Notes

Productive Cryopreservation regarding Inactive Buds regarding Blackcurrant (Ribes nigrum T.) by making use of Greenhouse-Grown Vegetation as well as in Vitro Healing.
Nanomaterials could be a robust candidate for the removal of an array of environmental contaminants in water.A lot of studies on spinel ferrites (MFe2O4, M = divalent metal ion) and their binary nanocomposites as photocatalysts in the decontamination of wastewater have been performed, because MFe2O4 nanoparticles are relatively stable, biocompatible and low-cost efficient photocatalyst. The separation of MFe2O4 photocatalyst is easy owing to its excellent magnetic behavior. With this background, the recent developments on photocatalytic performances of MFe2O4 based binary nanocomposites were comprehensively reviewed. Especially, a focus on MFe2O4/metal oxides, MFe2O4/carbon based materials, MFe2O4/polymers, MFe2O4/metal nanoparticles and MFe2O4/other compounds for the photocatalytic degradation of dyes, emerging contaminants and inorganic pollutants has been thoroughly given. The advantages of MFe2O4 based nanocomposites as photocatalysts were also discussed. In addition, the possible pathway of active free radical generation by these photocatalysts under visible and ultraviolet irradiation has been explained. A comparison of photocatalytic activities of MFe2O4 based binary nanocomposites with recent reports has been carried out. This review concludes that MFe2O4 based binary nanocomposites have potential capacity in water purification technology. Nevertheless, their practical utilization in water treatment plants still needs to be further studied.Cyanobacteria and their toxins present potential hazard to consumers of water from lakes, reservoirs and rivers, thus their removal via water treatment or at the source, is essential. Here, we report that alkyltrimethylammonium (ATMA) surfactants, such as octadecyltrimethylammonium (ODTMA) bromide, act as cyanocides that efficiently inhibit photosynthesis and growth of cyanobacteria. Green algae were found less sensitive than cyanobacteria to ATMA compounds. Fluorescence measurements and microscopic observations demonstrated that cyanobacteria cells (Aphanizomenon or Microcystis) disintegrate and lose their metabolic activity (photosynthesis) upon exposure to ATMA bromides (estimated ED50(1hr) ranged between 1.5 and 7 μM for ODTMA-Br or hexadecyltrimethylammonium (HDTMA) bromide). Other ATMA compounds, such as tetradecyltrimethylammonium (TDTMA) or dodecyltrimethylammonium (DDTMA) bromides had similar inhibitory effect but their toxicity to cyanobacteria (measured as ED50(1hr) for photosynthetic efficiency) decreased, as the length of the alkyl chain decreased. All ATMA compounds used in this study showed lower toxicity to green algae than to cyanobacteria. A toxicity mechanism for ATMA cations is proposed, based on real time fluorescence signals and on alteration of cell ultra-structure revealed by electron microscopy. The present study sheds light on the toxic effect of ATMA surfactants on cyanobacteria and its potential application for controlling the occurrence of cyanobacterial bloom in lakes, reservoirs or rivers to secure the safety of drinking water and to mitigate and manage bloom events.Solar light-active silver nanoparticle (Ag NP) and nonmetal nitrogen (N)-codoped zinc oxide (ZnON/Ag) nanocomposites were fabricated by a pulsed laser-assisted method. Simufilam N was considered as a promising candidate for tailoring the bandgap of ZnO due to the similar atomic radius as well as lower ionization energy and electronegativity compared to oxygen, which resulted in the formation of a shallow acceptor level in ZnO. Moreover, Ag NPs could enhance the optical properties of the ZnO materials as a consequence of the surface plasmon resonance (SPR) effect. The synthesized ZnON/Ag composite materials were characterized by X-ray diffraction (XRD), micro-Raman spectroscopy, X-ray photoelectron spectroscopy (XPS), field emission scanning electron microscopy (FE-SEM), high-resolution transmission electron microscopy (HR-TEM), energy-dispersive X-ray spectroscopy (EDS), UV-vis diffuse reflectance spectroscopy (UV-DRS), and photoluminescence (PL) analysis. The photocatalytic activity of the ZnON/Ag materials was evaluated for the efficient degradation of Rhodamine B (Rh.B) under solar light irradiation. The optimized ZnON/Ag-2 nanocomposite exhibited six times higher Rh·B degradation rate than pure ZnO. This was attributed to the enhanced absorption behavior in the solar region as well as the formation of the Schottky junction between ZnON and Ag NPs, which resulted in effective charge separation. In addition, the scavenger study revealed that •O2- radicals facilitated the degradation of Rh.B. The reusability test of the ZnON/Ag nanocomposite confirmed high photostability and efficiency of the material in each successive cycle. The present investigation illustrates a rational design of metal and nonmetal-codoped ZnO nanostructures employing a pulsed laser-assisted technique for effective application in photocatalytic remediation of wastewater.Bisphenol A (BPA), a typical endocrine disrupting chemical, widely exists in water and threatens human health. The degradation of BPA by ozone in water is limited by the gas-mass transfer due to the low solubility of ozone. In this study, a rotating packed bed (RPB) was employed to create a high gravity environment to intensify the ozone mass transfer and BPA degradation. The effects of operational parameters (rotation speed of RPB, pH of the solution, ozone concentration, BPA concentration, gas volumetric flow rate and liquid volumetric flow rate) on BPA degradation efficiency and overall volumetric mass transfer coefficient of ozone were investigated. The results show that RPB effectively promoted the ozone mass transfer and BPA degradation and can be used for the ozonation of micropollutants that have fast reaction rates with ozone. Quenching experiments suggest that both ozone and HO∙ participated in BPA degradation from acidic to alkaline environments. In addition, the effects of co-existing chemicals on BPA degradation efficiency