Dynamic Enamine-one Bond Based Vitrimer via Amino-yne Click Reaction.

Here, we report the fabrication of a dynamic enamine-one bond based vitrimer through amino-yne click chemistry. In contrast to amine-acetoacetate condensation, the amino-yne click reaction yields a dynamic enamine-one motif that is composed of / (3:1) isomers and has a relatively lower activation energy (35 ± 3 kJ/mol vs 59 ± 6 kJ/mol), owing to the absence of a methyl substituent. The resulting vitrimer network has superior mechanical properties and faster dynamic exchange than that of a reference vitrimer derived from amine-acetoacetate condensation, and they are attributed to the fewer network defects and the less sterically hindered exchange reaction, respectively.

Solvothermal synthesis of octahedral and magnetic CoFeO-reduced graphene oxide hybrids and their photo-Fenton-like behavior under visible-light irradiation.

We report a facile solvothermal synthesis of novel octahedral CoFeO-reduced graphene oxide (RGO) hybrid and pure CoFeO that were used as heterogeneous photo-Fenton catalysts for the degradation of organic dyes in water. We investigated the structures, morphologies and catalytic activity of both the CoFeO nanoparticles and CoFeO-RGO hybrids. The morphology of CoFeO nanoparticles displays size-dependent shapes changing from granular (or sheet) to octahedral shapes with the introduction of RGO.

Functional Characterization of Hydrophilic X2 Modules in the Cellulosomal Scaffolding Protein.

As part of free cellulases or scaffolding proteins in cellulosomes, the hydrophilic non-catalytic X2 module is widely distributed in cellulolytic or other bacteria. Previous biochemical studies suggest that X2 modules might increase the solubility and substrate binding affinity of X2-bearing proteins. However, their biological functions remain elusive.

Lotus seedpods biochar decorated molybdenum disulfide for portable, flexible, outdoor and inexpensive sensing of hyperin.

Biomass waste, a good candidate for advanced carbon materials for sustainable electrodes, is receiving more and more attention for high value-added materials because of its promising contribution to economic growth and sustainable development. We proposed a green co-hydrothermal approach to prepare lotus seedpods biochar (BC) decorated molybdenum disulfide (MoS) from waste lotus seedpods and precursors of MoS and a portable, flexible, outdoor and inexpensive sensing platform for hyperin on the integrated flexible three-electrode using U-disk potentiostat with smartphone was successfully developed. Structure and properties of MoS-BC were characterized, it was proved that BC improves microstructure and morphology, electronic conductivity, electrode stability and electrocatalytic properties of MoS.

A high-quality assembly reveals genomic characteristics, phylogenetic status, and causal genes for leucism plumage of Indian peafowl.

Background: The dazzling phenotypic characteristics of male Indian peafowl (Pavo cristatus) are attractive both to the female of the species and to humans. However, little is known about the evolution of the phenotype and phylogeny of these birds at the whole-genome level. So far, there are no reports regarding the genetic mechanism of the formation of leucism plumage in this variant of Indian peafowl.

An updated patent review of small-molecule ROS1 kinase inhibitors (2015-2021).

Introduction: C-ros oncogene 1 (ROS1) is the sole member of the ROS1 receptor tyrosine kinase (ROS1-RTK) family, which is involved in the formation of non-small cell lung cancer (NSCLC), gastric adenocarcinoma, colorectal cancer, and other malignant tumors. At present, only crizotinib was approved for the treatment of advanced ROS1-positive NSCLC, and there have been reports of ROS1 mutations resulting in drug resistance. Consequently, it is necessary to develop new generations of inhibitors to overcome the existing problems.

Improved highly efficient Dion-Jacobson type perovskite light-emitting diodes by effective surface polarization architecture.

Quasi-two-dimensional (quasi-2D) perovskites are emerging as promising materials for highly stable light-emitting diodes (LEDs). However, their lower charge transport mobilities and higher defect densities may constrain their light-emitting efficiency. Here, we combine an excessive-salt-assisted (ESA) process with antisolvent treatments to inhibit the defects in Dion-Jacobson-type perovskite LEDs.

Effects of ultrasonic treatment on color, carotenoid content, enzyme activity, rheological properties, and microstructure of pumpkin juice during storage.

Freshly squeezed pumpkin juice (Cucurbita moschata D.) was sonicated at various power levels at a constant frequency of 25 kHz and a treatment time of 10 min. Samples were stored in the dark for 0, 4, 8, and 12 days at 4 °C and were subsequently analyzed.

