Eosin Y, a well‐known economical alternative to metal catalysts in visible‐light‐driven single‐electron transfer‐based organic transformations, can behave as an effective direct hydrogen‐atom ...transfer catalyst for C−H activation. Using the alkylation of C−H bonds with electron‐deficient alkenes as a model study revealed an extremely broad substrate scope, enabling easy access to a variety of important synthons. This eosin Y‐based photocatalytic hydrogen‐atom transfer strategy is promising for diverse functionalization of a wide range of native C−H bonds in a green and sustainable manner.
Neutral eosin Y has been employed as an effective direct hydrogen‐atom transfer photocatalyst to activate a wide range of native C−H bonds in a green and sustainable fashion. This transformation is distinguished by its operational simplicity and amenability to large‐scale synthesis using continuous‐flow technology (EWG=aldehyde, ketone, ester, amide, imide, cyanide, sulfone, nitro, pyridine).
Chronic pain is a major clinical problem with limited treatment options. Previous studies have demonstrated that activation of adenosine monophosphate-activated protein kinase (AMPK) can attenuate ...neuropathic pain. Inflammation/immune response at the site of complete Freund's adjuvant (CFA) injection is known to be a critical trigger of the pathological changes that produce inflammatory pain. However, whether activation of AMPK produces an analgesic effect through inhibiting the proinflammatory cytokines, including interleukin-1β (IL-1β), in inflammatory pain remains unknown.
Inflammatory pain was induced in mice injected with CFA. The effects of AICAR (5-aminoimidazole-4-carboxyamide ribonucleoside, an AMPK activator), Compound C (an AMPK inhibitor), and IL-1ra (an IL-1 receptor antagonist) were tested at day 4 after CFA injection. Inflammatory pain was assessed with von Frey filaments and hot plate. Immunoblotting, hematoxylin and eosin (H&E) staining, and immunofluorescence were used to assess inflammation-induced biochemical changes.
The AMPK activator AICAR produced an analgesic effect and inhibited the level of proinflammatory cytokine IL-1β in the inflamed skin in mice. Moreover, activation of AMPK suppressed CFA-induced NF-κB p65 translocation from the cytosol to the nucleus in activated macrophages (CD68
and CX3CR1
) of inflamed skin tissues. Subcutaneous injection of IL-1ra attenuated CFA-induced inflammatory pain. The AMPK inhibitor Compound C and AMPKα shRNA reversed the analgesic effect of AICAR and the effects of AICAR on IL-1β and NF-κB activation in inflamed skin tissues.
Our study provides new information that AMPK activation produces the analgesic effect by inhibiting NF-κB activation and reducing the expression of IL-1β in inflammatory pain.
According to guidelines, endoscopic resection should only be performed for patients whose early gastric cancer invasion depth is within the mucosa or submucosa of the stomach regardless of lymph node ...involvement. The accurate prediction of invasion depth based on endoscopic images is crucial for screening patients for endoscopic resection. We constructed a convolutional neural network computer-aided detection (CNN-CAD) system based on endoscopic images to determine invasion depth and screen patients for endoscopic resection.
Endoscopic images of gastric cancer tumors were obtained from the Endoscopy Center of Zhongshan Hospital. An artificial intelligence–based CNN-CAD system was developed through transfer learning leveraging a state-of-the-art pretrained CNN architecture, ResNet50. A total of 790 images served as a development dataset and another 203 images as a test dataset. We used the CNN-CAD system to determine the invasion depth of gastric cancer and evaluated the system’s classification accuracy by calculating its sensitivity, specificity, and area under the receiver operating characteristic curve.
The area under the receiver operating characteristic curve for the CNN-CAD system was .94 (95% confidence interval CI, .90-.97). At a threshold value of .5, sensitivity was 76.47%, and specificity 95.56%. Overall accuracy was 89.16%. Positive and negative predictive values were 89.66% and 88.97%, respectively. The CNN-CAD system achieved significantly higher accuracy (by 17.25%; 95% CI, 11.63-22.59) and specificity (by 32.21%; 95% CI, 26.78-37.44) than human endoscopists.
We constructed a CNN-CAD system to determine the invasion depth of gastric cancer with high accuracy and specificity. This system distinguished early gastric cancer from deeper submucosal invasion and minimized overestimation of invasion depth, which could reduce unnecessary gastrectomy.
This study explored the effect of liver resection on perioperative circulating tumor cells (CTCs) and found that the prognostic significance of surgery was associated with changes in CTC counts in ...patients with hepatocellular carcinoma (HCC).
