.     

Chemical Composition and Antioxidant Activity of Essential Oil of Chinese Propolis

The chemical composition and in vitro antioxidant activity of the essential oil of propolis (EOP) collected from 25 locations in China was investigated. Steam‐distillation extraction was used to extract the EOP, and chemical composition was identified by GC/MS. The antioxidant activities of EOP were also measured. The result showed that a total of 406 compounds were detected in EOP. The major compounds of Chinese EOP were cedrol, γ‐eudesmol, benzyl alcohol, phenethyl alcohol, 2‐methoxy‐4‐vinylphenol, 3,4‐dimethoxystyrene and guaiol. Principal component analysis revealed the significant correlation between EOP compositions and their origins, and certain correlation was detected between EOP and their color. Linear discriminant analysis showed that 88 % and 84 % of the propolis samples were predicted correctly as the groupings identified by climatic zone and the color, respectively. Furthermore, the differences of antioxidant activities of EOP were significant. EOP of Shandong had the strongest antioxidant activities, whereas EOP of Guangdong, Yunnan and Hunan showed the poorest.     

Half‐Heusler Thermoelectric Module with High Conversion Efficiency and High Power Density

Half‐Heusler (HH) compounds have shown great potential in waste heat recovery. Among them, p‐type NbFeSb and n‐type ZrNiSn based alloys have exhibited the best thermoelectric (TE) performance. However, TE devices based on NbFeSb‐based HH compounds are rarely studied. In this work, bulk volumes of p‐type (Nb_0.8Ta_0.2)_0.8Ti_0.2FeSb and n‐type Hf_0.5Zr_0.5NiSn_0.98Sb_0.02 compounds are successfully prepared with good phase purity, compositional homogeneity, and matchable TE performance. The peak zTs are higher than 1.0 at 973 K for Hf_0.5Zr_0.5NiSn_0.98Sb_0.02 and at 1200 K for (Nb_0.8Ta_0.2)_0.8Ti_0.2FeSb. Based on an optimal design by a full‐parameters 3D finite element model, a single stage TE module with 8 n‐p HH couples is assembled. A high conversion efficiency of 8.3% and high power density of 2.11 W cm^?2 are obtained when hot and cold side temperatures are 997 and 342 K, respectively. Compared to the previous TE module assembled by the same materials, the conversion efficiency is enhanced by 33%, while the power density is almost the same. Given the excellent mechanical robustness and thermal stability, matchable thermal expansion coefficient and TE properties of NbFeSb and ZrNiSn based HH alloys, this work demonstrates their great promise for power generation with both high conversion efficiency and high power density.