Antitumor Activity of USP7 Inhibitor GNE-6776 in Non-Small Cell Lung Cancer Involves Regulation of Epithelial-Mesenchymal Transition, Cell Cycle, Wnt/β-Catenin, and PI3K/AKT/mTOR Pathways.

Non-small cell lung cancer (NSCLC) is a major cause of cancer-related deaths worldwide. This study investigated the effects and mechanisms of the USP7 inhibitor GNE-6776 on human NSCLC A549 and H1299 cells, providing insights for anti-NSCLC drug development. USP7 expression was analyzed in lung cancer tissue using data from public databases.

Dehydrocoupling of Ammonia/Amine Boranes and Related Transformations Catalysed by Group 4 Metal Complexes.

Ammonia borane and amine boranes are main group analogues of alkanes, which are characterised by their large gravimetric hydrogen content. This hydrogen can be released in dehydrocoupling and dehydropolymerisation reactions to obtain B-N oligomers and polymers that are of importance as precursors for functional B-N materials. Furthermore, amine boranes are potent reagents for application in transfer hydrogenation reactions, representing a versatile, easy-to-handle alternative to the use of gaseous hydrogen for the reduction of organic compounds.

Titanium-Catalyzed Reaction of Silacyclobutanes with Alkenes: Mimicking the Reactivity and Reversing the Selectivity Towards Late Transition Metals.

Transition metal-catalyzed ring opening and expansion reactions of silacyclobutanes (SCBs) constitute an atom- and step-economical strategy to construct value-added silicon-containing chemicals. Despite extensive studies, the reaction of SCBs with simple alkenes has only one precedent. Moreover, most reported reactions of SCBs use late transition metals (Pd, Ni, Rh) as catalysts.

Borane-Catalyzed Intermolecular Aryl Transfer between Hydrosilanes: Shifting the Equilibrium by Removal of a Gaseous Hydrosilane.

The preparation of organosilanes is indeed far from trivial, despite their vast application. Herein, we report a straightforward and general hydrosilane iterative evolution system for the on-demand synthesis of heteroleptic-substituted hydrosilanes. A series of previously difficult-to-prepare hydrosilanes with two or three diverse substituents were readily obtained.

Skeletal Editing of Aromatic N-Heterocycles via Hydroborative Cleavage of C-N Bonds-Scope, Mechanism, and Property.

Skeletal editing of the core structure of heterocycles offers new opportunities for chemical construction and is a promising yet challenging research topic that has recently gained increasing interest. However, several limitations of the reported systems remain to be addressed. For example, the reagents employed are generally in high-energy, such as chlorocarbene precursors, nitrene species, and metal carbenes, which are also associated with low atomic efficiencies.

Selective Hydroboration of C-C Single Bonds without Transition-Metal Catalysis.

Selective hydroboration of C-C single bonds presents a fundamental challenge in the chemical industry. Previously, only catalytic systems utilizing precious metals Ir and Rh, in conjunction with N- and P- ligands, could achieve this, ensuring bond cleavage and selectivity. In sharp contrast, we discovered an unprecedented and general transition-metal-free system for the hydroboration of C-C single bonds.

Zirconium and hafnium catalyzed C-C single bond hydroboration.

Selective cleavage and subsequent functionalization of C-C single bonds present a fundamental challenge in synthetic organic chemistry. Traditionally, the activation of C-C single bonds has been achieved using stoichiometric transition-metal complexes. Recently, examples of catalytic processes were developed in which use is made of precious metals.

Experimental-Computational Investigation of the Elastic Modulus of Mortar under Sulfate Attack.

External sulfate attack is an important factor causing a decrease in the mechanical properties of cement-based materials. In this paper, a computational prediction model of elastic modulus, considering the characteristics of sulfate corrosion from outside to inside and the influence of the interface transition zone (ITZ), was established to predict the elastic modulus of mortar under the external sulfate attack. Firstly, the backscattered electron (BSE) images of mortar and the algorithm of image threshold segmenting were used to determine a reasonable thickness of corroded ITZ.

