Essential hypertension (EH) is a leading cause of cardiovascular morbidity and mortality. Fructus Tribuli (FT), as a traditional medicine, has been frequently used for thousands of years. The crude ...Fructus Tribuli (CFT), decoction pieces being processed to remove impurities, have been listed as an important medicine for the treatment of hypertension in the elderly. According to the theory of traditional Chinese medicine, the CFT can enhance the EH treatment after being stir-fried into stir-fried Fructus Tribuli (SFT). At present, whether the SFT can enhance the EH treatment and its potential pharmacodynamic substances and mechanism are unknown. In this study, an integrated "spectrum-effect relationship-network pharmacology-metabolomics" strategy was used. Using male spontaneously hypertensive rats as an experimental model, we compared the therapeutic effects of CFT and SFT on EH. Subsequently, to define the pharmacodynamic material basis of SFT in enhancing the EH treatment, the steroidal saponins (main active components of FT) were selected for spectrum-effect relationship analysis. Furthermore, we applied the joint pathway analysis of network pharmacology and metabolomics to explore the underlying mechanism of SFT in enhancing the EH treatment. Results showed that SFT was better than CFT in the EH treatment. The steroidal saponins transformed by stir-frying were the potential pharmacodynamic substances that SFT could enhance the EH treatment. And the mechanism of action might be associated with regulating glycerophospholipid metabolism and arachidonic acid metabolism, especially arachidonic acid metabolism. This study provided a scientific basis for the clinical use of SFT as an important medicine for the EH treatment.
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•Providing a basis for treating essential hypertension by stir-fried Fructus Tribuli.•Pharmacodynamic substances were steroidal saponins transformed by stir-frying.•Combined network pharmacology and metabolomics to explore the underlying mechanism.
Face swapping is an intriguing and intricate task in the field of computer vision. Currently, most mainstream face swapping methods employ face recognition models to extract identity features and ...inject them into the generation process. Nonetheless, such methods often struggle to effectively transfer identity information, which leads to generated results failing to achieve a high identity similarity to the source face. Furthermore, if we can accurately disentangle identity information, we can achieve controllable face swapping, thereby providing more choices to users. In pursuit of this goal, we propose a new face swapping framework (ControlFace) based on the disentanglement of identity information. We disentangle the structure and texture of the source face, encoding and characterizing them in the form of feature embeddings separately. According to the semantic level of each feature representation, we inject them into the corresponding feature mapper and fuse them adequately in the latent space of StyleGAN. Owing to such disentanglement of structure and texture, we are able to controllably transfer parts of the identity features. Extensive experiments and comparisons with state-of-the-art face swapping methods demonstrate the superiority of our face swapping framework in terms of transferring identity information, producing high-quality face images, and controllable face swapping.
Triple-negative breast cancer (TNBC) is a nasty disease with extremely high malignancy and poor prognosis. Annexin A3 (ANXA3) is a potential prognosis biomarker, displaying an excellent correlation ...of ANXA3 overexpression with patients' poor prognosis. Silencing the expression of ANXA3 effectively inhibits the proliferation and metastasis of TNBC, suggesting that ANXA3 can be a promising therapeutic target to treat TNBC. Herein, we report a first-in-class ANXA3-targeted small molecule (R)-SL18, which demonstrated excellent anti-proliferative and anti-invasive activities to TNBC cells. (R)-SL18 directly bound to ANXA3 and increased its ubiquitination, thereby inducing ANXA3 degradation with moderate family selectivity. Importantly, (R)-SL18 showed a safe and effective therapeutic potency in a high ANXA3-expressing TNBC patient-derived xenograft model. Furthermore, (R)-SL18 could reduce the β-catenin level, and accordingly inhibit the Wnt/β-catenin signaling pathway in TNBC cells. Collectively, our data suggested that targeting degradation of ANXA3 by (R)-SL18 possesses the potential to treat TNBC.
A potent and moderate selective ANXA3 degrader was developed and showed excellent efficacy in a TNBC patient-derived xenograft (PDX) model with high ANXA3 expression. Display omitted
Deepfake aims to swap a face of an image with someone else’s likeness in a reasonable manner. Existing methods usually perform deepfake frame by frame, thus ignoring video consistency and producing ...incoherent results. To address such a problem, we propose a novel framework Neural Identity Carrier (NICe), which learns identity transformation from an arbitrary face-swapping proxy via a U-Net. By modeling the incoherence between frames as noise, NICe naturally suppresses its disturbance and preserves primary identity information. Concretely, NICe inputs the original frame and learns transformation supervised by swapped pseudo labels. As the temporal incoherence has an uncertain or stochastic pattern, NICe can filter out such outliers and well maintain the target content by uncertainty prediction. With the predicted temporally stable appearance, NICe enhances its details by constraining 3D geometry consistency, making NICe learn fine-grained facial structure across the poses. In this way, NICe guarantees the temporal stableness of deepfake approaches and predicts detailed results against over-smoothness. Extensive experiments on benchmarks demonstrate that NICe significantly improves the quality of existing deepfake methods on video-level. Besides, data generated by our methods can benefit video-level deepfake detection methods.