Adsorption of Transition-Metal Clusters on Graphene and N-Doped Graphene: A DFT Study.

Using the dispersion-corrected density functional theory (DFT-D3) method, we systematically studied the adsorption of 15 kinds of transition-metal (TM) clusters on pristine graphene (Gr) and N-doped graphene (N-Gr). It has been found that TM ( = 1-4) clusters adsorbed on the N-Gr surface are much stronger than those on the pristine Gr surface, while 3d series clusters present similar geometries on Gr and N-Gr surfaces. The most preferred sites of TMs migrate from hollow to bridge to the top site on the Gr surface along the d series in the periodic table, while the preferred sites of TMs migrate in a much more complex manner on the N-Gr surface.

Indole-Based Tubulin Inhibitors: Binding Modes and SARs Investigations.

Tubulin inhibitors can interfere with normal cell mitosis and inhibit cell proliferation through interfering with the normal structure and function of microtubules, forming spindle filaments. Indole, as a privileged pharmacological skeleton, has been widely used in anti-cancer inhibitors. A variety of alkaloids containing an indole core obtained from natural sources have been proven to inhibit tubulin polymerization, and an ever-increasing number of synthetic indole-based tubulin inhibitors have been reported.

Synthesis, bioevaluation and molecular dynamics of pyrrolo-pyridine benzamide derivatives as potential antitumor agents in vitro and in vivo.

A total of 27 novel pyrrolo-pyridine benzamide derivatives were designed, synthesized and biologically evaluated. 14 of these derivatives were superior to Cabozantinib in cytotoxic assay, and compound 21 exhibited the best antitumor effect in vitro and vivo. Apoptosis activity was implemented by compound 21 on A549 cells, especially for the greatly enhanced late apoptosis compared with the control group (8.

Design, synthesis and anticancer evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 1,8-naphthyridine-3-carboxamide moiety as novel multi-target TKIs.

Giving the fact that the disorders of multiple receptor tyrosine kinases (RTKs) are characteristics of various cancers, we assumed that developing novel multi-target drugs might have an advantage in treating the complex cancers. Taking the multi-target c-Met inhibitor Foretinib as the leading compound, we discovered a novel series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 1,8-naphthyridine-3-carboxamide moiety with the help of molecular docking. Among them, the most promising compound 33 showed a prominent activity against Hela (IC = 0.

Research Progress on Cordycepin Synthesis and Methods for Enhancement of Cordycepin Production in .

is an insect-born fungus that belongs to and . It has a variety of biological activities that can be applied in medicine, health-care products, cosmeceuticals and other fields. Cordycepin (COR) is one of the major bioactive components identified from .

Silver-mediated radical oxytrifluoromethylation of unsaturated carboxylic acids for the synthesis of γ-trifluoromethylthio lactones.

An efficient silver-mediated oxidative trifluoromethylthiolation of unsaturated carboxylic acids to construct trifluoromethylthiol-containing lactones has been disclosed. In this protocol no metal-catalysts was added, and preliminary mechanism investigations suggested that a free-radical pathway should be involved in the process. High functional group tolerance and excellent yields were demonstrated by the efficient preparation of a wide range of γ-trifluoromethylthiolated phthalides.

Improving effect of cordycepin on insulin synthesis and secretion in normal and oxidative-damaged INS-1 cells.

Diabetes mellitus (DM) has recently become one of the major diseases that have received attention. Cordycepin (molecular formula: CHNO), is one of the major bioactive components of Cordyceps militaris, decreases blood glucose levels. In this study, the effect and mechanism of cordycepin in normal and oxidative-damaged INS-1 cells were explored by using cell and molecular biology methods.

Biomineralized Cascade Enzyme-Encapsulated ZIF-8 Nanoparticles Combined with Antisense Oligonucleotides for Drug-Resistant Bacteria Treatment.

The unrestrained use of antibiotics accelerates the development of drug-resistant bacteria and leads to an increasing threat to human health. Therefore, there is an urgent need to explore novel and effective strategies for the treatment of bacterial infections. Herein, zeolite imidazole framework-8 (ZIF-8) material was utilized to construct biomineralized nanomaterial (GOx&HRP@ZIF-8/ASO) by encapsulating biological cascade enzymes and combining with antisense oligonucleotides (ASOs), which achieved effective and synergistic antidrug-resistant bacteria therapy.

Regulation of DNA-binding activity of the Staphylococcus aureus catabolite control protein A by copper (II)-mediated oxidation.

