Catalytic remodeling of complex alkenes to oxonitriles through C=C double bond deconstruction.

Deconstructive transformation of carbon-carbon double bonds (C=C) is a pivotal strategy in synthetic chemistry and drug discovery. Despite the substantial advances in olefin metathesis and ozonolysis for natural product synthesis through C=C double-bond cleavage, the catalytic remodeling of complex molecules through C=C double-bond deconstruction has been underdeveloped. We report a heterogeneous copper-catalyzed C=C double-bond cleavage, which enables the remodeling of complex molecules by converting the carbons on either side of the C=C double bond to carbonyl and cyano groups, respectively.

Changes of metabolic parameters, antioxidant capacity, and gut microbiota in response to substitution of ferrous sulfate with iron hydroxy methionine analog chelate in weaned piglets.

Introduction: Previous studies have suggested that dietary organic iron offers health advantages compared to its inorganic counterpart. However, the effects of iron hydroxy methionine analog chelate (Fe-HMA) supplementation in weaned piglets have not been fully explored. Therefore, this study aimed to investigate the effects of replacing ferrous sulfate with Fe-HMA as the iron source on serum biochemistry, antioxidant capacity, and gut microbiota in weaned piglets.

Molecular Ring Remodeling through C-C Bond Cleavage.

ConspectusStable and inert C-C bonds form the fundamental framework of organic compounds. Consequently, direct transformations involving C-C bond cleavage present an innovative approach for the rapid modification and remodeling of molecular skeletons. In recent years, the concept of molecular skeletal editing has garnered widespread attention and has been significantly developed, providing new opportunities for the late-stage modification of bioactive molecules, the high-value transformation of bulk chemicals, and a revolution in the traditional fragment coupling strategies of chemical synthesis.

Alleviating effects of dietary formic acid polymer supplementation on lipopolysaccharide-induced inflammatory injury in gut-liver axis of broilers.

A close interplay exists between the gut and liver, known as the "gut-liver axis", which plays a vital role in health and disease. This research aimed to explore the effects of dietary formic acid polymer (FAP) addition on inflammatory injury in gut-liver axis of broilers due to lipopolysaccharide (LPS) challenge. Four hundred and fifty 1-day-old male Arbor Acres broilers were assigned to three treatment groups: (1) control (non-challenged, basal diet); (2) LPS (LPS-challenged, basal diet); (3) LPS+FAP (LPS-challenged, basal diet with 1,000 mg/kg FAP).

Safety and efficacy of inclisiran in treating hypercholesterolemia: A systemic review and meta-analysis.

Aims: To evaluate the efficacy and safety of inclisiran in the treatment of hypercholesterolemia.

Date Synthesis: Randomized controlled trials comparing inclisiran with a placebo were searched until April 2024. Overall, 8 studies involving 4947 patients were included.

Mechanical properties of discarded shield residue improved by calcium carbide slag and fly ash as subgrade filling.

To utilize discarded shield residue and alleviate the shortage of subgrade filling, industrial wastes such as calcium carbide slag (CCS) and fly ash (FA) were considered to enhance the mechanical properties of the shield residue. A series of laboratory tests, including California Bearing Ratio (CBR) tests, unconfined compressive strength (UCS) tests, moisture content tests, pH tests, water stability tests, and dry-wet cycles tests were performed on discarded shield residue with additive contents. The results show that the UCS and CBR values enhanced significantly with the increase in curing time.

Liver transplantation for hepatocellular carcinoma: a proposal for including preoperative serological indicators improves the Milan criteria expanded.

Background: Liver transplantation (LT) is the most effective and radical treatment for hepatocellular carcinoma (HCC). Most LT criteria are based on the morphological characteristics of tumors, which are not enough to predict the risk of tumor recurrence. It is found that some serological biomarkers can predict tumor recurrence and may be a good indicator for selecting suitable HCC patients for LT.

Direct oxygen insertion into C-C bond of styrenes with air.

