Copper-catalyzed tandem cyclization reaction of ethynylbenzoxazinones and thiols: facile construction of 2-thiomethylene indoles.

The first successful copper-catalyzed decarboxylative cyclization reaction of ethynylbenzoxazinones and thiols has been developed. A rarely studied α-addition process to a copper-allenylidene intermediate promoted this reaction. Using this protocol, a range of 2-thiomethylene indole compounds have been obtained. This methodology offers significant advantages including mild reaction conditions, cheap catalysts, good yields and broad substrate compatibility.

Contrast-enhanced magnetic resonance image segmentation based on improved U-Net and Inception-ResNet in the diagnosis of spinal metastases.

Objective: The objective of this study was to investigate the use of contrast-enhanced magnetic resonance imaging (CE-MRI) combined with radiomics and deep learning technology for the identification of spinal metastases and primary malignant spinal bone tumor. Methods: The region growing algorithm was utilized to segment the lesions, and two parameters were defined based on the region of interest (ROI). Deep learning algorithms were employed: improved U-Net, which utilized CE-MRI parameter maps as input, and used 10 layers of CE images as input. Inception-ResNet model was used to extract relevant features for disease identification and construct a diagnosis classifier. Results: The diagnostic accuracy of radiomics was 0.74, while the average diagnostic accuracy of improved U-Net was 0.98, respectively. the PA of our model is as high as 98.001%. The findings indicate that CE-MRI based radiomics and deep learning have the potential to assist in the differential diagnosis of spinal metastases and primary malignant spinal bone tumor. Conclusion: CE-MRI combined with radiomics and deep learning technology can potentially assist in the differential diagnosis of spinal metastases and primary malignant spinal bone tumor, providing a promising approach for clinical diagnosis.

Dihydromyricetin protects against lipopolysaccharide­induced cardiomyocyte injury through the toll­like receptor­4/nuclear factor­κB pathway.

Dihydromyricetin (DHM) is a bioactive flavonoid compound extracted from the stems and leaves of Ampelopsis grossedentata. Previous studies have indicated that DHM has antioxidation and antitumor capabilities, while the effect of DHM on lipopolysaccharide (LPS)­induced cardiomyocyte injury has not been clarified. Therefore, the aim of the present study was to investigate the effect of DHM on LPS­induced cardiomyocyte injury. In the present study, cardiomyocytes were randomized to the control (PBS), LPS and DHM + LPS groups. The LPS group was treated with 10 µg/ml LPS for 12 h and the DHM + LPS group was treated with 100 or 25 µM DHM 12 h prior to treatment with LPS. The protective effect of DHM on LPS­induced cardiomyocytes injury was evaluated by Cell Counting kit­8 assay, TUNEL staining, reverse transcription­quantitative polymerase chain reaction and western blot analysis. The results demonstrated that LPS treatment led to cardiomyocyte apoptosis, and these effects were significantly attenuated by DHM. Furthermore, LPS treatment downregulated the expression of B­cell lymphoma 2 apoptosis regulator (Bcl­2) and induced increased expression of Bcl­2­associated X apoptosis regulator (Bax). Additionally, DHM treatment reversed LPS­induced changes in Bcl­2 expression and Bax expression in cardiomyocytes, and rescued cells from apoptosis. In addition, increased mRNA expression levels of tumor necrosis factor­α and interleukin­6 induced by LPS were attenuated following treatment with DHM. Further investigation demonstrated that DHM suppressed the activation of toll­like receptor­4 (TLR4), which is involved in regulating the downstream signaling pathway of nuclear factor­κB (NF­κB). DHM attenuated LPS­induced cardiomyocyte injury, the potential mechanism responsible for this effect may involve inhibition of TLR4 activation and subsequent regulation of the associated downstream signaling pathway of NF­κB. The current study indicates that DHM may protect cardiomyocytes against LPS­induced injury by inhibition of the TLR4/NF­κB signaling pathway. The results of the present study may provide support for the development DHM as a strategy for the treatment of heart failure in septic shock.

Grape seed proanthocyanidin extract attenuates airway inflammation and hyperresponsiveness in a murine model of asthma by downregulating inducible nitric oxide synthase.

Allergic asthma is characterized by hyperresponsiveness and inflammation of the airway with increased expression of inducible nitric oxide synthase (iNOS) and overproduction of nitric oxide (NO). Grape seed proanthocyanidin extract (GSPE) has been proved to have antioxidant, antitumor, anti-inflammatory, and other pharmacological effects. The purpose of this study was to examine the role of GSPE on airway inflammation and hyperresponsiveness in a mouse model of allergic asthma. BALB/c mice, sensitized and challenged with ovalbumin (OVA), were intraperitoneally injected with GSPE. Administration of GSPE remarkably suppressed airway resistance and reduced the total inflammatory cell and eosinophil counts in BALF. Treatment with GSPE significantly enhanced the interferon (IFN)- γ level and decreased interleukin (IL)-4 and IL-13 levels in BALF and total IgE levels in serum. GSPE also attenuated allergen-induced lung eosinophilic inflammation and mucus-producing goblet cells in the airway. The elevated iNOS expression observed in the OVA mice was significantly inhibited by GSPE. In conclusion, GSPE decreases the progression of airway inflammation and hyperresponsiveness by downregulating the iNOS expression, promising to have a potential in the treatment of allergic asthma.

Crystal habit-tuned nanoplate material of Li[Li1/3-2x/3NixMn2/3-x/3]O2 for high-rate performance lithium-ion batteries.

A cathode for high-rate performance lithium-ion batteries (LIBs) has been developed from a crystal habit-tuned nanoplate Li(Li(0.17)Ni(0.25)Mn(0.58))O2 material, in which the proportion of (010) nanoplates (see figure) has been significantly increased. The results demonstrate that the fraction of the surface that is electrochemically active for Li(+) transportation is a key criterion for evaluating the different nanostructures of potential LIB materials.