were studied. The addition of H2O2 or Cl- had no obvious impact on BPA degradation; the addition of HCO3- is beneficial for BPA degradation while the addition of fulvic acid suppressed the degradation. These results indicate that the pH value, which affects the reaction rate between ozone and BPA, is a major factor to be considered during the ozonation of BPA in RPB.Even today, the role of the histamine H2 receptor (H2R) in the central nervous system (CNS) is widely unknown. In previous research, many dimeric, high-affinity and subtype-selective carbamoylguanidine-type ligands such as UR-NK22 (5, pKi = 8.07) were reported as H2R agonists. However, their applicability to the study of the H2R in the CNS is compromised by their molecular and pharmacokinetic properties, such as high molecular weight and, consequently, a limited bioavailability. To address the need for more drug-like H2R agonists with high affinity, we synthesized a series of monomeric (thio)carbamoylguanidine-type ligands containing various spacers and side-chain moieties. This structural simplification resulted in potent (partial) agonists (guinea pig right atrium, [35S]GTPγS and β-arrestin2 recruitment assays) with human (h) H2R affinities in the one-digit nanomolar range (pKi (139, UR-KAT523) 8.35; pKi (157, UR-MB-69) 8.69). Most of the compounds presented here exhibited an excellent selectivity profile towards the hH2R, e.g. 157 being at least 3800-fold selective within the histamine receptor family. The structural similarities of our monomeric ligands to pramipexole (6), a dopamine receptor agonist, suggested an investigation of the binding behavior at those receptors. The target compounds were (partial) agonists with moderate affinity at the hD2longR and agonists with high affinity at the hD3R (e.g. pKi (139, UR-KAT523) 7.80; pKi (157, UR-MB-69) 8.06). In summary, we developed a series of novel, more drug-like H2R and D3R agonists for the application in recombinant systems in which either the H2R or the D3R is solely expressed. Furthermore, our ligands are promising lead compounds in the development of selective H2R agonists for future in vivo studies or experiments utilizing primary tissue to unravel the role and function of the H2R in the CNS.With the aim to obtain potent adenosine A2A receptor (A2AR) ligands, a series of eighteen derivatives of 4-hydroxy-N-(4-methoxy-7-morpholin-4-yl-1,3-benzo[d]thiazol-2-yl)-4-methylpiperidine-1-carboxamide (SYN-115, Tozadenant) were designed and synthesized. The target compounds were obtained by a chemical building block principle that involved reaction of the appropriate aminobenzothiazole phenyl carbamates with either commercially available or readily synthesized functionalized piperidines. Their affinity and subtype selectivity with regard to human adenosine A1-and A2A receptors were determined using radioligand binding assays. Ki values for human A2AR ranged from 2.4 to 38 nM, with more than 120-fold selectivity over A1 receptors for all evaluated compounds except 13k which had a Ki of 361 nM and 18-fold selectivity. The most potent fluorine-containing derivatives 13e, 13g and 13l exhibited Ki values of 4.9 nM, 3.6 nM and 2.8 nM for the human A2AR. Interestingly, the corresponding values for rat A2AR were found to be four to five times higher. Their binding to A2AR was further confirmed by radiolabeling with 18F and in vitro autoradiography in rat brain slices, which showed almost exclusive striatal binding and complete displacement by the A2AR antagonist ZM 241385. We conclude that these compounds represent potential candidates for the visualization of the A2A receptor and open pathways to novel therapeutic treatments of neurodegenerative disorders or cancer.Alzheimer's disease (AD) is one of the most common types of dementia, especially in elderly, with an increasing number of people suffering from this disease worldwide. There are no available disease-modifying therapies and only four drugs are approved for the relief of symptoms. Currently, the therapeutic approach used for AD treatment is based on single target drugs, which are not capable to stop its progression. To address this issue, multi-target compounds, combining two or more pharmacophores in a single molecular entity, have gained increasing interest to deal with the multiple factors related to AD. The exact cause of AD is not yet completely disclosed, and several hallmarks have been associated to this neurodegenerative disease. Even though, the accumulation of both amyloid-β plaques (Aβ) and neurofibrillary tangles (NFTs) are fully accepted as the main AD hallmarks, being object of lots of research for early-stage diagnosis and pharmacological therapy. In this context, this review summarizes the state-of-the-art in the field of dual-target inhibitors of both Aβ and tau aggregation simultaneously, including the design and synthetic strategy of the dual-target compounds, as well as a brief structure-activity relationships (SAR) analysis.The discovery of natural specialized pro-resolving mediators and their corresponding receptors, such as formyl peptide receptor 2 (FPR2), indicated that resolution of inflammation (RoI) is an active process which could be harnessed for innovative approaches to tame pathologies with underlying chronic inflammation. In this work, homology modelling, molecular docking and pharmacophore studies were deployed to assist the rationalization of the structure-activity relationships of known FPR2 agonists. The developed pharmacophore hypothesis was then used in parallel with the homology model for the design of novel ligand structures and in virtual screening. In the first round of optimization compound 8, with a cyclopentane core, was chosen as the most promising agonist (β-arrestin recruitment EC50 = 20 nM and calcium mobilization EC50 = 740 nM). In a human neutrophil static adhesion assay, compound 8 decreased the number of adherent neutrophils in a concentration dependent manner. Further investigation led to the more rigid cycloleucines (compound 22 and 24) with improved ADME profiles and maintaining FPR2 activity.
Website: https://www.selleckchem.com/products/simufilam.html