Synthesis and effect of 4-acetylphenylamine-based imidazole derivatives on migration and growth of 3D cultures of breast, prostate and brain cancer cells.

In this study, we have synthesized novel 4-acetophenone moiety-bearing functionalized imidazole derivatives containing S-, and N-ethyl substituents and evaluated their anticancer activity. Their anticancer activity was studied against human breast carcinoma (MDA-MB-231), human prostate carcinoma (PPC-1), and human glioblastoma (U-87). Compounds 4, 9, 14, and 22 were identified as the most promising anticancer agents from a series of imidazole derivatives.

Regenerated nanofibrous cellulose electrospun from ionic liquid: Tuning properties toward tissue engineering.

Regenerated fibrous cellulose possesses a unique set of properties, including biocompatibility, biodegradability, and high surface area potential, but its applications in the biomedical sector have not been sufficiently explored. In this study, nanofibrous cellulose matrices were fabricated via a wet-electrospinning process using a binary system of the solvent ionic liquid (IL) 1-butyl-3-methylimidazolium acetate (BMIMAc) and co-solvent dimethyl sulfoxide (DMSO). The morphology of the matrices was controlled by varying the ratio of BMIMAc versus DMSO in the solvent system.

The Complex Regulation of Cytokinesis upon Abscission Checkpoint Activation.

Cytokinetic abscission is a crucial process that guides the separation of daughter cells at the end of each cell division. This process involves the cleavage of the intercellular bridge, which connects the newly formed daughter cells. Over the years, researchers have identified several cellular contributors and intracellular processes that influence the spatial and temporal distribution of the cytoskeleton during cytokinetic abscission.

Exploring doxorubicin transport in 2D and 3D models of MDA-MB-231 sublines: impact of hypoxia and cellular heterogeneity on doxorubicin accumulation in cells.

Triple-negative breast cancer (TNBC) treatment is challenging due to its aggressive nature and heterogeneity of this type of cancer, characterized by various subtypes and intratumoral diversity. Doxorubicin (DOX) plays a crucial role in TNBC chemotherapy reducing the tumor size and improving patient survival. However, decreased drug uptake and increased resistance in specific cell subpopulations reduce the effectiveness of the treatment.

Comparative In Vitro Study: Assessing Phytochemical, Antioxidant, Antimicrobial, and Anticancer Properties of Aiton and L. Fruit Extracts.

The phytochemical diversity and potential health benefits of and fruits call for further scientific inquiry. Our study aimed to determine the phytochemical composition of extracts from these fruits and assess their antioxidant, antibacterial, and anticancer properties in vitro. It was found that the ethanolic extracts of and fruits, which contained more lipophilic compounds, had 2-14 times lower antioxidant activity compared to the dry aqueous extracts of cranberry fruit, which contained more hydrophilic compounds.

The Effect of 4-(Dimethylamino)phenyl-5-oxopyrrolidines on Breast and Pancreatic Cancer Cell Colony Formation, Migration, and Growth of Tumor Spheroids.

A series of hydrazones, azoles, and azines bearing a 4-dimethylaminophenyl-5-oxopyrrolidine scaffold was synthesized. Their cytotoxic effect against human pancreatic carcinoma Panc-1 and triple-negative breast cancer MDA-MB-231 cell lines was established by MTT assay. Pyrrolidinone derivatives and , with incorporated 5-chloro and 5-methylbenzimidazole fragments; hydrazone bearing a 5-nitrothien-2-yl substitution; and hydrazone with a naphth-1-yl fragment in the structure significantly decreased the viability of both cancer cell lines.

Synthesis and In Vitro Evaluation as Potential Anticancer and Antioxidant Agents of Diphenylamine-Pyrrolidin-2-one-Hydrazone Derivatives.

The title compounds were synthesized by the reaction of 5-oxo-1-(4-(phenylamino)phenyl)pyrrolidine-3-carbohydrazide with various aldehydes bearing aromatic and heterocyclic moieties and acetophenones, and their cytotoxicity was tested via MTT assay against human triple-negative breast cancer MDA-MB-231, human melanoma IGR39, human pancreatic carcinoma Panc-1, and prostate cancer cell line PPC-1. Furthermore, the selectivity of compounds towards cancer cells compared to fibroblasts was also investigated. Four compounds were identified as the most promising anticancer agents out of a series of pyrrolidinone-hydrazone derivatives bearing a diphenylamine moiety.

