A5051310534- Drug Transport and Resistance Mechanisms
- Phenothiazines and Benzothiazines Synthesis and Activities
- Lipid Membrane Structure and Behavior
- Cancer therapeutics and mechanisms
- Natural product bioactivities and synthesis
- Sphingolipid Metabolism and Signaling
- Bioactive Compounds and Antitumor Agents
- Antibiotics Pharmacokinetics and Efficacy
- Synthesis and biological activity
- DNA and Nucleic Acid Chemistry
- Polysaccharides and Plant Cell Walls
- Hops Chemistry and Applications
- Quinazolinone synthesis and applications
- Synthesis and Characterization of Heterocyclic Compounds
- Metal complexes synthesis and properties
- Traditional and Medicinal Uses of Annonaceae
- Inflammatory mediators and NSAID effects
- Computational Drug Discovery Methods
- Synthesis and bioactivity of alkaloids
- Fungal Plant Pathogen Control
- Bioactive Natural Diterpenoids Research
- Surfactants and Colloidal Systems
- Essential Oils and Antimicrobial Activity
- Biological Activity of Diterpenoids and Biflavonoids
- Phytochemicals and Antioxidant Activities
Wroclaw Medical University
2015-2025
National Institute of Standards and Technology
2023
Université de Lorraine
2023
Meiji Pharmaceutical University
2003
University of Wrocław
2001
Model systems such as black lipid membranes or conventional uni- multilamellar liposomes are commonly used to study membrane properties and structure. However, the construction dimensions of these models excluded their direct optical microscopic observation. Since introduction simple method liposome electroformation in alternating electric field giant unilamellar vesicles (GUVs) have become an important model imitating biological membranes. Due average diameter GUVs reaching up 100 microm,...
In this research, a series of novel hydrazone derivatives based on pyrazolopyridothiazinylacetohydrazide were designed, synthesized, and evaluated for their in vitro cytotoxic potency several human colon cancer cells (HTC116, HT‐29, LoVo). After MTT SRB assays four the most active derivatives: hydrazide GH hydrazones GH7, GH8, GH11, chosen further investigation. Hydrazone GH11 had highest activity (IC50 values c.a. 0.5 μM). Additionally, impact oxidative stress level, apoptosis induction,...
Multidrug resistance (MDR) of cancer cells constitutes one the main reasons for chemotherapy failure. The search nontoxic modulators that reduce MDR is a task great importance. An ability to enhance apoptosis resistant would also be beneficial. In present study, reversal and apoptosis-inducing potency three flavonoids produced by Citrus plants, namely, naringenin (1a), aromadendrin (2), tangeretin (3), methylated derivatives (1b, 1c), have been studied in sensitive (LoVo) multidrug-resistant...
Multidrug resistance (MDR) of cancer cells poses a serious obstacle to successful chemotherapy. The overexpression multispecific ATP-binding cassette transporters appears be the main mechanism MDR. A search for MDR-reversing agents able sensitize resistant chemotherapy is ongoing in hope their possible clinical use. Studies MDR modulators, although they have not produced clinically beneficial effects yet, may greatly enrich our knowledge about transporters, specificity and action, especially...
The resistance of cancer cells to a variety structurally non-related cytotoxic drugs is known as multidrug phenomenon (MDR). In cellular membranes an activity MDR transporters such P-glycoprotein (ABCB1) affected by their lipid environment. Many various compounds have been examined for ability restore drug-sensitivity resistant cells. Statins, inhibitors the key enzyme mevalonate pathway HMG-CoA (3-hydroxy-3-methyl-glutaryl-coenzyme A) reductase are commonly prescribed in order reduce serum...
Colorectal cancer (CRC) is the second cause of death worldwide. The composition and enzymatic activity colonic microbiota can significantly affect effectiveness CRC chemotherapy. Irinotecan a drug widely used to treat colon cancer. However, transformation drug-glucuronide (SN-38G) back its active form (SN-38) by bacterial β-glucuronidase (GUS) constitutes primary reason for observed intestinal toxicity irinotecan. It was demonstrated that novel enzymatically extracted apple pectin (PC) might...
Chalcones, potential anticancer agents, have shown promise in the suppression of multidrug resistance due to inhibition drug efflux driven by certain adenosine triphosphate (ATP)-binding cassette (ABC) transporters. The gene and protein expression chosen ABC transporters (multidrug 1, ABCB1; resistance-associated ABCC1; breast cancer protein, ABCG2) human colorectal cells (COLO 205 COLO 320, which overexpress active ABCB1) was mainly studied this work under influence a novel synthetic...
Since none of the multidrug resistance (MDR) modulators tested so far found their way into clinic, a novel approach to overcome MDR cancer cells has been proposed. The combined use two dissimilar mechanisms action was suggested benefit from synergy between them. effect three phenothiazine derivatives that were used as single agents and in combination with simvastatin on cell growth, apoptosis induction, activity, expression cyclooxygenase-2 (COX-2) doxorubicin-resistant colon (LoVo/Dx)...
Incidence of cancer is still increasing. Chemotherapy often unsuccessful; moreover, anticancer drugs cause serious side-effects. It necessary to develop effective agents for combination therapies that would increase antitumor effects treatment and reduce its side-effects.Anticancer activity oxicam derivatives (PR17 PR18) alone in with simvastatin on doxorubicin-resistant colon cells was studied. Apoptosis investigated via caspase-3 activation assay as well western blot analysis expression...
Abstract The expression of transmembrane transporter multidrug resistance-associated protein 1 (MRP1) confers the multidrug-resistant phenotype (MDR) on cancer cells. Since activity other MDR transporter, P-glycoprotein, is sensitive to membrane perturbation, we aimed check whether changes in lipid bilayer properties induced by flavones (apigenin, acacetin) and flavonols (morin, myricetin) were related their MRP1 inhibitory activity. All flavonoids inhibited efflux fluorescent substrate from...