Anion-substitution interfacial engineering to construct C@MoS hierarchical nanocomposites for broadband electromagnetic wave absorption.

Developing an effective strategy to regulate the interfacial properties of hierarchical structure is of great significance for preparation of high-performance electromagnetic wave absorption (EMA) materials. Ion-substitution can change intrinsic structure and properties of a materials, but its effect on the interfacial properties of hierarchical structure remained to be explored. Herein, we first constructed a C@MoS hierarchical structure via simple hydrothermal reaction, then used the ion-substitution strategy to replace the S atoms in MoS with O, F and Se, and finally obtained anion-substituted hierarchical structure (C@X-MoS, X = O, F, Se).

Si-B Functional Group Exchange Reaction Enabled by a Catalytic Amount of BH: Scope, Mechanism, and Application.

Functional group exchanges based on single-bond transformation are rare and challenging. In this regard, functional group exchange reactions of hydrosilanes proved to be more problematic. This is because this exchange requires the cleavage of the C-Si bond, while the Si-H bond is relatively easily activated for hydrosilanes.

Enhancing the stability, BBB permeability and neuroprotective activity of verbascoside in vitro using lipid nanocapsules in combination with menthol.

Verbascoside (VER) shows promising neuroprotective activity. However, the instability and low permeability in crossing the blood-brain barrier (BBB) greatly hinder its application. In the present study, verbascoside was encapsulated into lipid nanocapsules (LNC) by reverse micelle (RM) to increase its stability.

male flower as a remarkable edible floral resource exerts lifespan/healthspan-promoting effects on .

Natural products, especially phytochemicals, can effectively improve the health of various model organisms and ultimately prolong their lifespan. As an emerging resource of plant-based food, edible flowers have potential anti-aging effects. Here, we showed that twelve out of 30 drug-food homologous flowers' extracts significantly extended the lifespan of , and the male flower was screened out by comparing centrally.

Titanium-Catalyzed Exhaustive Reduction of Oxo-Chemicals.

Catalytic reduction of carboxylic acids and derivatives all the way to their corresponding methyl-compounds is very rare and still challenging for homogeneous transition-metal catalysis. Herein, we report an unprecedented and general catalytic exhaustive reduction of carboxylic functional group straightforwardly to a methyl group. This reaction was achieved using earth-abundant and readily available titanium as a catalyst.

Stigmasterol attenuates inflammatory response of microglia via NF-κB and NLRP3 signaling by AMPK activation.

Alzheimer's disease (AD) is the most common cause of dementia in the elderly. Although its pathogenesis remains unclear, studies have indicated microglia-mediated neuroinflammation playing an important role. Phytosterols are a class of natural compounds presented in food, and have anti-inflammatory abilities.

Visible-Light-Promoted Unsymmetrical Phosphine Synthesis from Benzylamines.

Herein, by applying visible-light photoredox catalysis, we have achieved the catalytic deaminative alkylation of diphenylphosphine and phenyl phosphine with benzylamine-derived Katritzky salts at room temperature. The use of Eosin Y as photoredox catalyst and visible light can largely promote the reaction. A series of unsymmetrical tertiary phosphines were successfully synthesized, including phosphines with three different substituents that are otherwise difficult to obtain.

Exploration of Osmanthus fragrans Lour.'s composition, nutraceutical functions and applications.

Osmanthus fragrans (Thunb.) Lour. has been cultivated in China for over 2500 years.

Site-Fixed Hydroboration of Terminal and Internal Alkenes using BX / Pr NEt*.

An unprecedented and general hydroboration of alkenes with BX (X=Br, Cl) as the boration reagent in the presence of Pr NEt is reported. The addition of Pr NEt not only suppresses alkene polymerization and haloboration side reactions but also provides an "H" source for hydroboration. More importantly, the site-fixed installation of a boryl group at the original position of the internal double bond is readily achieved in contrast to conventional transition-metal-catalyzed hydroboration processes.