Catabolite control protein A (CcpA) of the human pathogen Staphylococcus aureus is an essential DNA regulator for carbon catabolite repression and virulence, which facilitates bacterial survival and adaptation to a changing environment. Here, we report that copper (II) signaling mediates the DNA-binding capability of CcpA in vitro and in vivo. Copper (II) catalyzes the oxidation of two cysteine residues (Cys216 and Cys242) in CcpA to form intermolecular disulfide bonds between two CcpA dimers, which results in the formation and dissociation of a CcpA tetramer of CcpA from its cognate DNA promoter.

Synthesis and biological evaluation of ruthenium polypyridine complexes with 18β-glycyrrhetinic acid as antibacterial agents against .

Four new ruthenium(II) polypyridine complexes bearing 18β-glycyrrhetinic acid derivatives, [Ru(bpy)L](PF) (Ru1), [Ru(dmb)L](PF) (Ru2), [Ru(dtb)L](PF) (Ru3) and [Ru(phen)L](PF) (Ru4) (bpy = 2,2-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine, dtb = 4,4'-di--butyl-2,2'-bipyridine, phen = 1,10-phenanthroline and L is the GA modified new ligand) were designed and synthesized. Their antimicrobial activities against () were evaluated and all complexes showed an obvious inhibitory effect, especially, the minimum inhibitory concentration (MIC) value of Ru2 was 3.9 μg mL.

Green synthesis of kudzu vine biochar decorated graphene-like MoSe with the oxidase-like activity as intelligent nanozyme sensing platform for hesperetin.

It is an urgent need to exploit a potentially green, cost efficient and eco-friendly strategy for the utilization of waste kudzu vine. We developed a one-step green preparation of kudzu vine biochar (BC) decorated graphene-like molybdenum selenide (MoSe) with the oxidase-like activity as intelligent nanozyme sensing platform for voltametric detection of hesperetin (HP) in orange peel using the in-situ hydrothermal synthesis method. The structure and properties of MoSe-BC was characterized, and found that BC significantly improved electrochemical cycle stability, electronic conductivity, electrochemical active area, and electrocatalytic activity of MoSe.

Cordycepin suppresses glutamatergic and GABAergic synaptic transmission through activation of A adenosine receptor in rat hippocampal CA1 pyramidal neurons.

Cordycepin (known as 3-deoxyadenosine, CRD), a natural product from the valuable traditional Chinese medicine Cordyceps militaris, has been reported to improve cognitive function and modulate neuroprotective effects on the central nervous system (CNS). However, the modulating mechanisms of cordycepin on information processing in hippocampal CA1 pyramidal neurons are not fully understood. To clarify how cordycepin modulates synaptic responses of pyramidal neurons in rat hippocampal CA1 region, we conducted an electrophysiological experiment using whole-cell patch-clamp technique.

An updated patent review of small-molecule c-Met kinase inhibitors (2018-present).

Introduction: c-Met tyrosine kinase receptor is a high-affinity ligand of hepatocyte growth factor (HGF). c-Met is widely expressed in a variety of normal human tissues, but shows abnormally high expression, amplification or mutation in tumour tissues such as lung, gastric and breast cancers. Therefore, the use of c-Met as a target can achieve the inhibition of a series of abnormal physiological processes such as tumourigenesis, development and metastasis.

A Galactosidase-Activatable Fluorescent Probe for Detection of Bacteria Based on BODIPY.

Pathogenic infection is one of the most widespread foodborne diseases, so the development of sensitive, reliable and easy operating detection tests is a key issue for food safety. Identifying bacteria with a fluorescent medium is more sensitive and faster than using chromogenic media. This study designed and synthesized a -galactosidase-activatable fluorescent probe BOD-Gal for the sensitive detection of .

TRPM7 is critical for short-term synaptic depression by regulating synaptic vesicle endocytosis.

Transient receptor potential melastatin 7 (TRPM7) contributes to a variety of physiological and pathological processes in many tissues and cells. With a widespread distribution in the nervous system, TRPM7 is involved in animal behaviors and neuronal death induced by ischemia. However, the physiological role of TRPM7 in central nervous system (CNS) neuron remains unclear.

Whole-genome resequencing reveals genetic structure and introgression in Pudong White pigs.

Pudong White (PDW) pigs, historically originating from Shanghai, are the only Chinese indigenous pigs characterised by their completely white coats, with the exception of Rongchang pigs. However, there is limited information concerning their overall genetic structure or relationship with other breeds, especially the East Chinese (ECN) and European pigs. To uncover the genetic structure, selection signatures, and potential exotic introgression in PDW pigs, we sampled 15 PDW pigs using whole-genome sequencing (~20×).