Hot rolling work rolls are essential components in the hot rolling process. However, they are subjected to high temperatures, alternating stress, and wear under prolonged and complex working conditions. Due to these factors, the surface of the work rolls gradually degrades, which significantly impacts the quality of the final product.
View Article and Find Full Text PDFA total of 12 carbonyl compounds were synthesized, their lipopolysaccharide induced inhibition, and activity of RAW264.7 cells was evaluated. The most active compound inhibited RAW264.
View Article and Find Full Text PDFRibosomal proteins (RPs) play an important role in the overall stability, function, and integrity of ribosomes. Ribosomal protein L4 (RPL4), which is encoded by , is assumed to play different roles in different cancers due to the strong correlation between them. However, research based on the underlying mechanisms of this correlations is limited.
View Article and Find Full Text PDFA series of 1-(2-oxocyclohexyl)butane-1, 3-dione derivatives were designed and synthesized as TLR4 inhibitors by modifying the core structure of the lead compound ((6, 8-dioxo-1, 2, 3, 4, 6, 7, 8, 8a-octahydronaphthalen-2-yl) carbamate)). In vitro, compound 3p significantly inhibited the proliferation of rat synovial cells, inhibited the proliferation of LPS-induced RAW264.7 cells, and inhibited TLR4 activity, with IC values of 1.
View Article and Find Full Text PDFThe natural products have a new chemical structure and biological active diversity, so they are favored by scientific researchers. Gout is a high incidence and high-risk disease, and the current treatments are not satisfactory. Xanthine oxidase (XO) is a key enzyme responsible for the development and progression of various metabolic and oxidative stress-related diseases.
View Article and Find Full Text PDFRheumatoid arthritis (RA) is a chronic and systemic disease of inflammatory synovitis with unknown etiology. In previous studies, we found that the double-ring conjugated enone structure has anti-rheumatoid arthritis activity and could effectively inhibit the proliferation of rat synovial cells and has good anti-inflammatory activity . Herein, we further modified the structure, which was a novel double-ring conjugated enone, to study its anti-rheumatoid arthritis activity.
View Article and Find Full Text PDFIn order to explore the potential anti-tumor activity functional molecules, a series of Fissitungfine B derivatives were designed and synthesized. Their anti-tumor activity effects on Hela, MCF-7 and A-549 cell lines were evaluated in vitro. The results showed that some of these Fissitungfine B derivatives exhibited moderate to good anti-tumor activities.
View Article and Find Full Text PDFBackground: Acute sleep loss increases the brain's reactivity toward positive and negative affective stimuli. Thus, despite well-known reduced attention due to acute sleep loss, we hypothesized that humans would gaze longer on happy, angry, and fearful faces than neutral faces when sleep-deprived. We also examined if facial expressions are differently perceived after acute sleep loss.
View Article and Find Full Text PDFThe preparation of purified polysaccharides was described from fresh onions by hot water extraction, protein removal and dialysis treatment. The structure of onion polysaccharide was confirmed by C NMR, DEPT, COSY, HSQC and HMBC. In order to study the structure-activity relationship of onion polysaccharide, the derivatives of onion polysaccharide including acetylated onion polysaccharide and phosphoric onion polysaccharide were prepared.
View Article and Find Full Text PDFChem Biol Drug Des
April 2022
The polysaccharide from Morinda citrifolia fermentation liquor was extracted by the hot water method. The acetylated polysaccharide, phosphorylated polysaccharide, carboxymethylated polysaccharide, and sulfated polysaccharide were identified by IR and NMR spectra. The results showed that Morinda citrifolia polysaccharide and its derivatives showed the good antioxidant activity, and them up to V level.
View Article and Find Full Text PDFAcetylcholinesterase (AChE) inhibitor is the first choice for the treatment of Alzheimer's disease (AD), but it has some defects, such as dose limitation and unsatisfactory long-term treatment effect. Recent studies have shown that butyrylcholinesterase (BuChE) inhibitors or double acetyl and butyryl cholinesterase inhibitors have better curative effects on AD, and the side effects are lower than those of specific AChE inhibitors. Dual target cholinesterase inhibitors have become a new hotspot in the research of anti-AD drugs.