Effects of soil amendments on fractions and stability of soil organic matter in saline-alkaline paddy.

Soil amelioration is an effective practice to alleviate the adverse effects of soil salinization. However, increasing the fertility of salt-affected soils has been challenging, particularly in coastal saline-alkaline paddy soils. Here, we carried out a 45-day incubation experiment to evaluate the impacts of soil amendments on fractions and stability of soil organic matter (SOM) in a saline-alkaline paddy.

Catalytic Boration of Alkyl Halides with Borane without Hydrodehalogenation Enabled by Titanium Catalyst.

An unprecedented and general titanium-catalyzed boration of alkyl (pseudo)halides (alkyl-X, X=I, Br, Cl, OMs) with borane (HBpin, HBcat) is reported. The use of titanium catalyst can successfully suppress the undesired hydrodehalogenation products that prevail using other transition-metal catalysts. A series of synthetically useful alkyl boronate esters are readily obtained from various (primary, secondary, and tertiary) alkyl electrophiles, including unactivated alkyl chlorides, with tolerance of other reducing functional groups such as ester, alkene, and carbamate.

Linking phytosterols and oxyphytosterols from food to brain health: origins, effects, and underlying mechanisms.

Phytosterols and their oxidation products, namely oxyphytosterols, are natural compounds present in plant foods. With increased intake of phytosterol-enriched functional food products, the exposure of both phytosterols and oxyphytosterols is rising. Over the past ten years, researches have been focused on their absorption and metabolism in human body, as well as their biological effects.

Natural P-gp inhibitor EGCG improves the acteoside absorption in Caco-2 cell monolayers and increases the oral bioavailability of acteoside in rats.

Acteoside is one of the most widespread phenylethanoid glycosides with pharmacological activities, including antioxidant, neuroprotective property, etc. However, its bioavailability is poor due to the low absorption and P-gp efflux. This study aimed to select food derived P-gp inhibitors for promoting the acteoside absorption and investigate whether the inhibitors could increase the bioavailability and stability of acteoside.

Visible-Light-Promoted Photoredox Dehydrogenative Coupling of Phosphines and Thiophenols.

Herein, by applying visible-light photoredox catalysis, we have now achieved the first example of catalytic dehydrogenative coupling of phosphines and thiophenols that proceeds at room temperature. Key to our success is the use of benzaldehyde as a soft oxidant, which avoids the issue of phosphine oxidation. Furthermore, we observed the unexpected dealkylative coupling of secondary and tertiary alkylphosphine with thiophenols.

Therapeutic potential of phenylethanoid glycosides: A systematic review.

Phenylethanoid glycosides (PhGs) are generally water-soluble phenolic compounds that occur in many medicinal plants. Until June 2020, more than 572 PhGs have been isolated and identified. PhGs possess antibacterial, anticancer, antidiabetic, anti-inflammatory, antiobesity, antioxidant, antiviral, and neuroprotective properties.

Facile fabrication of functional hydrogels consisting of pullulan and polydopamine fibers for drug delivery.

With the rapid development of biomedicine applications, more flexible and efficient fabrication strategies are required for drug delivery vehicles. Naturally resourced polymers have gained considerable attention for construction of drug carriers. Here, biocompatible hydrogel reservoir system (named PHG-PDA) based on pullulan and polydopamine (PDA) are designed and fabricated by one-pot incorporation of PDA fibers into pullulan hydrogel (PHG).

Zirconium-Catalyzed Atom-Economical Synthesis of 1,1-Diborylalkanes from Terminal and Internal Alkenes.

A general and atom-economical synthesis of 1,1-diborylalkanes from alkenes and a borane without the need for an additional H acceptor is reported for the first time. The key to our success is the use of an earth-abundant zirconium-based catalyst, which allows a balance of self-contradictory reactivities (dehydrogenative boration and hydroboration) to be achieved. Our method avoids using an excess amount of another alkene as an H acceptor, which was required in other reported systems.