The stems of Cynomorium songaricum are used in traditional Chinese medicine as a tonic and also used locally as a food material and livestock feed. It is known that some of the falvan‐3‐ol monomers ...and dimers that entered the milk of dairy sheep fed with C. songaricum stems are biotransformation products of the original flavan‐3‐ol polymers in C. songaricum stems. This study was performed to investigate the biotransformation process of the flavan‐3‐ols in dairy sheep and to evaluate the bioactivities. The results showed that procyanidin A2 and epicatechin could be released from the polymeric flavan‐3‐ols of C. songaricum through rumen microbial metabolism. On traumatic and lipopolysaccharide (LPS)‐induced inflammation models of Tg (mpx: EGFP) zebrafish larvae and LPS‐induced liver injury models of Tg (fabp10a: DsRed) zebrafish larvae, the milk from sheep fed with C. songaricum stems showed stronger anti‐inflammatory and hepatoprotective activities compared to blank milk. The absorbed chemical constituents of C. songaricum stems and the metabolites also exhibited anti‐inflammatory and hepatoprotective activities, with the dimeric flavan‐3‐ols being more effective than the monomers. The milk, the absorbed chemical constituents of C. songaricum stems, and the metabolites alleviated the increased level of reactive oxygen species induced by LPS in zebrafish larvae.
Practical Application
This study found that C. songaricum stems as livestock feed could produce milk that has a beneficial impact on consumer and livestock health in terms of anti‐inflammation and hepatoprotection.
Tissue engineering has become a promising strategy for repairing damaged cartilage and bone tissue. Among the scaffolds for tissue-engineering applications, injectable hydrogels have demonstrated ...great potential for use as three-dimensional cell culture scaffolds in cartilage and bone tissue engineering, owing to their high water content, similarity to the natural extracellular matrix (ECM), porous framework for cell transplantation and proliferation, minimal invasive properties, and ability to match irregular defects. In this review, we describe the selection of appropriate biomaterials and fabrication methods to prepare novel injectable hydrogels for cartilage and bone tissue engineering. In addition, the biology of cartilage and the bony ECM is also summarized. Finally, future perspectives for injectable hydrogels in cartilage and bone tissue engineering are discussed.
Effective control of melting and solidification behaviours of materials is significant for numerous applications. It has been a long-standing challenge to increase the melted zone (MZ) depth while ...shrinking the heat-affected zone (HAZ) size during local melting and solidification of materials. In this paper, nanoparticle-induced unusual melting and solidification behaviours of metals are reported that effectively solve this long-time dilemma. By introduction of Al
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nanoparticles, the MZ depth of Ni is increased by 68%, while the corresponding HAZ size is decreased by 67% in laser melting at a pulse energy of 0.18 mJ. The addition of SiC nanoparticles shows similar results. The discovery of the unusual melting and solidification of materials that contain nanoparticles will not only have impacts on existing melting and solidification manufacturing processes, such as laser welding and additive manufacturing, but also on other applications such as pharmaceutical processing and energy storage.
The rational design of atomic‐scale interfaces in multiphase nanohybrids is an alluring and challenging approach to develop advanced electrocatalysts. Herein, through the selection of two different ...metal oxides with particular intrinsic features, advanced Co3O4/CeO2 nanohybrids (NHs) with CeO2 nanocubes anchored on Co3O4 nanosheets are developed, which show not only high oxygen vacancy concentration but also remarkable 2D electron gas (2DEG) behavior with ≈0.79 ± 0.1 excess e−/u.c. on the Ce3+ sites at the Co3O4–CeO2 interface. Such a 2DEG transport channel leads to a high carrier density of 3.8 × 1014 cm−2 and good conductivity. Consequently, the Co3O4/CeO2 NHs demonstrate dramatically enhanced oxygen evolution reaction (OER) performances with a low overpotential of 270 mV at 10 mA cm−2 and a high turnover frequency of 0.25 s−1 when compared to those of pure Co3O4 and CeO2 counterparts, outperforming commercial IrO2 and some recently reported representative OER catalysts. These results demonstrate the validity of tailoring the electrocatalytic properties of metal oxides by 2DEG engineering, offering a step forward in the design of advanced hybrid nanostructures.
