Deep learning-based discovery of compounds for blood pressure lowering effects.

The hypotensive side effects caused by drugs during their use have been a vexing issue. Recent studies have found that deep learning can effectively predict the biological activity of compounds by mining patterns and rules in the data, providing a potential solution for identifying drug side effects. In this study, we established a deep learning-based predictive model, utilizing a data set comprised of compounds known to either elevate or lower blood pressure.

Design, synthesis and FXR partial agonistic activity of anthranilic acid derivatives bearing aryloxy moiety as therapeutic agents for metabolic dysfunction-associated steatohepatitis.

Farnesoid X receptor (FXR) is considered a promising therapeutic target for the treatment of metabolic dysfunction-associated steatohepatitis (MASH). Increasing evidence suggests that targeting FXR with full agonists may lead to side effects. FXR partial agonists, which moderately activate FXR signaling, are emerging as a feasible approach to mitigate side effects and address MASH.

p-Hydroxy benzaldehyde, a phenolic compound from Nostoc commune, ameliorates DSS-induced colitis against oxidative stress via the Nrf2/HO-1/NQO-1/NF-κB/AP-1 pathway.

Background: Ulcerative colitis (UC), a chronic idiopathic inflammatory bowel disease (IBD), presents with limited current drug treatment options. Consequently, the search for safe and effective drug for UC prevention and treatment is imperative. Our prior studies have demonstrated that the phenolic compound p-Hydroxybenzaldehyde (HD) from Nostoc commune, effectively mitigates intestinal inflammation.

VT204: A Potential Small Molecule Inhibitor Targeting KRASG12C Mutation for Therapeutic Intervention in Non-Small Cell Lung Cancer.

The development of effective treatments for non-small cell lung cancer (NSCLC), particularly targeting the KRASG12C mutation, remains a challenge. In this study, we investigated the therapeutic potential of VT204, a small molecule inhibitor of KRASG12C, in NSCLC. To achieve the objectives, we conducted a comprehensive set of experimental methods.

FXR activation remodels hepatic and intestinal transcriptional landscapes in metabolic dysfunction-associated steatohepatitis.

The escalating obesity epidemic and aging population have propelled metabolic dysfunction-associated steatohepatitis (MASH) to the forefront of public health concerns. The activation of FXR shows promise to combat MASH and its detrimental consequences. However, the specific alterations within the MASH-related transcriptional network remain elusive, hindering the development of more precise and effective therapeutic strategies.

Sodium p-hydroxybenzoate alleviates osteoporosis through inhibiting bone metabolism and oxidative stress via activating ERα.

As the population ages, the incidence of osteoporosis (OP) gradually increases and is becoming a growing public health problem. Meanwhile, although traditional pharmacological therapy is extremely efficient in the treatment of OP, its application is constrained because of irreversible adverse drug reactions. Therefore, scientists should actively develop safer drugs while ensuring the therapeutic effect of OP.

Licochalcone A induces cell cycle arrest and apoptosis via suppressing MAPK signaling pathway and the expression of FBXO5 in lung squamous cell cancer.

Lung squamous cell carcinoma (LSCC) is a highly heterogeneous malignancy with high mortality and few therapeutic options. Licochalcone A (LCA, PubChem ID: 5318998) is a chalcone extracted from licorice and possesses anticancer and anti‑inflammatory activities. The present study aimed to elucidate the anticancer effect of LCA on LSCC and explore the conceivable molecular mechanism.

Relative safety and efficacy of topical and oral NSAIDs in the treatment of osteoarthritis: A systematic review and meta-analysis.

Background: Osteoarthritis (OA) often affects the hands, knees, and hip joints, causing considerable pain and disability, and often affecting the patient's quality of life. Non-steroidal anti-inflammatory drugs (NSAIDs) are common pain relievers often applied as first line therapies for OA. However, prolonged NSAIDs application can have unwanted side effects.

A novel ALG10/TGF-β positive regulatory loop contributes to the stemness of colorectal cancer.

The roles of asparagine-linked glycosylation (ALG) members in tumorigenic process have been widely explored. However, their effects in colorectal cancer progression are still confusing. Here, we screened 12 ALGs' expression through online datasets and found that was mostly upregulated in colorectal cancer tissues.

Subchronic Oral Toxicity of Sodium p-Hydroxybenzoate in Sprague-Dawley Rats.

p-Hydroxybenzoic acid (p-HBA), which exists extensively in plants, is well known for its anti-inflammatory effects, but various adverse side effects have also been reported. Previous research has found that acid translated to its sodium salt improves the safety profile of compounds. Therefore, we hypothesized that p-HBA translated to sodium p-hydroxybenzoate would improve its safety profile.

VSP‑17 suppresses the migration and invasion of triple‑negative breast cancer cells through inhibition of the EMT process via the PPARγ/AMPK signaling pathway.

VSP‑17, a novel peroxisome proliferator‑activated receptor γ (PPARγ) agonist, has been previously demonstrated to suppress the metastasis of triple‑negative breast cancer (TNBC) by upregulating the expression levels of E‑cadherin, which is a key marker of epithelial‑mesenchymal transition (EMT). However, the mechanism of action of VSP‑17, in particular whether it may be associated with the EMT process, remains unknown. The present study investigated the ability of VSP‑17 to inhibit the invasiveness and migratory ability of TNBC cell lines (MDA‑MB‑231 and MDA‑MB‑453) performed in in vitro experiments.

Species Quantification in Complex Herbal Formulas-Vector Control Quantitative Analysis as a New Method.