Intrinsic Solubility of Ionizable Compounds from p Shift.

Aqueous solubility of pharmaceutical substances plays an important role in small molecule drug discovery and development, with ionizable groups often employed to enhance solubility. Drug candidate compounds often contain ionizable groups to increase their solubility. Recognizing that the electrostatically charged form of the compound is much more soluble than the uncharged form, this work proposes a model to explore the relationship between the p shift of the ionizable group and dissolution equilibria.

Interaction of phenotypic sublines isolated from triple-negative breast cancer cell line MDA-MB-231 modulates their sensitivity to paclitaxel and doxorubicin in 2D and 3D assays.

Breast cancer is a rapidly evolving, multifactorial disease that accumulates numerous genetic and epigenetic alterations. These result in molecular and phenotypic heterogeneity within the tumor, the complexity of which is further amplified through specific interactions between cancer cells. We aimed to analyze cell phenotypic sublines and the influence of their interaction on drug resistance, spheroid formation, and migration.

Assessing Adipocyte Viability and Surgeons' Work Efficiency by Comparing Different Liposuction Methods.

Background: Autologous fat grafting is widely used in plastic and reconstructive surgery. Liposuction methods play a key role in surgeons' work efficiency, adipocyte viability, graft survival, and outcomes. We investigated the effect of four liposuction methods on adipocyte viability, debris, and surgeons' work efficiency by measuring the active energy expenditure and changes in heart rate.

Effect of sunitinib derivatives on glioblastoma single-cell migration and 3D cell cultures.

This study aimed to evaluate the anticancer activity of 16 new sunitinib derivatives in brain cancer cells (2D model) and spheroids (3D model). The effect on cell viability was determined by the MTT assay. Single-cell migration assay was performed to examine the effect of selected compounds on individual cell migration.

Anticancer Activity of Sunitinib Analogues in Human Pancreatic Cancer Cell Cultures under Normoxia and Hypoxia.

Pancreatic cancer remains one of the deadliest cancer types. It is usually characterized by high resistance to chemotherapy. However, cancer-targeted drugs, such as sunitinib, recently have shown beneficial effects in pancreatic in vitro and in vivo models.

Nanocarriers overcoming biological barriers induced by multidrug resistance of chemotherapeutics in 2D and 3D cancer models.

Multidrug resistance (MDR) is currently a big challenge in cancer therapy and limits its success in several patients. Tumors use the MDR mechanisms to colonize the host and reduce the efficacy of chemotherapeutics that are injected as single agents or combinations. MDR mechanisms are responsible for inactivation of drugs and formbiological barriers in cancer like the drug efflux pumps, aberrant extracellular matrix, hypoxic areas, altered cell death mechanisms, etc.

Synthesis of novel sulphamethoxazole derivatives and exploration of their anticancer and antimicrobial properties.

A series of new derivatives based on sulfamethoxazole were designed and synthesized in this study. The structures of the new compounds were confirmed based on a comprehensive characterization of spectral data by applied IR and 1H as well as 13C NMR spectroscopy. The prepared compounds were tested for their anticancer and antimicrobial properties.

Fractionation and Characterization of Triterpenoids from L. Cuticular Waxes and Their Potential as Anticancer Agents.

Fruit and leaf cuticular waxes are valuable source materials for the isolation of triterpenoids that can be applied as natural antioxidants and anticancer agents. The present study aimed at the semi-preparative fractionation of triterpenoids from cuticular wax extracts of L. (lingonberry) leaves and fruits and the evaluation of their cytotoxic potential.

The Chemo-Sensitizing Effect of Doxorubicin of Apple Extract-Enriched Triterpenic Complex on Human Colon Adenocarcinoma and Human Glioblastoma Cell Lines.

Cancer cells' resistance to anticancer drugs represents a major clinical problem and the most important failure of treatment. Combination chemotherapy is more effective than monotherapy due to additive or synergistic effects. The aim of our research was to assess the effects of the combinations of apple extract's triterpenic compounds, individual triterpenic acids, and doxorubicin (DOX) on human colon adenocarcinoma (HT-29) and human glioblastoma (U-87) cell lines in 2D and 3D cultures.

Proanthocyanidins from L. Leaves: Perspectives in Wound Healing and Designing for Topical Delivery.