A novel 2D electron gas (2DEG) behavior, which is realized by integrating CeO2 nanocubes into Co3O4 nanosheets, is demonstrated, and the obtained Co3O4/CeO2 nanohybrids show high electrocatalytic oxygen evolution reaction (OER) performances due to the increased concentration of oxygen vacancies and 2DEG‐promoted high conductivity and electron mobility at the Co3O4–CeO2 interface.
Lysine specific demethylase 1 (LSD1) and Histone deacetylases (HDACs) are promising drug targets for cancers. Recent studies reveal an important functional interplay between LSD1 and HDACs, and there ...is evidence for the synergistic effect of combined LSD1 and HDAC inhibitors on cancers. Therefore, development of inhibitors targeting both LSD1 and HDACs might be a promising strategy for epigenetic therapy of cancers. We report herein the synthesis of a series of tranylcypromine derivatives as LSD1/HDACs dual inhibitors. Most compounds showed potent LSD1 and HDACs inhibitory activity, especially compound 7 displayed the most potent inhibitory activity against HDAC1 and HDAC2 with IC50 of 15 nM and 23 nM, as well as potent inhibition against LSD1 with IC50 of 1.20 μM. Compound 7 demonstrated stronger anti-proliferative activities than SAHA with IC50 values ranging from 0.81 to 4.28 μM against MGC-803, MCF-7, SW-620 and A-549 human cancer cell lines. Further mechanistic studies showed that compound 7 treatment in MGC-803 cells dose-dependently increased cellular H3K4 and H3K9 methylation, as well as H3 acetylation, decreased the mitochondrial membrane potential and induced remarkable apoptosis. Docking studies showed that compound 7 can be well docked into the active binding sites of LSD1 and HDAC2. This finding highlights the potential for the development of LSD1/HDACs dual inhibitors as novel anticancer drugs.
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•A series of tranylcypromine derivatives were discovered as novel LSD1/HDACs dual inhibitors.•Compound 7 exhibited potent dual LSD1/HDACs inhibition with strong antiproliferative activity.•Compound 7 dose-dependently increased cellular H3K4 and H3K9 methylation, as well as H3 acetylation.•Compounds 7 induced remarkable apoptosis and decreased mitochondrial membrane potential.
Postsynthetic modification (PSM) has been demonstrated to be a powerful method for achieving new covalent organic frameworks (COFs) via single-step or multistep organic functional group ...transformations on established COF frameworks. PSM, however, might sometimes lead to collapse of the COF framework, decreases in crystallinity, or low postsynthetic yield due to the inherent limit of solid-state synthesis. Herein we report, for the first time, a new synthetic strategy that can generate new COFs via multicomponent one-pot in situ reactions. In total, 12 α-aminonitrile- and quinoline-linked COFs with high crystallinity and permanent porosity are successfully achieved by three-component one-pot in situ Strecker and Povarov reactions under solvothermal conditions in high yields. The obtained COFs feature the same structures as those obtained from the stepwise PSM approach on an established imine-linked COF. This in situ multicomponent assembly strategy, as a synthetic methodology parallel to PSM, might open a new route for constructing COFs that is not possible under PSM conditions.
In response to the recent growth of multitudes of theoretical literature analysing the corruption impact on the economy and environment, this paper subjects the corruption–carbon emission ...relationship in China to a detailed empirical examination through the autoregressive distributed lag modelling approach and panel quantile regressions. Based on panel data from Chinese provinces, spanning the period 1998–2016, this study explores the impact of long- and short-term corruption on per capita carbon emissions by considering the heterogeneous distribution of those emissions. The results document that corruption increases per capita carbon emissions in Chinese provinces in the short run, reducing per capita carbon emissions in the long run. Moreover, an increase in corruption leads to an increase in carbon emissions per capita in all quantiles, indicating that these emissions increase with corruption severity. The coefficients in low quantiles are slightly larger than those in high quantiles, indicating that corruption leads to more carbon emissions in provinces with lower per capita carbon emissions.
