Zobrazení zdroje stránky Ankerellegaard6695

The first facile and efficient acid-catalyzed direct coupling of a wide range of unprotected 2,3-allenols with arylphosphine oxides was developed, offering a general, one-step approach for the synthesis of structurally diverse γ-ketophosphine oxides accompanied by concurrent C-P/C═O bond formation with remarkable functional group tolerance and complete atom-economy under metal- and additive-free conditions. Mechanistic studies showed that this transformation involved a rearrangement and a phospha-Michael reaction.This study aimed to evaluate the neuroprotective function of shrimp-derived peptides QMDDQ and KMDDQ. [https://www.selleckchem.com/products/abc294640.html read more] Biochemical results revealed that both peptides exhibited neuroprotective effects by increasing acetylcholine (ACh) content and inhibiting acetylcholinesterase (AChE) activity in PC12 cells; QMDDQ was more active than KMDDQ. COSY-NOESY spectroscopic data showed that the superior neuroprotective function of QMDDQ might be attributed to its N-terminal glutamine as it exhibited an extended spatial conformation, facilitating its interactions with AChE. QMDDQ can promote the basic energy metabolism of cells more than KMDDQ. The peptides showed neuroprotective ability due to the activation of the antiapoptosis and PKA/CREB/BNDF signaling pathway. QMDDQ was selected to investigate its memory-enhancing activity in scopolamine-induced amnesic mice, revealing memory protection in mice, as it improved their performance in the Morris water maze experiment. In addition, QMDDQ increased ACh content (4.98 ± 0.51 μg/mg prot) and decreased AChE activity (4.72 ± 0.11 U/mg prot) in the mouse hippocampus. These data indicate the systemic mechanism through which naturally derived QMDDQ improved neuroprotection and memory ability.In the present work, a novel series of trifluoromethyl-substituted tetrahydropyran derivatives were rationally designed and synthesized as potent DPP-4 inhibitors with significantly improved duration time of action over current commercially available DPP-4 inhibitors. The incorporation of the trifluoromethyl group on the 6-position of the tetrahydropyran ring of omarigliptin with the configuration of (2R,3S,5R,6S) not only significantly improves the overall pharmacokinetic profiles in mice but also maintains comparable DPP-4 inhibition activities. Further preclinical development of compound 2 exhibited its extraordinary efficacy in vivo and good safety profile. Clinical studies of compound 2 (Haisco HSK7653) are now ongoing in China, which revealed that inhibitor 2 could serve as an efficient candidate with a once-biweekly therapeutic regimen.Short-chain fatty acids (SCFAs), especially propionate, originate from the fermentation of dietary fiber in the gut and play a key role in inhibiting pulmonary inflammation. Chronic inflammation may induce an epithelial-mesenchymal transition (EMT) in alveolar epithelial cells and result in fibrotic disorders. This study was designed to investigate the beneficial effect of sodium propionate (SP) on lipopolysaccharide (LPS)-induced EMT. In cultured BEAS-2B cells, the protein expression levels of E-cadherin, α-smooth muscle actin (SMA), and vimentin were 0.66 ± 0.20, 1.44 ± 0.23, and 1.32 ± 0.21 in the LPS group vs 1.11 ± 0.36 (P less then 0.05), 1.04 ± 0.30 (P less then 0.05), and 0.96 ± 0.13 (P less then 0.01) in the LPS + SP group (mean ± standard deviation), respectively. Meanwhile, LPS-triggered inflammatory cytokines and extracellular proteins were also reduced by SP administration in BEAS-2B cells. Moreover, SP treatment attenuated inflammation, EMT, extracellular matrix (ECM) deposition, and even fibrosis in a mouse EMT model. In terms of mechanism, LPS-treated BEAS-2B cells exhibited a higher level of phosphatidylinositol 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) phosphorylation, which was interrupted by SP treatment. It is worth noting that the blockade of the PI3K/Akt/mTOR signaling cascade reduced the LPS-evoked EMT process in BEAS-2B cells. These results suggest that SP can block LPS-induced EMT via inhibition of the PI3K/Akt/mTOR signaling cascade, which provides a basis for possible clinical use of SP in airway and lung diseases.To replace the hazardous and complicated Boliden-Norzink technology, the technology of Hg0 recovery from smelting flue gas by a magnetic and reproducible sulfureted MoO3/Fe-Ti spinel was employed to keep the produced H2SO4 free of Hg. The sulfureted MoO3/Fe-Ti spinel showed excellent performance in capturing gaseous Hg0, with an average adsorption rate of 93.3 μg g-1 min-1 and an adsorption capacity of 66.3 mg g-1 at 60 °C, which were much better than those of most of the other reported sorbents. Meanwhile, the sulfureted MoO3/Fe-Ti spinel exhibited excellent superparamagnetism and magnetization of 19.9 emu g-1, which ensured that it could easily be magnetically separated without a specialized precipitator or the molding of pulverous sorbents to monolithic sorbents. To investigate the promotion mechanism of MoO3 loading on Hg0 adsorption onto the sulfureted Fe-Ti spinel, the Hg0 adsorption kinetic parameters of the sulfureted MoO3/Fe-Ti spinel and sulfureted Fe-Ti spinel, resulting from the fitting of the adsorption breakthrough curves based on the kinetic model, were compared. The promotion of MoO3 loading was attributed to the remarkable increase in the adsorption sites on the sulfureted Fe-Ti spinel for Hg0 physical adsorption, which was mainly related to the formation of the MoS3 layer.A highly-efficient, autonomous electrochemical-osmotic system (EOS) is developed for simultaneous recovery of electric energy, water, and metals from wastewater. We demonstrate that the system can generate a maximum electric power density of 10.5 W m-2 using a spontaneous Fe/Cu2+ galvanic cell, while simultaneously achieving copper recovery from wastewater. With an osmotic pressure difference generated by the deployed electrochemical reactions, water is osmotically extracted from the feed solution with the EOS at a water flux of 5.1 L m-2 h-1. A scaled-up EOS realizes a power density of 105.8 W per m-3 of treated water to light an LED over 24 h while also enhancing water extraction and metal recovery. The modularized EOS obtains ultrahigh (&gt;97.5%) Faradaic efficiencies under variable operating conditions, showing excellent system stability. The EOS is also versatile it can recover Au, Ag, and Hg from wastewaters with simultaneous electricity and water coproduction. Our study demonstrates a promising pathway for realizing multiresource recycling from wastewater by coupling electrochemical and osmosis-driven processes.