The flavonoids from the fruits of Psoralea corylifolia and their potential in inhibiting metastasis of human non-small cell lung cancers.

Nineteen flavonoids were isolated from the fruits of Psoralea corylifolia L., including a novel flavanol (3) and three novel isoflavones (12-14). Their chemical structures were unequivocally determined through comprehensive spectral data analysis. The anti-proliferative effect of the isolated flavonoids was assessed in vitro using the MTT assay. Molecular docking and ELISA were employed to determine the inhibitory effects of the active compounds on ALK5. Isobavachalcone was found to inhibit TGF-ß1 induced EMT in A549 cells by Wound healing assay and Transwell chamber assay. Immunofluorescence assay and Western blot assay showed that IBC could inhibit cytoskeleton rearrangement, reduce the phosphorylation of ALK5, ERK, and Smad, down-regulate Snail expression, and up-regulate E-cadherin expression in TGF-ß1 induced A549 cells, thereby exerting the potential inhibitory effects on epithelial-mesenchymal transition (EMT) process in A549 cells. The findings presented herein establish a fundamental basis for investigating the anti-proliferative and anti-metastatic properties of psoralen flavonoids in human non-small cell lung cancer.

Inhibition of piezo1 prevents chronic cerebral hypoperfusion-induced cognitive impairment and blood brain barrier disruption.

Chronic cerebral hypoperfusion (CCH) plays a critical role in the onset and progression of vascular dementia (VD), which is now recognized as the second most common form of dementia after Alzheimer's disease (AD). The mechanosensitive piezo1 channel has been identified to play important roles in several neurological disorders. However, the roles and possible mechanisms of piezo1 in CCH-induced cognitive decline and blood brain barrier (BBB) disruption, as well as the underlying mechanisms remain elusive. In this study, the CCH model was established by bilateral common carotid artery occlusion in rats and by oxygen and glucose deprivation/reoxygenation (OGD/R) in bEnd.3 cells. The results demonstrated that the antagonist of piezo1 GsMTx4 ameliorated CCH-induced cognitive dysfunction and mitigated cerebral edema. Furthermore, this study indicated that GsMTx4 improved the permeability and integrity of BBB and protected cerebral microvasculature after CCH. In vitro, GsMTx4 improved cell viability, promoted the ability of cell motility and migration, and inhibited the degradation of BBB integrity-related proteins by inhibiting NLRP3 inflammasome activation. In addition, NLRP3 agonist abolished the beneficial effects of GsMTx4. Collectively, our results demonstrate that piezo1 might be involved in CCH-induced cognitive impairment and BBB damage, which may be at least partially mediated through regulation of NLRP3 inflammasome.

Antichilblain Components in Eggplant Based on Network Pharmacology and Biological Evaluation.

Eggplant, the fruit of Solanum melongena L. (Solanaceae), is applied externally to relieve the symptoms of chilblains in the folk in East Asia. However, the mechanisms and biological ingredients are not clear. A network pharmacology approach was used to shed light on the mechanisms of eggplant against chilblains, which illustrated that anti-inflammation and antioxidation are mainly involved in the curative effects. Bioassay-guided assays led to the isolation of 44 ingredients (1-44), including two new natural compounds (1-2) and 42 known compounds. Thirteen compounds (3-15) were first reported from the Solanum genus. The anti-inflammatory and antioxidative effects of all isolates were evaluated, and the results showed that 11 compounds have anti-inflammatory activity and 27 have antioxidant activity. Fatty acids, flavonoids, alkaloids, phenolic acids, saponins, and lignans from eggplant have certain anti-inflammatory and antioxidant effects. These results provide a scientific basis for eggplant to treat chilblains.

Improving the Accuracy of an R-CNN-Based Crack Identification System Using Different Preprocessing Algorithms.

The accurate intelligent identification and detection of road cracks is a key issue in road maintenance, and it has become popular to perform this task through the field of computer vision. In this paper, we proposed a deep learning-based crack detection method that initially uses the idea of image sparse representation and compressed sensing to preprocess the datasets. Only the pixels that represent the crack features remain, while most pixels of non-crack features are relatively sparse, which can significantly improve the accuracy and efficiency of crack identification. The proposed method achieved good results based on the limited datasets of crack images. Various algorithms were tested, namely, linear smooth, median filtering, Gaussian smooth, and grayscale threshold, where the optimal parameters of the various algorithms were analyzed and trained with faster regions with convolutional neural network features (faster R-CNN). The results of the experiments showed that the proposed method has good robustness, with higher detection efficiency in the presence of, for example, road markings, shallow cracks, multiple cracks, and blurring. The result shows that the improvement of mean average precision (mAP) can reach 5% compared with the original method.

Effects of MaiLiuPian on carotid thrombosis in rats and acute pulmonary embolism in mice and its antithrombotic mechanism.