•DESs are green solvents with unique physicochemical properties.•UAE-DESs was developed for extraction and determination of the dopamine from Portulaca oleracea L. leaves.•The approach was optimized ...by evaluating the influence of different parameters.•HPLC with fluorescent detection was developed for determination of dopamine in Portulaca oleracea L. leaves.
Deep eutectic solvents (DESs) are a recently developed class of green, efficient, and versatile alternatives to traditional organic solvents in natural product extractions. Inspired by the emergence of natural DESs and their green nature, we herein optimized the experimental variables for the extraction of dopamine from purslane (Portulaca oleracea L., POL) using DESs. Nine choline chloride (ChCl)-based DESs were tested to select the optimum solvent for ultrasound-assisted extraction (UAE), and the combination of ChCl:glycerol (1:2) with 30% water extracted more dopamine from POL than ethanol. The amount of dopamine in the extracts was quantified by HPLC equipped with a fluorescence detector. The influence of UAE treatment on the morphology of plant material was studied by SEM. Based on single-factor experiments, the UAE conditions were optimized by response surface methodology using the Box-Behnken design. The optimum conditions were: extraction time of 30 min, water content in DESs of 32%, temperature of 58 °C, and plant material-liquid ratio of 40 mg/mL, which resulted in 2.96 mg of dopamine per 1 g of POL. The percentage of water in DESs and the extraction temperature were the most significant factors influencing the extraction efficiency of dopamine from POL. The results of this study promote the application of DESs for green and efficient extractions of bioactive alkaloids and other target molecules from plant materials.
•The accuracy of FSCK and MGFSK in oxy-fuel flames is investigated.•MGFSK includes 3 correlated-K solution schemes and 2 grouping strategies.•MGFSK is more accurate than corresponding FSCK for both ...dry and wet oxy-fuel flames.•MGFSK reduces the dependence of FSCK on the reference (or Planck) temperature.•MGFSK reduces the dependence of FSCK on the flame scale.
Oxy-fuel combustion has drawn much attention as a promising CO2 capture and storage/sequestration technology. Radiative heat transfer of oxy-fuel flames is more important than that of conventional flames owing to higher concentrations of radiating gases. The Full-Spectrum Correlated K-distribution (FSCK) methods with original correlated-K scheme (Modest and Zhang, 2002), the improved one (Cai and Modest, 2014), and the rank correlated one (Solovjov and Webb, 2018) provide obvious errors in the low-temperature regions of dry and wet oxy-fuel flames. To improve the accuracy of FSCK, the accuracy of the Multi-Group FSK (MGFSK) method with the three correlated-K schemes and two grouping strategies based on the scaling function and intervals of comonotonicity are investigated in two 1D, a 2D and a 3D oxy-fuel flames. The results show that MGFSK with different correlated-K schemes and grouping strategies demonstrate better accuracies than corresponding FSCK for both dry and wet oxy-fuel flames. MGFSK reduce the dependence of FSCK on the reference (or Planck) temperature and flame scale. The volume-averaged mole fractions of the maximum and minimum temperatures are recommend as the high- and low-temperature grouping states respectively. Dividing the spectral absorption coefficients into 2 to 4 groups is a good compromise between accuracy and efficiency.
Nitrogen-doping can increase the charge density and the wettability of electrode materials, to further reinforce the electrochemical performances of energy storage devices. It is difficult to ...directly convert small molecular nitrogen-containing organics into N-doped porous carbon materials. Here we demonstrate a bottom-up strategy to prepare N-doped porous carbons by sodium metal-assisted carbonization of pyrrole. Pyrrole is not only a nitrogen source, but also a carbon source. In the process of pyrolysis, sodium assists the formation of the thermally stable polymer structures and catalyzes the graphitization of carbonaceous structures. As the pyrolysis temperature increases, the microstructures of porous carbons become more ordered and the pore structures of porous carbons change from the micropore-dominated structures to the mesopore-dominated structures. The material obtained at 800 °C with the nitrogen content of circa 3.3 wt% displays high-rate performances and long lifetime, when used as the supercapacitor electrodes. The device delivers 14.4 W h kg−1 (8.7 W h L−1) at a high power density of 40.5 kW kg−1 (24.5 kW L−1) and 20.9 W h kg−1 (12.6 W h L−1) at a power density of 13.5 kW kg−1 (8.2 kW L−1). Simultaneously, the technique provides a new idea for the preparation of other heteroatoms-doped porous carbons.
