A5023870102- Invertebrate Immune Response Mechanisms
- Peptidase Inhibition and Analysis
- Insect symbiosis and bacterial influences
- Insect Resistance and Genetics
- Phytochemical compounds biological activities
- Insect Pest Control Strategies
- Multiple Myeloma Research and Treatments
- Protease and Inhibitor Mechanisms
- Natural product bioactivities and synthesis
- Entomopathogenic Microorganisms in Pest Control
- Bone Metabolism and Diseases
- Aquaculture disease management and microbiota
- Histone Deacetylase Inhibitors Research
- Hops Chemistry and Applications
- PI3K/AKT/mTOR signaling in cancer
- Cancer, Hypoxia, and Metabolism
- Antimicrobial Peptides and Activities
- Fungal Biology and Applications
- Microbial Natural Products and Biosynthesis
- Ubiquitin and proteasome pathways
- Neurobiology and Insect Physiology Research
- Computational Drug Discovery Methods
- Plant chemical constituents analysis
- Liver Disease Diagnosis and Treatment
- Protein Degradation and Inhibitors
Maria Curie-Skłodowska University
2014-2025
Marie Curie
2008
Butein has been reported to prevent and partly reverse liver fibrosis in vivo; however, the mechanisms of its action are poorly understood. We, therefore, aimed determine antifibrotic potential butein.We assessed influence incubation hepatic stellate cells (HSCs) hepatoma (HepG2) with butein on sensitivity ethanol- or acetaldehyde-induced toxicity; production reactive oxygen species (ROS); expression markers HSC activation, including smooth muscle α-actin (α-SMA) procollagen I; transforming...
A new exopolysaccharide preparation isolated from stationary cultures of the white rot fungus Ganoderma applanatum (GpEPS) was tested in terms its bioactive properties including cytotoxic and immunostimulatory effect. The results indicate that GpEPS (at concentrations above 22.85 µg/mL 228.5 µg/mL) may exhibit selective activity against tumor cells (cell lines SiHa) stimulate production TNF-α THP-1-derived macrophages at level 752.17 pg/mL. showed antibacterial Staphyloccoccus aureus a toxic...
Although betulin (BET), a naturally occurring pentacyclic triterpene, has variety of biological activities, its osteogenic potential not been investigated so far. The aim this study was to assess the effect BET on differentiation human osteoblasts (hFOB 1.19 and Saos-2 cells) in vitro (with ascorbic acid as an supplement) osteoinductive (without additional conditions. Osteoblast evaluated based mRNA expression (RT-qPCR) Runt-related transcription factor 2 (RUNX2), alkaline phosphatase (ALP),...
A new series of hybrid compounds with tropinone and thiazole rings in the structure was designed synthesized as potential anticancer agents. They were tested against human multiple myeloma (RPMI 8226), lung carcinoma (A549), breast adenocarcinoma (MDA-MB-231), mouse skin melanoma (B16-F10) cell lines. Toxicity on normal fibroblasts (HSF) colon (CCD-18Co). The growth inhibition mechanism most active derivative analyzed through investigation its effect distribution cycle phases ability to...
Xanthohumol (XN), the main prenylated flavonoid from hop cones, has been recently reported to exert significant proapoptotic, anti-proliferative, and growth inhibitory effects against lung cancer in both vitro vivo studies. However, its anti-metastatic potential towards this malignancy is still unrevealed. Previously, we indicated that human adenocarcinoma A549 cell line was sensitive XN treatment. Therefore, using same tumour model, have studied influence of on...
This work presents a rational synthesis of 14 innovative methyl salicylate based thiazole (MSBT) derivatives, designed as protein tyrosine phosphatase 1B (PTP1B) inhibitors with potent anticancer activity. Enzyme inhibition studies were performed for all compounds. In addition, molecular docking simulations and assessment antiproliferative activity the most active lot. For studies, cell lines breast cancer (T47D) non-small-cell lung carcinoma (A549), well healthy control human skin...