One hundred thirty-nine patients with HCC were consecutively enrolled. The time-points for collecting blood were one day before operation and three days after operation. CTCs in the peripheral blood were detected by the CellSearch™ System.
Both CTC detection incidence and mean CTC counts showed greater increases postoperatively (54%, mean 1.54 cells) than preoperatively (43%, mean 1.13 cells). The postoperative CTC counts increased in 41.7% of patients, decreased in 25.2% of patients and did not change in 33.1% of patients. The increase in postoperative CTC counts was significantly associated with the macroscopic tumor thrombus status. Patients with increased postoperative CTC counts (from preoperative CTC < 2 to postoperative CTC ≥ 2) had significantly shorter disease-free survival (DFS) and overall survival (OS) than did patients with persistent CTC < 2. Patients with persistent CTC levels of ≥2 had the worst prognoses.
Surgical liver resection is associated with an increase in CTC counts, and increased postoperative CTC numbers are associated with a worse prognosis in patients with HCC.
An investigation is performed into the efficiency of the
Streptomyces griseus
HUT 6037 enzyme immobilized in three different mesoporous silicas, namely mesoporous silica film, mesocellular foam, and ...rod-like SBA-15. It is shown that for all three supports, the pH value changes the surface charge and charge density and hence determines the maximum loading capacity of the enzyme. The products of the enzyme hydrolytic reaction are analyzed by
1
H-NMR. The results show that among the three silica supports, the mesoporous silica film (with a channel length in the range of 60-100 nm) maximizes the accessibility of the immobilized enzyme. The loading capacity of the enzyme is up to 95% at pH 7 and the activity of the immobilized enzyme is maintained for more than 15 days when using a silica film support. The order of the activity of the enzyme immobilized in different mesoporous silica supports is: mesoporous silica film > mesocellular foam > rod-like SBA-15. Furthermore, the immobilized enzyme can be easily separated from the reaction solution
via
simple filtration or centrifugation methods and re-used for hydrolytic reaction as required.
Mesoporous silica films were used as supports with high loading capacity and enzyme activity.
Abstract
We study the long-term radial transport of micron to millimeter-size grains in protostellar disks (PSDs) based on diffusion and viscosity coefficients measured from 3D global stratified-disk ...simulations with a Lagrangian hydrodynamic method. While gas drag tends to transport dust species radially inwards, stochastic diffusion can spread a considerable fraction of dust radially outwards (upstream) depending on the nature of turbulence. In gravitationally unstable disks, we measure a high radial diffusion coefficient
D
r
∼
H
2
Ω with little dependence on altitude. This leads to strong and vertically homogeneous upstream diffusion in early PSDs. In the solar nebula, the robust upstream diffusion of micron to millimeter-size grains not only efficiently transports highly refractory micron-size grains (such as those identified in the samples of comet 81P/Wild 2) from their regions of formation inside the snow line out to the Kuiper Belt, but can also spread millimeter-size calcium–aluminum-rich inclusions formed close to the Sun to distances where they can be assimilated into chondritic meteorites. In disks dominated by magnetorotational instability, the upstream diffusion effect is generally milder, with a separating feature due to diffusion being stronger in the surface layer than in the midplane. This variation becomes much more pronounced if we additionally consider a quiescent midplane with lower turbulence and larger characteristic dust size due to nonideal MHD effects. This segregation scenario helps to account for the dichotomy of the spatial distribution of two dust populations as observed in scattered light and Atacama Large Millimeter/submillimeter Array images.
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•Bio-methanol is employed as a feedstock for H2 produciton from bio-methanol steam reforming.•Cu-Ni / aluminate composites without organic template is used as catalysts to produces ...H2.•ANOVA analysis reveals that temperature is the primary factor affecting H2 productivity.•The catalysts achieve 100% bio-methanoal conversion and 2.93 mol / mol CH3OH H2 yield.•Long-term tests confirm the catalysts’ stability and effectivenes as a commercial one.