Skeletal editing of single-atom insertion to basic chemicals has been demonstrated as an efficient strategy for the discovery of structurally diversified compounds. Previous endeavors in skeletal editing have successfully facilitated the insertion of boron, nitrogen, and carbon atoms. Given the prevalence of oxygen atoms in biologically active molecules, the direct oxygenation of C-C bonds through single-oxygen-atom insertion like Baeyer-Villiger reaction is of particular significance.

Effects of Dietary Supplementation with Cocrystals of Thymol and Carvacrol on Quality, Nutrient Composition, and Oxidative Stability of Broiler Meat.

Consumer demand for high-quality meat has increased. This study aimed to investigate the potential application of cocrystals of thymol and carvacrol in broilers for high-quality meat production. Eight hundred 1-day-old chicks were assigned to four groups fed diets supplemented with 0, 40, 60, and 80 mg/kg of Crystal EO (CEO), containing 25% cocrystals of thymol and carvacrol in a 42-d feeding trial.

Late-Stage Halogenation of Complex Substrates with Readily Available Halogenating Reagents.

ConspectusLate-stage halogenation, targeting specific positions in complex substrates, has gained significant attention due to its potential for diversifying and functionalizing complex molecules such as natural products and pharmaceutical intermediates. Utilizing readily available halogenating reagents, such as hydrogen halides (HX), N-halosuccinimides (NXS), and dichloroethane (DCE) reagents for late-stage halogenation shows great promise for expanding the toolbox of synthetic chemists. However, the reactivity of haleniums (X, X = Cl, Br, I) can be significantly hindered by the presence of various functional groups such as hydroxyl, amine, amide, or carboxylic acid groups.

Selective Upcycling of Polyolefins into High-Value Nitrogenated Chemicals.

The selective upcycling of polyolefins to create products of increased value has emerged as an innovative approach to carbon resource stewardship, drawing significant scientific and industrial interest. Although recent advancements in recycling technology have facilitated the direct conversion of polyolefins to hydrocarbons or oxygenated compounds, the synthesis of nitrogenated compounds from such waste polyolefins has not yet been disclosed. Herein, we demonstrate a novel approach for the upcycling of waste polyolefins by efficiently transforming a range of postconsumer plastic products into nitriles and amides.

Selective nitrogen insertion into aryl alkanes.

Molecular structure-editing through nitrogen insertion offers more efficient and ingenious pathways for the synthesis of nitrogen-containing compounds, which could benefit the development of synthetic chemistry, pharmaceutical research, and materials science. Substituted amines, especially nitrogen-containing alkyl heterocyclic compounds, are widely found in nature products and drugs. Generally, accessing these compounds requires multiple steps, which could result in low efficiency.

Effects of Chinese Gallotannins on Antioxidant Function, Intestinal Health, and Gut Flora in Broilers Challenged with Lipopolysaccharide.

This experiment was conducted to study the protective effects of dietary Chinese gallotannins (CGT) supplementation against lipopolysaccharide (LPS)-induced intestinal injury in broilers. Four hundred and fifty healthy Arbor Acres broilers (one-day-old) were randomly divided into three groups: (1) basal diet (CON group), (2) basal diet with LPS challenge (LPS group), and (3) basal diet supplemented with 300 mg/kg CGT as well as LPS challenge (LPS+CGT group). The experiment lasted for 21 days.

Lysine 2-hydroxyisobutyrylation levels determined adipogenesis and fat accumulation in adipose tissue in pigs.

Background: Excessive backfat deposition lowering carcass grade is a major concern in the pig industry, especially in most breeds of obese type pigs. The mechanisms involved in adipogenesis and fat accumulation in pigs remain unclear. Lysine 2-hydroxyisobutyrylation (Khib), is a novel protein post-translational modification (PTM), which play an important role in transcription, energy metabolism and metastasis of cancer cells, but its role in adipogenesis and fat accumulation has not been shown.

Research progress on GPX4 targeted compounds.

Blocking the System X GSHGPX4 pathway to induce ferroptosis in tumor cells is a novel strategy for cancer treatment. GPX4 serves as the core of the System Xc-/GSH/GPX4 pathway and is a predominant target for inducing ferroptosis in tumor cells. This article summarizes compounds identified in current research that directly target the GPX4 protein, including inhibitors, activators, small molecule degraders, chimeric degraders, and the application of combination therapies with other drugs, aiming to promote further research on the target and related diseases.