Product mislabeling and/or species fraud in Traditional Chinese Medicine (TCM) not only decrease TCM quality, but also pose a potential health issue to the end user. Up to now, methods to control TCM quality have been developed to detect specific metabolites or identify the original species. However, species quantification in complex herbal formulas is rarely concerned.

Palmatine-loaded electrospun poly(ε-caprolactone)/gelatin nanofibrous scaffolds accelerate wound healing and inhibit hypertrophic scar formation in a rabbit ear model.

Hypertrophic scar (HS) has been considered as a great concern for patients and a challenging problem for clinicians as it can cause functional debility, cosmetic disfigurement and psychological trauma. Although many methods have been developed to prevent and treat HS, the scarless healing is still a worldwide medical problem. In this study, palmatine-loaded poly(-caprolactone)/gelatin nanofibrous scaffolds (PCL/GE/PALs) were fabricated by electrospinning, and their effects on wound healing and HS formation were investigated.

Targeting SLC7A11 specifically suppresses the progression of colorectal cancer stem cells via inducing ferroptosis.

Recent studies have revealed the critical roles of ferroptosis in different physiological and pathological processes, however, its effects on the progression of colorectal cancer stem cells (CSCs) are still unclear. Here, we found that colorectal CSCs exhibited a remarkably lower level of reactive oxygen species (ROS), a higher level of cysteine, glutathione and SLC7A11 compared to colorectal cancer cells. Knockout of SLC7A11 increased the ROS level and reduced the levels of cysteine and glutathione, subsequently attenuating the viability of colorectal CSCs.

Hepatocyte nuclear factor-1β suppresses the stemness and migration of colorectal cancer cells through promoting miR-200b activity.

The effects of hepatocyte nuclear factors (HNFs) have been established in various tumors; however, the roles of HNF-1β in colorectal cancer progression are never been found. In the present study, HNF-1β expression was initially detected in clinical tissue samples and online datasets and HNF-1β was found to be highly expressed in colorectal cancer tissues. In addition, a positive correlation existed between HNF-1β expression and the overall survival of patients with colorectal cancer.

Natural product-derived icaritin exerts anti-glioblastoma effects by positively modulating estrogen receptor β.

Glioblastoma is the most common malignancy of the central nervous system, and patients typically have a poor prognosis. Previous studies indicate a gender bias in the development of glioblastoma; women are at a lower risk compared with men, suggesting that estrogen may confer protective effects. Icaritin, a prenylflavonoid derivative from a Chinese herb of the , selectively regulates the estrogen receptor (ER) and possesses anti-cancer properties.

Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.

Antibiotic resistance in bacteria has been an emerging public health problem, thus discovery of novel and effective antibiotics is urgent. A series of novel hybrids of N-aryl pyrrothine-base α-pyrone hybrids was designed, synthesized and evaluated as bacterial RNA polymerase (RNAP) inhibitors. Among them, compound 13c exhibited potent antibacterial activity against antibiotic-resistant S.

Paris saponin VII extracted from trillium tschonoskii suppresses proliferation and induces apoptosis of human colorectal cancer cells.

Ethnopharmacological Relevance: Saponins of many herbs could inhibit the growth of colorectal cancer cells. In the study, we investigated the effects of Paris saponin Ⅶ (PSⅦ), and elucidated its mechanism in colorectal carcinoma cells and a xenograft mouse model.

Materials And Methods: HT-29 and HCT-116 cells were treated with different concentrations of PSⅦ (0-100 μM).

GVS-12 attenuates non-alcoholic steatohepatitis by suppressing inflammatory responses PPARγ/STAT3 signaling pathways.

Non-alcoholic steatohepatitis (NASH), a type of fatty liver disease, is characterized by excessive inflammation and fat accumulation in the liver. Peroxisome proliferator-activated receptor γ (PPARγ) agonist rosiglitazone has great potential in protecting against the development of NASH. However, long-term usage of rosiglitazone probably leads to many adverse reactions.

Preparation, characterization and in vitro and in vivo evaluation of a solid dispersion of Naringin.

Naringin (NA) is one of typical flavanone glycosides widely distributed in nature and possesses several biological activities including antioxidant, anti-inflammatory, and antiapoptotic. The aim of this study was to develop solid dispersion (SD) and to improve the dissolution rate and oral bioavailability of NA. NA-SD was prepared by the traditional preparation methods using PEG6000, F68, or PVP K30 as carrier at different drug to carrier ratios.

VSP-17, a New PPARγ Agonist, Suppresses the Metastasis of Triple-Negative Breast Cancer via Upregulating the Expression of E-Cadherin.

Triple-negative breast cancer (TNBC), an aggressive subtype of breast cancer, shows higher metastases and relapse rates than other subtypes. The metastasis of TNBC is the main reason for the death of TNBC patients. Increasing evidence has shown that inhibiting the metastasis of TNBC is a good method for TNBC treatment.

Hepatoprotective effects of Dicliptera chinensis polysaccharides on dimethylnitrosamine-induced hepatic fibrosis rats and its underlying mechanism.

Ethnopharmacological Relevance: Dicliptera chinensis is a traditional herbal medicine used anciently in China for hepatopathy treatment, especially in south areas. Our several studies have demonstrated that dicliptera chinensis polysaccharides (DCP), which has a markedly protective effects on chemistry-induced models of acute liver injury in rats. In this study, we further investigated the potentially hepatoprotective effect of dicliptera chinensis polysaccharides (DCP) on hepatic fibrosis (HF) rats induced by dimethylnitrosamine (DMN).