Substituted indole derivatives as UNC-51-like kinase 1 inhibitors: Design, synthesis and anti-hepatocellular carcinoma activity.

The five-year survival rate for patients with hepatocellular carcinoma (HCC) is only 20 %, highlighting the urgent need to identify new therapeutic targets and develop potential therapeutic options to improve patient prognosis. One promising approach is inhibiting autophagy as a strategy for HCC treatment. In this study, we established a virtual docking conformation of the autophagy promoter ULK1 binding XST-14 derivatives.

Multi-Omics Research Accelerates the Clarification of the Formation Mechanism and the Influence of Leaf Color Variation in Tea () Plants.

Tea is a popular beverage with characteristic functional and flavor qualities, known to be rich in bioactive metabolites such as tea polyphenols and theanine. Recently, tea varieties with variations in leaf color have been widely used in agriculture production due to their potential advantages in terms of tea quality. Numerous studies have used genome, transcriptome, metabolome, proteome, and lipidome methods to uncover the causes of leaf color variations and investigate their impacts on the accumulation of crucial bioactive metabolites in tea plants.

Design and synthesis of dabigatran etexilate derivatives with inhibiting thrombin activity for hepatocellular carcinoma treatment.

Hepatocellular carcinoma (HCC) is one of the most fatal solid malignancies worldwide. Evidence suggests that thrombin stimulates tumor progression via fibrin formation and platelet activation. Meanwhile, we also found a correlation between thrombin and HCC through bioinformatics analysis.

Efficacy, Mechanism, and Structure-Activity Relationship of 6-Methoxy Benzofuran Derivatives as a Useful Tool for Senile Osteoporosis.

Most patients with senile osteoporosis (SOP) are severely deficient in bone mass, and treatments using bone resorption inhibitors, such as bisphosphonates, have shown limited efficacy. Small-molecule osteogenesis-promoting drugs are required to improve the treatment for this disease. Previously, we demonstrated that a compound with a benzofuran-like structure promoted bone formation by upregulating BMP-2, and it exhibited a therapeutic effect in SAMP-6 mice, glucocorticoid-induced osteoporosis rats, and ovariectomized rats.

Structure-based virtual screening identified novel FOXM1 inhibitors as the lead compounds for ovarian cancer.

Ovarian cancer (OC) is a gynecological tumor with possibly the worst prognosis, its 5-year survival rate being only 47.4%. The first line of therapy prescribed is chemotherapy consisting of platinum and paclitaxel.

Self-adhesive PMIA membranes with chitosan porous beads immobilized pullulanase for efficient biological aging of beer.

A novel pulluanase@chitosan porous beads/Poly (m-phthaloyl-m-phenylenediamine) (PULL@CPB/PMIA) membrane with good separation and biocatalysis properties was prepared by a self-adhesive method by introducing an immobilized enzyme (PULL@CPB) onto the PMIA membrane. The combination of PULL@CPB and PMIA could increase the one-step refining of protoplasmic beer as well as the ability of biocatalysis to lower the alcohol-to-ester ratio. The experimental results showed that the addition of PULL@CPB and the increase in the ratio of EtOH/water in the coagulation bath both increased the load of pullulanase on the membrane surface, while excessive addition decreased the activity of pullulanase.

Crystal structure and pale-yellow emitting properties of KGdDyBO solid solutions.

A new potassium dysprosium polyborate, KDyBO, has been prepared via the high-temperature molten salt method and structurally characterized by single-crystal X-ray diffraction analysis. The structure can be described as a three-dimensional framework composed of isolated bicyclic [BO] groups and Dy and K ions. The Fourier transform IR (FT-IR) and ultraviolet-visible (UV-Vis) spectra were investigated.

Novel Metabolites from the Endophytic Fungus Chaetomium subaffine L01.

One natural p-terphenyl glycoside, gliocladinin C, and two furano-polyene derivatives, chaetominins A and B, were isolated from potato endophytic fungus Chaetomium subaffine. The absolute configurations of these compounds were elucidated by HR-ESI-MS, NMR, the DP4+ probabilities and electronic circular dichroism (ECD) spectra. Furthermore, gliocladinin C and chaetominin A showed cytotoxic activity against two selected human tumor cell lines (Hep-2 and HepG-2).

KEu(PO): hydrothermal synthesis, crystal structure and photoluminescence properties.

An anhydrous orthophosphate, KEu(PO) (tripotassium pentaeuropium hexaphosphate), has been prepared by a high-temperature solid-state reaction combined with hydrothermal synthesis, and its crystal structure was determined by single-crystal X-ray diffraction analysis (SC-XRD). The results show that the compound crystallizes in the monoclinic space group C2/c and the structure features a three-dimensional framework of [Eu(PO)], with the tunnel filled by K ions. The IR spectrum, UV-Vis spectrum and luminescence properties of polycrystalline samples of KEu(PO), annealed at temperatures of 650, 700, 750, 800 and 850 °C, were investigated.

[Vertical distribution characteristics and temporal stability of soil water in deep profile on the Loess Tableland, Northwest China.].

Study of impacts of land uses on spatiotemporal dynamics of soil water content (SWC) is of great significance for understanding the performance characteristics of regional water cycling under changing environment. Based on long-term located field observations, this paper explored the temporal dynamics of soil water in 0-15 m soil profile under four land use types on the Loess Tableland from September 2012 to December 2015. Results showed that the annually averaged SWCs over the 0-15 m soil profile for alfalfa field, fallow field, fertilized cropland and unfertilized cropland were 15.

Protective effect of heme oxygenase-1 on Wistar rats with heart failure through the inhibition of inflammation and amelioration of intestinal microcirculation.

Background: Myocardial infarction (MI) has likely contributed to the increased prevalence of heart failure (HF). As a result of reduced cardiac function, splanchnic blood flow decreases, causing ischemia in villi and damage to the intestinal barrier. The induction of heme oxygenase-1 (HO-1) could prevent, or lessen the effects of stress and inflammation.