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A series of pyrimidine-bridged CA-4 derivatives (9a-u) targeting colchicine site were designed, synthesized and evaluated. Among them, the most potent compound 9j showed favorable anti-proliferative ...activities against a panel of cervical cancer cells (IC50 = 0.09–0.15 μM) and tubulin polymerization inhibitory activity (IC50 = 4.6 μM). Meanwhile, compound 9j exhibited superior anti-proliferative activity against cisplatin-resistant HeLa/DDP and SiHa/DDP cells than CA-4 and cisplatin. Particularly, the combination of 30 mg/kg 9j with 3 mg/kg cisplatin resulted in a 73% tumor suppression rate in HeLa xenograft model and reduced the renal dysfunction and injuries caused by high doses of cisplatin. Moreover, 9j was highly selective over the normal human proximal tubular cells (HK-2 cells, IC50 = 188 μM). Mechanism studies revealed that 9j could disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Further druggability characterization in terms of pharmacokinetic profile, acute toxicity, and hERG inhibition confirmed 9j could serve as a promising and safe combination agent for cervical cancer therapy.
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•Novel pyrimidine-bridged CA-4 analogs targeting colchicine site were synthesized as anti-cervical cancer agents.•9j exhibited superior anti-proliferative activity against DDP-resistant cervical cancer cells than CA-4.•9j showed high selectivity against normal human proximal tubular cells (HK-2 cells, IC50 = 188 μM).•Combination of 9j with DDP could improve TGI value to 73% and reduce renal damage caused by high dosage of DDP.
•Recent researches on face swapping methods focus on adjusting the identity extraction methods on one-shot scenarios. However, no matter how these models are adjusted, the identity information is ...always obtained from one shot source image. In other words, the identity information these methods leverage are guessed by a prior model. To achieve better performance, we develop an integrated, flexible and extensible framework, DeepFaceLab, to conduct cinema-level face-swapping with multi-shot data.•To make our framework practical, we invente a lot of auxiliary tools in each steps of DeepFaceLab. We develop a lot of human-in-the-loop designes in the whole framework. For examples, DeepFaceLab can swap any area of faces and conduct high-quality face-swapping even under heavy occlusion with the help of few-shot human labeling and XSeg. There are also dozens of image editing algorithms available in the mergence phase to generate satisfactory results.•DeepFaceLab is the leading software for creating deepfakes. As an open-source project, DeepFaceLab has obtained more than 35,000 stars on Github.
Face swapping has drawn a lot of attention for its compelling performance. However, current deepfake methods suffer the effects of obscure workflow and poor performance. To solve these problems, we present DeepFaceLab, the current dominant deepfake framework for practical face-swapping. It provides the necessary tools as well as an easy-to-use way to conduct high-quality face-swapping. It also offers a flexible and loose coupling structure for people who need to strengthen their pipeline with other features without writing complicated boilerplate code. We detail the principles that drive the implementation of DeepFaceLab and introduce its pipeline. DeepFaceLab could achieve cinema-level results with high fidelity as our supplemental video shows. We also demonstrate the advantage of our system by comparing our approach with other face-swapping methods.
Deepfake defense not only requires the research of detection but also requires the efforts of generation methods. As for a popular and practical toolkit, we encourage users to promote harmless deepfake-entertainment content on social media, reminding the public of the existence of deepfake when they are looking for entertainment.
Traditional synthesis methods of mesoporous carbon include hard templates (e.g., metal oxides, metal salts and mesoporous silica) and soft templates (e.g., surfactant and block copolymer). However, ...complicated and time-consuming procedures, high template costs, and harsh preparation conditions hinder the scale-up of these methods. Here, we report a simple and bottom-up strategy to synthesize mesoporous carbon by using the sodium-assisted carbonization of bromobenzene without additional templates added. Depending on the pyrolysis temperature, the obtained material with nanorod structures has a high surface area of 1902 m2 g−1, a large pore volume of 1.21 cm3 g−1 and a high degree of graphitization. Meanwhile, the pore-forming mechanism of this strategy is explored and attributed to the “in situ templating” effect of NaBr. The resultant material at 800 °C shows considerable rate performance, long lifetime and high power density. Additionally, the versatility and feasibility of the technique are validated via carbonization of six halogenated aromatic hydrocarbons by three alkali metals. Compared with lithium and potassium, sodium has better pore-forming effect and the obtained products possess a high surface area (1450–2100 m2 g−1) and a large pore volume (1.1–1.6 cm3 g−1). Furthermore, these mesoporous carbons show high adsorption capacity on dye macromolecules.
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