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•Entecavir and imipenem alleviated LPS-induced cytokine storm syndrome.•Entecavir and imipenem mitigated LPS-induced acute lung injury.•Entecavir and imipenem inhibited LPS-stimulated ...TNF-α and IL-10 in hPBMC.•Entecavir and imipenem attenuated LPS-activated NF-κB.
Coronavirus Disease 2019 (COVID-19) caused by Severe Acute Respiratory Syndrome Coronavirus -2 (SARS-CoV-2) has been widely spread in the world with a high mortality. Cytokine storm syndrome (CSS) and acute lung injury caused by SARS-CoV-2 infection severely threaten the patients. With the purpose to find effective and low-toxic drugs to mitigate CSS, entecavir and imipenem were identified to reduce TNF-α using a LPS-induced macrophage model from the anti-infective drug library. Entecavir and imipenem efficiently suppressed the release of inflammatory cytokines by partly intervention of NF-κB activity. The acute lung injury was also alleviated and the survival time was prolonged in mice. In addition, entecavir and imipenem inhibited the release of TNF-α and IL-10 in human peripheral blood mononuclear cells (hPBMCs). Collectively, we proposed that entecavir and imipenem might be candidates for the treatment of CSS.
Cannabinoid receptors belong to the large family of G-protein-coupled receptors, which can be divided into two receptor types, cannabinoid receptor type-1 (CB1) and cannabinoid receptor type-2 (CB2). ...Marinol, Cesamet and Sativex are marketed CB1 drugs which are still in use and work well, but the central nervous system side effects caused by activation CB1, which limited the development of CB1 ligands. So far, no selective CB2 ligand has been approved for marketing, but lots of its ligands in the clinical stage and pre-clinical stage have positive effects on the treatment of some disease models and have great potential for development. Most selective CB2 agonists are designed and synthesized based on non-selective CB2 agonists through the classical med-chem strategies,
e.g.
molecular hybridization, scaffold hopping, bioisosterism,
etc.
During these processes, the balance between selectivity, activity, and pharmacokinetic properties needs to be achieved. Hence, we summarized some reported ligands on the basis of the optimization strategies in recent 10 years, and the limitations and future directions.
Cannabinoid receptors belong to the large family of G-protein-coupled receptors, which can be divided into two receptor types, cannabinoid receptor type-1 (CB1) and cannabinoid receptor type-2 (CB2).
As a member of the group IVB transition metal dichalcogenides (TMDs) family, hafnium disulfide (HfS2) is recently predicted to exhibit higher carrier mobility and higher tunneling current density ...than group VIB (Mo and W) TMDs. However, the synthesis of high‐quality HfS2 crystals, sparsely reported, has greatly hindered the development of this new field. Here, a facile strategy for controlled synthesis of high‐quality atomic layered HfS2 crystals by van der Waals epitaxy is reported. Density functional theory calculations are applied to elucidate the systematic epitaxial growth process of the S‐edge and Hf‐edge. Impressively, the HfS2 back‐gate field‐effect transistors display a competitive mobility of 7.6 cm2 V−1 s−1 and an ultrahigh on/off ratio exceeding 108. Meanwhile, ultrasensitive near‐infrared phototransistors based on the HfS2 crystals (indirect bandgap ≈1.45 eV) exhibit an ultrahigh responsivity exceeding 3.08 × 105 A W−1, which is 109‐fold higher than 9 × 10−5 A W−1 obtained from the multilayer MoS2 in near‐infrared photodetection. Moreover, an ultrahigh photogain exceeding 4.72 × 105 and an ultrahigh detectivity exceeding 4.01 × 1012 Jones, superior to the vast majority of the reported 2D‐materials‐based phototransistors, imply a great promise in TMD‐based 2D electronic and optoelectronic applications.
A facile strategy for the synthesis of high‐quality monolayer HfS2 crystals by van der Waals epitaxy is reported. Ultrasensitive near‐infrared phototransistors based on the HfS2 crystals exhibit an ultrahigh responsivity 3.08 × 105 A W−1, and an ultrahigh detectivity exceeding 4.01 × 1012 Jones, superior to most 2D materials‐based phototransistors.
Coronavirus Disease 2019 (COVID-19) infected by Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) has been declared a public health emergency of international concerns. Cytokine storm ...syndrome (CSS) is a critical clinical symptom of severe COVID-19 patients, and the macrophage is recognized as the direct host cell of SARS-CoV-2 and potential drivers of CSS. In the present study, peramivir was identified to reduce TNF-α by partly intervention of NF-κB activity in LPS-induced macrophage model.
, peramivir reduced the multi-cytokines in serum and bronchoalveolar lavage fluid (BALF), alleviated the acute lung injury and prolonged the survival time in mice. In human peripheral blood mononuclear cells (hPBMCs), peramivir could also inhibit the release of TNF-α. Collectively, we proposed that peramivir might be a candidate for the treatment of COVID-19 and other infections related CSS.
Polyphenols, present in a broad range of plants, have been thought to be responsible for many beneficial health effects, such as an antidepressant. Despite that polyphenols can be absorbed in the ...small intestine directly, most of them have low bioavailability and reach the large intestine without any modifications due to their complex structures. The interaction between microbial communities and polyphenols in the intestine is important for the latter to exert antidepressant effects. Gut microbiota can improve the bioavailability of polyphenols; in turn, polyphenols can maintain the intestinal barrier as well as the community of the gut microbiota in normal status. Furthermore, gut microbita catabolize polyphenols to more active, better-absorbed metabolites, further ameliorating depression through the microbial-gut-brain (MGB) axis. Based on this evidence, the review illustrates the potential role of gut microbiota in the processes of polyphenols or their metabolites acting as antidepressants and further envisions the gut microbiota as therapeutic targets for depression.