View Article and Find Full Text PDFAlzheimer's disease (AD) is a neurodegenerative disease with unknown etiology and pathogenesis, in which butyrylcholinesterase (BuChE) plays an important role in the pathogenesis and progression. Inhibition of BuChE is a potential strategy for the treatment of advanced AD. Herein, the advantages and disadvantages of various synthesis methods on BuChE inhibitors and their inhibitory activities were summarized.
View Article and Find Full Text PDFRheumatoid arthritis (RA) is a chronic disease that seriously affects human health and quality of life, and it is one of the main causes of labor loss and disability. Many countries have listed rheumatoid arthritis as one of the national a key diseases to tackle. The pathogenesis of RA in humans is still unknown, and medical researchers believe that the pathogenesis of RA may be the result of a combination of genetic and environmental factors.
View Article and Find Full Text PDFBiomed Pharmacother
December 2021
Polysaccharides have anti-virus, anti-cancer, anti-oxidation, immune regulation, hypoglycemia and other biological activities. Because of their safety, fewer side effects and other advantages, polysaccharides are considered as ideal raw materials in food and drugs. The biological activity of polysaccharides can be improved by structural modification (such as sulfation, carboxymethylation, phosphorylation, etc.
View Article and Find Full Text PDFCholinesterase (ChE) inhibitors can be divided into two categories: acetylcholinesterase (AChE) inhibitors and butylcholinesterase (BuChE) inhibitors. Therefore, the development of selective inhibition of AChE and BuChE activities is the central content of ChE pharmacochemistry research. In order to clarify the progress of AChE inhibitor-based design, synthesis, and activity studies, we reviewed the pharmacochemical and pharmacological properties of selective AChE inhibitors over the past decade.
View Article and Find Full Text PDFBioorg Med Chem Lett
October 2021
The relationship between TLR4 and inflammation-related diseases has been paid more and more attention. The studies have shown that TLR4/NF-κB signaling pathway plays an important role in the transmission of inflammatory signals. A large number of pro-inflammatory factors, chemokines, adhesion factors, TLR4 and its ligands interact with each other, and jointly promote the development of diseases.
View Article and Find Full Text PDFThe polysaccharide of yam was extracted by hot water method and purified by column chromatography. The physicochemical properties of Chinese yam polysaccharide were analyzed by UV, IR, GPC, 1D-NMR and 2D-NMR spectra. The results showed that Chinese yam polysaccharide had α-d-Gluc-(1 → 4) glycoside bond, and the C2 hydroxyl group was replaced by ethoxyl group.
View Article and Find Full Text PDFChem Biol Drug Des
August 2021
The activities of marine alkaloids are manifested in antifungus and antimalaria. The optimization process, chemical synthesis, antimalarial activity, and antibacterial activity of various compounds were discussed.
View Article and Find Full Text PDFMarine alkaloids were divided into five categories from the perspective of anti-tumor activity. The optimization process, chemical synthesis, anti-tumor activity evaluation and structure-activity relationship of various compounds were discussed.
View Article and Find Full Text PDFFour series of double-ring conjugated enones were designed, synthesized and studied for the inhibition of synovial cell activity through the modification of Dysodensiol K core structure, double-ring, double-bond and double-carbonyl groups. For in vitro synovial cell assay of rats, compound 151 and 168 exhibited good inhibitory activities, with IC values of 2.71 ± 0.
View Article and Find Full Text PDFBioorg Med Chem Lett
January 2021
Antioxidants is a kind of substances that can effectively inhibit the oxidation reaction of free radicals. There are many chemical components with antioxidant activity in natural products. Sesamol is one of the natural products with antioxidant activity, and it is often used as an antioxidant in food, medicine and other fields.
View Article and Find Full Text PDFIn this study, a series of novel 7H-benzo [c] [1,3] dioxolo [4, 5-f] chromen-7-one derivatives were obtained by structural modification of the lead compounds with Fissitungfine B. A total 15 compounds were designed, synthesized and evaluated as inhibitors of tumor. These target compounds have the novel chemical structures that named three six-membered rings including one lactone six-membered ring.
View Article and Find Full Text PDFThe ocean is the origin of life, with a unique ecological environment, which has given birth to a wealth of marine organisms. The ocean is an important source of biological resources and tens of thousands of monomeric compounds have been separated from marine organisms using modern separation technology. Most of these monomeric compounds have some kind of biological activity that has attracted extensive attention from researchers.
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