•The paper explores the impact of corruption on CO2 emissions in China provinces.•It uses quantile methods, spanning the period 1998–2016.•The results show that corruption increases CO2 emissions in the short run.•In the long run it reduces CO2 emissions.•The findings imply that emissions increase with the severity of corruption.
(S)-2-(2-Chlorophenyl)-2-(6,7-dihydrothieno3,2-cpyridin-5(4H)-yl)acetonitrile ((S)-CIK) is a key intermediate in the synthesis of (S)-clopidogrel, which is one of the most saleable worldwide ...antiplatelet and antithrombotic drugs. We show herein a facile method for the direct synthesis of (S)-CIK via Strecker reaction using a homochiral covalent framework catalyst in a heterogeneous way. The asymmetric synthesis involves a photothermal-conversion-triggered, thermally driven reaction which affords (S)-CIK in 98% yield with 94% enantiomeric excess under visible-light irradiation. Furthermore, the above approach is readily extended to a gram-scale level on a fixed-bed continuous-flow model reactor. The potential utility of this strategy is highlighted by the preparation of many more other types of chiral drugs and drug intermediates in a green and facile way.
Owing to their permanent porosity, highly ordered and extended structure, good chemical stability, and tunability, covalent organic frameworks (COFs) have emerged as a new type of organic materials ...that can offer various applications in different fields. Benefiting from the huge database of organic reactions, the required functionality of COFs can be readily achieved by modification of the corresponding organic functional groups on either polymerizable monomers or established COF frameworks. This striking feature allows homochiral covalent organic frameworks (HCCOFs) to be reasonably designed and synthesized, as well as their use as a unique platform to fabricate asymmetric catalysts. This contribution provides an overview of new progress in HCCOF‐based asymmetric catalysis, including design, synthesis, and their application in asymmetric organic synthesis. Moreover, major challenges and developing trends in this field are also discussed. It is anticipated that this review article will provide some new insights into HCCOFs for heterogeneous asymmetric catalysis and help to encourage further contributions in this young but promising field.
Chirality from COFs: Owing to their permanent porosity, highly ordered and extended structure, good chemical stability, and tunability, covalent organic frameworks have emerged as a new type of organic materials that can offer various applications in different fields. Herein, the design and synthesis of chiral covalent organic frameworks and their applications in asymmetric catalysis are highlighted.
Since nuclear factor of κ‐light chain of enhancer‐activated B cells (NF‐κB) was discovered in 1986, extraordinary efforts have been made to understand the function and regulating mechanism of NF‐κB ...for 35 years, which lead to significant progress. Meanwhile, the molecular mechanisms regulating NF‐κB activation have also been illuminated, the cascades of signaling events leading to NF‐κB activity and key components of the NF‐κB pathway are also identified. It has been suggested NF‐κB plays an important role in human diseases, especially inflammation‐related diseases. These studies make the NF‐κB an attractive target for disease treatment. This review aims to summarize the knowledge of the family members of NF‐κB, as well as the basic mechanisms of NF‐κB signaling pathway activation. We will also review the effects of dysregulated NF‐κB on inflammation, tumorigenesis, and tumor microenvironment. The progression of the translational study and drug development targeting NF‐κB for inflammatory diseases and cancer treatment and the potential obstacles will be discussed. Further investigations on the precise functions of NF‐κB in the physiological and pathological settings and underlying mechanisms are in the urgent need to develop drugs targeting NF‐κB for inflammatory diseases and cancer treatment, with minimal side effects.
This year (2021) marks the 35th anniversary of the discovery of NF‐κB. With so many years of in‐depth research on NF‐κB, people have realized that the NF‐κB signaling pathway plays an important role in inflammation, immunity, cell survival and proliferation. This review summarizes the relevant knowledge of the NF‐κB signaling pathway, inflammation, and cancer. The progression of the translational study and drug development targeting NF‐κB for inflammatory diseases and cancer treatment and the potential obstacles will also be discussed.
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