The compositions and health-beneficial properties of lingonberry leaves ( L.) are well established; however, their proanthocyanidins are still heavily underutilized. Optimizing their delivery systems is key to enabling their wider applications.

The Effect of 1,2,4-Triazole-3-thiol Derivatives Bearing Hydrazone Moiety on Cancer Cell Migration and Growth of Melanoma, Breast, and Pancreatic Cancer Spheroids.

4-Phenyl-3-[2-(phenylamino)ethyl]-1-1,2,4-triazole-5(4)-thione was used as a starting compound for the synthesis of the corresponding 1,2,4-triazol-3-ylthioacetohydrazide, which reacts with isatins and various aldehydes bearing aromatic and heterocyclic moieties provided target hydrazones. Their cytotoxicity was tested by the MTT assay against human melanoma IGR39, human triple-negative breast cancer (MDA-MB-231), and pancreatic carcinoma (Panc-1) cell lines. The selectivity of compounds towards cancer cells was also studied.

Effect of natural flavonoids to reverse P-glycoprotein-related multidrug resistance in breast cancer cell cultures.

The aim of the research was to evaluate the influence of two P-glycoprotein (P-gp) inhibitors silymarin and quercetin on anticancer drug doxorubicin (DOX) and pegylated liposomal doxorubicin (PLD) delivery into breast cancer cells (2D cultures) and cancer cell spheroids (3D cultures) at different pH. The cytotoxicity of the compounds was assessed using MTT assay. Spheroids were generated using magnetic 3D Bioprinting method.

Reduction of gastrointestinal tract colonization by Klebsiella quasipneumoniae using antimicrobial protein KvarIa.

Background: Klebsiella quasipneumoniae is an opportunistic pathogen causing antibiotic-resistant infections of the gastrointestinal tract in many clinical cases. Orally delivered bioactive Klebsiella-specific antimicrobial proteins, klebicins, could be a promising method to eradicate Klebsiella species infecting the gut.

Methods: Mouse infection model was established based on infection of antibiotic-treated BALB/C mice with K.

The Effect of Beta Adrenoreceptor Blockers on Viability and Cell Colony Formation of Non-Small Cell Lung Cancer Cell Lines A549 and H1299.

Beta adrenoblockers are a large class of drugs used to treat cardiovascular diseases, migraines, glaucoma and hyperthyroidism. Over the last couple of decades, the anticancer effects of these compounds have been extensively studied. However, the exact mechanism is still not known, and more detailed studies are required.

Exploring Vaccinium vitis-idaea L. as a potential source of therapeutic agents: antimicrobial, antioxidant, and anti-inflammatory activities of extracts and fractions.

Ethnopharmacological Relevance: Vaccinium vitis-idaea L. (lingonberry) leaves and fruits have traditionally been used in Asian and European countries as a natural solution for urinary tract infections, gastrointestinal distress, neurodegenerative diseases, and related inflammatory disorders, which are overall associated with free radical damage and presence of triggering pathogenic strains in the human body. Considering growing attention to natural products, there are not enough scientific data to confirm predominant specialized metabolites, responsible for the traditional therapeutic use of lingonberries.

Pharmacological Potential and Chemical Composition of Leaf Extracts.

L. (saffron) has been traditionally used as a food coloring or flavoring agent, but recent research has shown its potent pharmacological activity to tackle several health-related conditions. sp.

3D Cell Culture Models as Recapitulators of the Tumor Microenvironment for the Screening of Anti-Cancer Drugs.

Today, innovative three-dimensional (3D) cell culture models have been proposed as viable and biomimetic alternatives for initial drug screening, allowing the improvement of the efficiency of drug development. These models are gaining popularity, given their ability to reproduce key aspects of the tumor microenvironment, concerning the 3D tumor architecture as well as the interactions of tumor cells with the extracellular matrix and surrounding non-tumor cells. The development of accurate 3D models may become beneficial to decrease the use of laboratory animals in scientific research, in accordance with the European Union's regulation on the 3R rule (Replacement, Reduction, Refinement).

Homing Peptide-Based Targeting of Tenascin-C and Fibronectin in Endometriosis.

The current diagnostic and therapeutic strategies for endometriosis are limited. Although endometriosis is a benign condition, some of its traits, such as increased cell invasion, migration, tissue inflammation, and angiogenesis are similar to cancer. Here we explored the application of homing peptides for precision delivery of diagnostic and therapeutic compounds to endometriotic lesions.