Cyclic sulfones play an important role in the field of drug discovery and design due to their valuable properties broad range applications. Herein, we report efficient cerium(IV)-catalyzed allylic oxidation a simple 3-sulfolene. This process provides straightforward facile approach sulfol-2-en-4-one, versatile synthetic intermediate. Notably, this study represents first instance cerium catalysis employed oxidation. Furthermore, demonstrated transformation sulfol-2-en-4-one into 4-substituted...
The influence of infection with an entomopathogenic strain Pseudomonas aeruginosa on Galleria mellonella hemocytes was investigated. Extensive bacteriaemia developed 18 h after infection. This correlated significant changes in morphology, viability and the spreading ability immunocompetent hemocytes, namely granulocytes plasmatocytes. Since developed, membrane blebbing, cytoplasm vacuolization, cell organelle swelling, chromatin condensation were observed among others. These features are...
Osteosarcoma (OS) is the most common type of primary bone tumor. Currently, there are limited treatment options for metastatic OS. Alpha-ketoglutarate (AKG), i.e., a multifunctional intermediate Krebs cycle, one central metabolic regulators tumor fate and plays an important role in cancerogenesis progression. There growing evidence suggesting that AKG may represent novel adjuvant therapeutic opportunity anti-cancer therapy. The present study was intended to check whether supplementation...
Susceptibility of proteins and peptides present in immune hemolymph Galleria mellonella Fabricius (Lepidoptera: Pyralidae) larvae to proteolytic degradation by purified elastase B Pseudomonas aeruginosa was studied. Results showed that apoLp-III protein gradually digested vitro . Additionally, polipeptides with molecular mass 6.5 4 kDa were degraded after treatment the studied enzyme. The lack these decrease anti– Escherichia coli activity could indicate inducible antimicrobial B. On...
Ammi majus L. (Apiaceae) is a medicinal plant with well-documented history in phytotherapy. The aim of the present work was to isolate isopimpinellin (5,8-methoxypsoralen; IsoP) from fruit this and evaluate its biological activity against selected tumor cell lines. methanol extract obtained use an accelerated solvent extraction (ASE) method most suitable for quantitative analysis coumarins A. matrix. coumarin content estimated by RP-HPLC/DAD, amount IsoP found be 404.14 mg/100 g dry wt.,...
The presented studies were aimed at exploring the role of neutral endopeptidase (NEP) in function colon cancer cell lines LS 180 and SW 620, derived from different grades stages tumor development. NEP silencing by siRNA resulted decreased viability proliferation accompanied increased apoptosis both lines. Additionally, cycle arrest G2/M phase was observed, but only cells. Opposite to these results, serum-stimulated migration Furthermore, influenced invasive activity 620 cells an opposite...
A series of 3,3-diethylazetidine-2,4-dione based thiazoles 3a-3j were designed and synthesized as new human neutrophil elastase (HNE) inhibitors in nanomolar range. The representative compounds 3c, 3e, 3h exhibit high HNE inhibitory activity with IC50 values 35.02-44.59 nM, mixed mechanism action. Additionally, the most active 3c 3e demonstrate stability under physiological conditions. molecular docking study showed good correlation binding energies values, suggesting that inhibition...
Many organophosphorus compounds (OPs), especially various α-aminophosphonates, exhibit anti-cancer activities. They act, among others, as inhibitors of the proteases implicated in cancerogenesis. Thesetypes weredescribed, e.g., for neutral endopeptidase (NEP) expressed different cancer cells, including osteosarcoma (OS). The aim present study isto evaluate new borane-protected derivatives phosphonous acid (compounds 1–7) terms their drug-likeness properties, anti-osteosarcoma activities...
Here, we rationally designed a human neutrophil elastase (HNE) inhibitors 4a-4f derived from thalidomide. The HNE inhibition assay showed that synthesized compounds 4a, 4b, 4e and 4f demonstrated strong inhibiton properties with IC50 values of 21.78-42.30 nM. Compounds 4c, 4d competitive mode action. most potent compound shows almost the same as sivelestat. molecular docking analysis revealed strongest interactions occur between azetidine-2,4-dione group following three aminoacids: Ser195,...