Carbene-Assisted Arene Ring-Opening.

Despite the significant achievements in dearomatization and C-H functionalization of arenes, the arene ring-opening remains a largely unmet challenge and is underdeveloped due to the high bond dissociation energy and strong resonance stabilization energy inherent in aromatic compounds. Herein, we demonstrate a novel carbene assisted strategy for arene ring-opening. The understanding of the mechanism by our DFT calculations will stimulate wide application of bulk arene chemicals for the synthesis of value-added polyconjugated chain molecules.

Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation.

Farnesoid X receptor (FXR) is a bile acids receptor and plays a crucial role in regulating bile acids, lipids, and glucose metabolism. Previous research suggests that inhibiting FXR activation can be beneficial in reducing cholesterol and low-density lipoprotein cholesterol (LDL-C) levels, offering potential treatment options for metabolic syndrome with lipid disorders. Herein, we report p-acetylaminobenzene sulfonate derivatives as a novel scaffold of FXR antagonists by multistage screening.

Late-stage modification of bioactive compounds: Improving druggability through efficient molecular editing.

Synthetic chemistry plays an indispensable role in drug discovery, contributing to hit compounds identification, lead compounds optimization, candidate drugs preparation, and so on. As Nobel Prize laureate James Black emphasized, "the most fruitful basis for the discovery of a new drug is to start with an old drug". Late-stage modification or functionalization of drugs, natural products and bioactive compounds have garnered significant interest due to its ability to introduce diverse elements into bioactive compounds promptly.

Selective Ring-Opening Amination of Isochromans and Tetrahydroisoquinolines.

The molecular structure-editing through selective C-C bond cleavage allows for the precise modification of molecular structures and opens up new possibilities in chemical synthesis. By strategically cleaving C-C bonds and editing the molecular structure, more efficient and versatile pathways for the synthesis of complex compounds could be designed, which brings significant implications for drug development and materials science. o-Aminophenethyl alcohols and amines are the essential key motifs in bioactive and functional material molecules.

Dioxygen compatible electron donor-acceptor catalytic system and its enabled aerobic oxygenation.

The photochemical properties of Electron Donor-Acceptor (EDA) complexes present exciting opportunities for synthetic chemistry. However, these strategies often require an inert atmosphere to maintain high efficiency. Herein, we develop an EDA complex photocatalytic system through rational design, which overcomes the oxygen-sensitive limitation of traditional EDA photocatalytic systems and enables aerobic oxygenation reactions through dioxygen activation.

Catalytic conversion of mixed polyolefins under mild atmospheric pressure.

The chemical recycling of polyolefin presents a considerable challenge, especially as upcycling methods struggle with the reality that plastic wastes typically consist of mixtures of polyethylene (PE), polystyrene (PS), and polypropylene (PP). We report a catalytic aerobic oxidative approach for polyolefins upcycling with the corresponding carboxylic acids as the product. This method encompasses three key innovations.

isoquinoline alkaloids attenuate lipopolysaccharide-induced intestinal epithelium injury in broiler chickens by co-regulating the TLR4/MyD88/NF-κB and Nrf2 signaling pathways.

This study sought to explore the effects and potential mechanisms of dietary supplementation with isoquinoline alkaloids (IA) from to alleviate lipopolysaccharide (LPS)-induced intestinal epithelium injury in broilers. A total of 486 1-day-old broilers were assigned at random to a control (CON) group, LPS group, and LPS+IA group in a 21-d study. The CON and LPS groups received a basal diet, while the LPS+IA group received a basal diet supplemented with 0.

Glutamine attenuates bisphenol A-induced intestinal inflammation by regulating gut microbiota and TLR4-p38/MAPK-NF-κB pathway in piglets.

Bisphenol A (BPA), as a kind of widely exerted environmental hazardous material, brings toxicity to both humans and animals. This study aimed to investigate the role of glutamine (Gln) in intestinal inflammation and microbiota in BPA-challenged piglets. Thirty-two piglets were randomly divided into four groups according to 2 factors including BPA (0 vs.