Mailiupian (MLP) is a new patent functional food that consists of Crataegi Fructus, Notoginseng Radix, and Ginkgo Folium, which was reported to be active in improving the microcirculation based on formulation screening. However, whether it is effective in inhibiting thrombus and its mechanism has not been evaluated. Therefore, in the present study, the models of arterial thrombosis induced by FeCl3 and the models of APE by ADP were established to evaluate the antithrombosis effect of MLP. Results showed that MLP markedly reduced the weight and size of wet thrombosis in FeCl3 -induced rats and decreased the recovery time from symptoms of APE mice. MLP was proved to prolong APTT, PT, TT and improve the levels of t-PA and 6-keto-PGF1α significantly, meanwhile, PAI-1 and TXB2 were reduced apparently. By comparing tail bleeding time, MLP showed antithrombotic effects, but without the risk of bleeding, taking aspirin as a control. PRACTICAL APPLICATIONS: Our experiments proved that MLP, a new patent health food, acted on both coagulation and fibrinolytic systems and the platelet aggregation to play antithrombosis roles, providing a theoretical basis for applications of MLP in preventing or curing thrombosis diseases.

Crack Detection and Comparison Study Based on Faster R-CNN and Mask R-CNN.

The intelligent crack detection method is an important guarantee for the realization of intelligent operation and maintenance, and it is of great significance to traffic safety. In recent years, the recognition of road pavement cracks based on computer vision has attracted increasing attention. With the technological breakthroughs of general deep learning algorithms in recent years, detection algorithms based on deep learning and convolutional neural networks have achieved better results in the field of crack recognition. In this paper, deep learning is investigated to intelligently detect road cracks, and Faster R-CNN and Mask R-CNN are compared and analyzed. The results show that the joint training strategy is very effective, and we are able to ensure that both Faster R-CNN and Mask R-CNN complete the crack detection task when trained with only 130+ images and can outperform YOLOv3. However, the joint training strategy causes a degradation in the effectiveness of the bounding box detected by Mask R-CNN.

Three new compounds from the dried root bark of Wikstroemia indica and their cytotoxicity against HeLa cells.

Three new compounds (1-3) and twelve known compounds (4-15) were isolated from the n-butanol extraction of the 70% ethanol extract of the dried root barks of Wikstroemia indica. The structures of new compounds were identified by chemical evidence and extensive analysis of spectroscopic data (HR-ESI-MS, 1 D and 2 D NMR) and ECD calculations. All isolated compounds were evaluated for their cytotoxicity against HeLa cells using MTT assay and the results showed that daphnoretin (compound 5) owned the highest cytotoxicity against HeLa cells (IC50=28.89 µmol/L).

The effects of cryopreservation on the acrosome structure, enzyme activity, motility, and fertility of bovine, ovine, and goat sperm.

The study was designed to investigate the effects of cryopreservation on bovine, ovine, and goat sperm motility, acrosome structure, enzyme activity, and fertilization ability. Percentage of sperm with hyaluronidase enzyme (HYD) activity was detected by a modified sodium hyaluronate-gelatin membrane. The N-α-benzoyl-DL-arginine-p-nitroanilide (BNPNA) method was used to assess the sperm acrosome enzyme (ACE). The mean percentage of sperm acrosome integrity dropped significantly (P < 0.01) after cryopreservation. The ACE activity of bovine sperm (100.48) was higher (P < 0.01) than that of ovine (57.88) or goat sperm (50.30), while the percentage of sperm with HYD activity of bovine (71.10%) and ovine (67.60%) sperm was higher than that of goat sperm (58.52%) after cryopreservation (P < 0.01). Sperm motility was positively correlated with the activity of the two acrosome enzymes before and after cryopreservation (P < 0.01). Cryopreservation had a negative effect on acrosomal morphology, motility, and acrosomal enzyme activity in their sperm. The fertilization ability of ovine and goat sperm decreased significantly after cryopreservation, but that of frozen bovine sperm did not differ significantly when compared with fresh sperm. There was no significant difference between ovine and goat sperm indices, except for percentage of sperm with HYD activity.

Deformation of the aquifer system under groundwater level fluctuations and its implication for land subsidence control in the Tianjin coastal region.

This study demonstrates characteristics and mechanisms of deformation of an aquifer system in response to seasonal fluctuations of groundwater level when groundwater pumping has been strictly regulated after experiencing longtime land subsidence. Two boreholes with depth of 1226 m (G2 site) and 905 m (G3 site) were drilled at the Tianjin coastal region where severe land subsidence had occurred since the 1950s. Extensometer/piezometer groups installed at the G2 site illustrate synchronized variations of compaction and groundwater level since 2010 in the aquifer system between depth of 100-400 m which contributes most groundwater pumpage. Monitored land subsidence demonstrates that the shallow aquifer has become the main contributor to the land subsidence, and inelastic compaction still occurred in the aquifers where groundwater level has recovered. Pre-consolidation stresses show that clayey soils in depth < 100 m are under-consolidated, and deep clayey soils show the state of normal- to over-consolidation. The effects of the cyclic groundwater level oscillation on deformation were investigated using repeated loading and unloading tests. Void ratio changes in loading/unloading cycles illustrate that inelastic deformation rate decreases gradually and elastic deformation rate remains almost unchanged with increases of cyclic numbers. The deformation of soil samples from 100 to 400 m is mostly elastic for loading stress in the over-consolidation stress range. These findings suggest that groundwater dewatering in the shallow (depth < 100 m) aquifer will be the primary target to control land subsidence. Groundwater level fluctuations higher than pre-consolidation value in 100-400 m only lead to elastic and recoverable deformation even small residual permanent deformation may continue for a long time. The results improve the understanding of deformation in complex urban aquifers affected by groundwater level fluctuations and highlight the importance of city planning management for controlling land subsidence in coastal cities.