A New Orientation Detection Method for Tilting Insulators Incorporating Angle Regression and Priori Constraints.

The accurate detection of insulators is an important prerequisite for insulator fault diagnosis. To solve the problem of background interference and overlap caused by the axis-aligned bounding boxes in the tilting insulator detection tasks, we construct an improved detection architecture according to the scale and tilt features of the insulators from several perspectives, such as bounding box representation, loss function, and anchor box construction. A new orientation detection method for tilting insulators based on angle regression and priori constraints is put forward in this paper. Ablation tests and comparative validation tests were conducted on a self-built aerial insulator image dataset. The results show that the detection accuracy of our model was increased by 7.98% compared with that of the baseline, and the overall detection accuracy reached 82.33%. Moreover, the detection effect of our method was better than that of the YOLOv5 detection model and other orientation detection models. Our model provides a new idea for the accurate orientation detection of insulators.

A New Bolt Defect Identification Method Incorporating Attention Mechanism and Wide Residual Networks.

Bolts are important components on transmission lines, and the timely detection and exclusion of their abnormal conditions are imperative to ensure the stable operation of transmission lines. To accurately identify bolt defects, we propose a bolt defect identification method incorporating an attention mechanism and wide residual networks. Firstly, the spatial dimension of the feature map is compressed by the spatial compression network to obtain the global features of the channel dimension and enhance the attention of the network to the vital information in a weighted way. After that, the enhanced feature map is decomposed into two one-dimensional feature vectors by embedding a cooperative attention mechanism to establish long-term dependencies in one spatial direction and preserve precise location information in the other direction. During this process, the prior knowledge of the bolts is utilized to help the network extract critical feature information more accurately, thus improving the accuracy of recognition. The test results show that the bolt recognition accuracy of this method is improved to 94.57% compared with that before embedding the attention mechanism, which verifies the validity of the proposed method.

Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.

Piperlongumine 1 increases reactive oxygen species (ROS) levels and preferably induces cancer cell apoptosis by triggering different pathways. However, the poor solubility of 1 limits its intensive investigation and clinical application. Ligustrazine possesses a water-soluble pyrazine skeleton and can inhibit proliferation and metastasis of cancer cells. We synthesized compound 3 by replacement of the trimethoxyphenyl of 1 with ligustrazine moiety and further introduced 2-Cl, -Br, and -I to 3 for synthesis of 4-6, respectively. Compound 4 possessed 14-fold greater aqueous solubility than 1 and increased ROS levels in colorectal cancer HCT-116 cells. Additionally, 4 preferably inhibited proliferation, migration, invasion, and heteroadhesion of HCT-116 cells. Treatment with 4 suppressed tumor growth and lung metastasis in vivo and prolonged the survival of tumor-bearing mice. Furthermore, 4 mitigated TGF-ß1-induced epithelial-mesenchymal transition and Wnt/ß-catenin activation by inhibiting the Akt and GSK-3ß phosphorylation in HCT-116 cells. Collectively, 4 displayed significant antiproliferation and antimetastasis activities, superior to 1.

Fragment-based discovery of novel pentacyclic triterpenoid derivatives as cholesteryl ester transfer protein inhibitors.

Cholesteryl Ester Transfer Protein (CETP) is an important therapeutic target for the treatment of atherosclerotic cardiovascular disease. Our molecular modeling study revealed that pentacyclic triterpenoid compounds could mimic the protein-ligand interactions of the endogenous ligand cholesteryl ester (CE) by occupying its binding site. Alignment of the docking conformations of oleanolic acid (OA), ursolic acid (UA) and the crystal conformations of known CETP inhibitor Torcetrapib in the active site proposed the applicability of fragment-based drug design (FBDD) approaches in this study. Accordingly, a series of pentacyclic triterpenoid derivatives have been designed and synthesized as novel CETP inhibitors. The most potent compound 12e (IC50:0.28 µM) validated our strategy for molecular design. Molecular dynamics simulations illustrated that the more stable hydrogen bond interaction of the UA derivative 12e with Ser191 and stronger hydrophobic interactions with Val198, Phe463 than those of OA derivative 12b mainly led to their significantly different CETP inhibitory activity. These novel potent CETP inhibitors based on ursane-type scaffold should deserve further investigation.