Hydrogen has emerged its importance for decarbonization to approach net-zero emissions in 2050. This study aims to develop three highly-porous Ni-Cu/Al2O3 catalysts (Ni-to-Cu weight ratio = 10 %, 20 %, and 30 %) for hydrogen production from the steam reforming of “Green” methanol (or bio-methanol). The prepared catalysts require no organic templates, thereby efficiently reducing unnecessary costs. With Taguchi orthogonal array design and analysis of variance (ANOVA), the impacts of selected operating factors on hydrogen productivity under ultrasonic sprays are investigated. The results reveal that the carrier gas flow rate is the most influential factor in H2 yield at the steam-to-methanol molar ratio (S/C) of 1.5, whereas the temperature is the most impactful factor at S/C = 2.0. The regression between the Taguchi effect value and the ANOVA F value develops a strong linear relationship. The optimal experimental conditions of Ni-Cu(30 %)/Al2O3, reaction temperature of 300 °C, N2 flow rate of 1,000 mL⋅min−1, and S/C = 2.0, achieve 100 % methanol conversion, 39.74 vol% H2 concentration in the product gas, and 2.93 mol⋅(mol CH3OH)-1 H2 yield. Thes data also show superior performance compared to those in the literature. In long-term stability tests, the prepared catalysts also exhibit high stability and effectiveness commensurate with commercialized Cu-based catalysts.
is widely used in Asian countries and its active constituents-ginsenosides-need to be systematically studied. However, only a small part of ginsenosides have been characterized in the roots and ...rhizomes of
(RRPG) up to date, mainly because of a lack of the fragmentation ions of many more ginsenosides. In order to comprehensively identify ginsenosides in RRPG, molecular features of ginsenosides orienting precursor ions selection and targeted tandem mass spectrometry (MS/MS) analysis strategy were proposed in our study, in which the precursor ions were selected according to the molecular features of ginsenosides irrespective of their peak abundances, and targeted MS/MS analysis was then performed to obtain their fragmentation ions for substance characterization. Using this strategy, a total of 620 ginsenosides were successfully characterized in RRPG, including 309 protopanaxadiol-type ginsenosides, 258 protopanaxatriol-type ginsenosides and 53 oleanane-type ginsenosides. It is worth noting that, except for the known aglycones mass-to-charge ratio (
) 459, 475 and 455, twelve other aglycones, including
509, 507, 493, 491, 489, 487, 477, 473, 461, 457, 443 and 441, were first reported in our experiment and they were probably the derivatizations of the protopanaxatriol and protopanaxadiol. Our study will not only help people to improve the cognition of ginsenosides in RRPG, but will also play a guiding and reference role for the isolation and characterization of potentially new ginsenosides from RRPG.
Melanoma is the deadliest form of skin cancer, and its incidence has continuously increased over the past 20 years. Therefore, the discovery of a novel targeted therapeutic strategy for melanoma is ...urgently needed. In our study, MTT-based cell proliferation assay, cell cycle, and apoptosis assays through flow cytometry, protein immunoblotting, protein immunoprecipitation, designing of melanoma xenograft models, and immunohistochemical/immunofluorescent assays were carried out to determine the detailed molecular mechanisms of a novel HSP90-PI3K dual inhibitor. Our compound, named DHP1808, was found to suppress A375 cell proliferation through apoptosis induction by activating the Fas/FasL signaling pathway; it also induced cell-cycle arrest and inhibited the cell migration and invasion of A375 cells by interfering with Hsp90-EGFR interactions and downstream signaling pathways. Our results indicate that DHP1808 could be a promising lead compound for the Hsp90/PI3K dual inhibitor.
was a traditional Chinese medicine with various pharmacological activities and one of its important activities was hypoglycemic activity; therefore,
has been used in China as an adjuvant in the ...treatment of diabetes mellitus. In vivo and in vitro tests have revealed that ginsenosides, which are derived from the roots and rhizomes of
have anti-diabetic effects and produce different hypoglycemic mechanisms by acting on some specific molecular targets, such as SGLT1, GLP-1, GLUTs, AMPK, and FOXO1. α-Glucosidase is another important hypoglycemic molecular target, and its inhibitors can inhibit the activity of α-Glucosidase so as to delay the absorption of dietary carbohydrates and finally reduce postprandial blood sugar. However, whether ginsenosides have the hypoglycemic mechanism of inhibiting α-Glucosidase activity, and which ginsenosides exactly attribute to the inhibitory effect as well as the inhibition degree are not clear, which needs to be addressed and systematically studied. To solve this problem, affinity ultrafiltration screening coupled with UPLC-ESI-Orbitrap-MS technology was used to systematically select α-Glucosidase inhibitors from
. The ligands were selected through our established effective data process workflow based on systematically analyzing all compounds in the sample and control specimens. As a result, a total of 24 α-Glucosidase inhibitors were selected from
, and it was the first time that ginsenosides were systematically studied for the inhibition of α-Glucosidase. Meanwhile, our study revealed that inhibiting α-Glucosidase activity probably was another important mechanism for ginsenosides treating diabetes mellitus. In addition, our established data process workflow can be used to select the active ligands from other natural products using affinity ultrafiltration screening.
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