As one of the most active nonlinear inversion methods in transient electromagnetic (TEM) inversion, the back propagation (BP) neural network has high efficiency because the complicated forward model ...calculation is unnecessary in iteration. The global optimization ability of the particle swarm optimization (PSO) is adopted for amending the BP's sensitivity to its initial parameters, which avoids it falling into a local optimum. A chaotic-oscillation inertia weight PSO (COPSO) is proposed for accelerating convergence. The COPSO-BP algorithm performance is validated by two typical testing functions, two geoelectric models inversions and a field example. The results show that the COPSO-BP method is more accurate, stable and needs relatively less training time. The proposed algorithm has a higher fitting degree for the data inversion, and it is feasible to use it in geophysical inverse applications.
The resonant magnetoelectric (ME) effect of Fe78Si9B13/Pb(Zr,Ti)O3 (FeSiB/PZT) composites with a surface-modified Fe78Si9B13 amorphous alloy has been studied. The surface-modified FeSiB can improve ...the ME coefficient at the resonant frequency by optimizing the magnetomechancial power conversion efficiency. The maximum ME coefficient of the surface-modified ribbons combined with soft PZT (PZT5) is two-thirds larger than that of the composites with fully amorphous ribbons. Meanwhile, the maximum value of the ME coefficient with surface-modified FeSiB ribbons and hard PZT (PZT8) is one-third higher compared with the fully amorphous composites. In addition, experimental results of magnetomechanical coupling properties of FeSiB/PZT composites with or without piezoelectric layers indicate that the power efficiency of the composites first decreases and then increases with the increase in the number of FeSiB layers. When the surface crystalline FeSiB ribbons are combined with a commercially available hard piezoelectric ceramic plate, the maximum magnetoelectric coupling coefficient of the ME composite reaches 5522 V/(Oe*cm), of which the electromechanical resonant frequency is 23.89 kHz.
In this work we addressed a key challenge in realizing multiferroics-based reconfigurable magnetic devices, which is the ability to switch between distinct collective magnetic states in a reversible ...and stable manner with a control voltage. Three possible non-volatile switching mechanisms have been demonstrated, arising from the nature of the domain states in pervoskite PZN-PT crystal that the ferroelectric polarization reversal is partially coupled to the ferroelastic strain. Electric impulse non-volatile control of magnetic anisotropy in FeGaB/PZN-PT and domain distribution of FeGaB during the ferroelectric switching have been observed, which agrees very well with simulation results. These approaches provide a platform for realizing electric impulse non-volatile tuning of the order parameters that are coupled to the lattice strain in thin-film heterostructures, showing great potentials in achieving reconfigurable, compact, light-weight and ultra-low-power electronics.
Accurate assessment of biodiversity is important for scientists, conservationists and policy makers. With the development of DNA barcoding and metabarcoding, many cryptic species have been identified ...based on the sequence diversity of a ‘barcode’ region in the mitochondrial genome. These molecular identifications have increased the estimated number of species on Earth ten‐fold. Mitochondrial DNA heteroplasmy, in which multiple mitochondrial haplotypes coexist in a single organism, can interfere with the accuracy of these estimates. However, this phenomenon is still infrequently documented. The main reason is that it is difficult to distinguish heteroplasmic sequences from nuclear mitochondrial segments (Numts). We investigated the prevalence of multiple haplotypes in DNA barcoding sequences in fig wasps (Insect: Hymenoptera) by performing high‐throughput sequencing on individual specimens. DNA metabarcoding was artificially simulated by combining all the haplotype sequences. Using conventional DNA barcoding by Sanger sequencing, the 28 morphological species we studied were divided into 38 taxa, suggesting the existence of ten cryptic species. However, the haplotypes originating from a single specimen clustered into different cryptic species clades, which conflicted with the conventional barcoding results. Furthermore, when we artificially simulated DNA metabarcoding by mixing all haplotype sequences, the number of molecular operational taxonomic units (or putative species) was 3.2× the number of morphological species. These results indicate that the prevalence of multiple haplotypes within individual specimens may have an important impact on DNA barcode‐based species identification and biodiversity assessment more broadly.
We obtained multiple haplotypes within individual specimens by high‐throughput sequencing.
Multiple haplotypes originating from a single specimen could mislead DNA barcoding result.
Multiple haplotypes within individual specimens could result in overestimation of biodiversity in DNA metabarcoding.
A quaternary ammonium salt covalently bound to chitosan (a functionalized biopolymer) is reported as an efficient and recyclable single-component catalyst for the synthesis of propylene carbonate ...from propylene oxide and CO
2 without any organic solvent or co-catalyst. Notably, this environmental benign and cost-effective process has great potential to be applied in various continuous flow reactors in industry.
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A quaternary ammonium salt covalently bound to chitosan is reported as an efficient and recyclable single-component catalyst for the synthesis of propylene carbonate (PC) from propylene oxide (PO) and carbon dioxide without any organic solvent or co-catalyst. The catalyst can be easily recovered by filtration and reused for at least five times without obvious loss of its catalytic activity. The effects of the catalyst structure and various reaction parameters on the catalytic performance were in detail investigated. Moreover, the catalyst was found to be applicable to a variety of terminal epoxides, producing the corresponding cyclic carbonates in high yield and selectivity. Notably, this environmentally benign and cost-effective process has great potential to be applied in various continuous flow reactors in industry.
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