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Search results for: anticancer%20drug
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The role of glucuronidation in drug resistance
PublicationThe final therapeutic effect of a drug candidate, which is directed to a specific molecular target strongly depends on its absorption, distribution, metabolism and excretion (ADME). The disruption of at least one element of ADME may result in serious drug resistance. In this work we described the role of one element of this resistance: phase II metabolism with UDP-glucuronosyltransferases (UGTs). UGT function is the transformation...
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In vitro enzyme kinetics and NMR-based product elucidation for glutathione S-conjugation of the anticancer unsymmetrical bisacridine C-2028 in liver microsomes and cytosol: major role of glutathione S-transferase M1-1 isoenzyme
PublicationThis work is the next step in studying the interplay between C-2028 (anticancer-active unsymmetrical bisacridine developed in our group) and the glutathione S-transferase/glutathione (GST/GSH) system. Here, we analyzed the concentration- and pH-dependent GSH conjugation of C-2028 in rat liver microsomes and cytosol. We also applied three recombinant human GST isoenzymes, which altered expression was found in various tumors. The...
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Cancer stem cells and escape from drug-induced premature senescence in human lung tumor cells: implications for drug resistance and in vitro drug screening models
PublicationBadania z użyciem modelu komórek nowotworu płuc A549 wykazały, że komórki te po traktowaniu lekami uszkadzającymi DNA zatrzymują proliferację i wchodzą w stan starzenia komórkowego. Jednak post-inkubacja tych komórek prowadzi do powrotu do stanu proliferacji małej frakcji komórek. Wykazaliśy, że frakcja ta związana jest z obecnością komórek pierwotnych nowotworu w populacji komórek A549. Powrót do stanu proliferacji komóek A549...
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HPV16 E6 Gene Transcripts in Primary Type II Endometrial Carcinomas
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Antimicrobial molecular nanocarrier–drug conjugates
PublicationMany antimicrobial drugs are poorly active against pathogenic microbes causing intracellular infections, such as Mycobacterium tuberculosis or Plasmodium falciparum. On the other hand, several known antimicrobial agents are not effective enough because of their limited cellular penetration. A common feature of both challenges is the inability of an active agent to cross the biological membrane(s). One of the possible approaches...
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Pharmacokinetics and pharmacodynamics of propofol and fentanyl in patients undergoing abdominal aortic surgery - a study of pharmacodynamic drug-drug interactions
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Antipsychotic drug prescription sequence analysis in relation to death occurrence and cardiometabolic drug usage: A retrospective longitudinal study
PublicationThe potential role of antipsychotics in increasing cardiovascular risk of mortality is still debated. The aim of this study was to assess the death risk associated with sequences of first-generation antipsychotic (FGA) and second-generation antipsychotic (SGA) prescriptions, including clozapine and lithium, and drugs for cardiometabolic diseases. We conducted a retrospective longitudinal analysis involving 84,881 patients who received...
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Thin layer chromatography in drug discovery process
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Biopolymers and Their Composites for Drug Delivery: A Brief Review
PublicationIn recent years, excipient development has become a core area of research in pharmaceutical drug delivery because it influences the formulation development and drug delivery process in various ways. Polymeric drug delivery systems have been of great interest for controlled delivery as they show the great advantage in drug delivery systems because of optimized drug loading and releasing property. Then, the side effects of synthetic...
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Customizing nano-chitosan for sustainable drug delivery
PublicationChitosan is a natural polymer with acceptable biocompatibility, biodegradability, and mechanical stability; hence, it has been widely appraised for drug and gene delivery applications. However, there has been no comprehensive assessment to tailor-make chitosan cross-linkers of various types and functionalities as well as complex chitosan-based semi- and full-interpenetrating networks for drug delivery systems (DDSs). Herein, various...
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Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery
PublicationAbstract: Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development. After a century since the 1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists’ attention, leading to the discovery of a few presently...
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Using anticipatory and drug-evoked appetitive ultrasonic vocalization for monitoring the rewarding effect of amphetamine in a rat model of drug self-administration
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The Significance of MicroRNAs Expression in Regulation of Extracellular Matrix and Other Drug Resistant Genes in Drug Resistant Ovarian Cancer Cell Lines
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Function and Frustration of Multi-Drug ABC Exporter Protein and Design of Model Proteins for Drug Delivery Using Protein Hydration Thermodynamics
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Thermodynamics aspects of interactions between acridine derivatives and DNA
PublicationDNA is a molecular target for many anticancer and antiviral drugs. Therefore, a clear understanding of the interaction of small molecules with DNA is important in the rational design of ligands that can bind to DNA with high affinity and selectivity. There are several methods to investigate interactions between drug and DNA. Some of them measure changing into DNA structures, such as lengthening and untwisting of helix of DNA. Other...
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Naturally-derived hydrogels for 3D pancreatic tumor models: A short review
PublicationStatistics suggest a high proportion of mortality rate by pancreatic cancer, which is a solid tumor characterized by high heterogeneity and the presence of a complex extracellular matrix. The very low effectiveness of pancreatic cancer treatment roots in the high metastatic potential and drug resistance of this tumor. Therefore, the quest for efficient cellular models enabling precise mimicking in vivo conditions, and anticancer...
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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublicationBackground The compound 9-(2′-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes – UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. Methods UGT-mediated...
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Feasibility study of a Raman spectroscopic route to drug detection
PublicationWe present an surface-enhanced Raman spectroscopy (SERS) approach for detection of drugs of abuse in whole human blood. We utilize a near infrared laser with 830 nm excitation wavelength in order to reduce the influence of fluorescence on the spectra of blood. However, regular plasmon resonance peak of plasmonic nanoparticles, such as silver or gold fall in a much lower wavelength regime about 400 nm. Therefore, we have shifted...
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Biopolymer based nanomaterials in drug delivery systems: A review
PublicationDrug delivery systems (DDS) are used to achieve a higher therapeutic effects of a pharmaceutical drug or natural compound in a specific diseased site with minimal toxicological effect and these systems consists of liposomes, microspheres, gels, prodrugs and many. Nanotechnology is a rapidly developing multi-disciplinary science that ensures the fabrication of the polymers to nanometer scale for various medical applications. Uses...
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Targeting DNA Topoisomerase II in Antifungal Chemotherapy.
PublicationTopoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand...
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Cancer stem cells in drug resistance and drug screening: can we exploit the cancer stem cell paradigm in search for new antitumor agents?
PublicationPraca przedstawia przegląd literatury dotyczącej hipotezy komórek pierwotnych nowotworu, w szczególności w ich oporności na istniejące terapie. Dyskutowane jest także zagadnienie możliwości wykorzystania wiedzy o tych komórkach do konstrukcji nowych testów do badań przesiewowych in vitro w celu poszukiwania nowych leków przeciwnowotworowych.
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Filling of Carbon Nanotubes: Containers for Magnetic Probes and Drug Delivery
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The Role of miRNA-7 in the Biology of Cancer and Modulation of Drug Resistance
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Recent Advances in Polymer-Based Vaginal Drug Delivery Systems
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Chitosan-Based Nanoparticles as Effective Drug Delivery Systems—A review
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Mesoporous silica nanoflakes – Biocompatibility, cellular uptake and drug transport
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Controlled Drug Release by the Pore Structure in Polydimethylsiloxane Transdermal Patches
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Synthetic strategies in construction of organic macromolecular carrier–drug conjugates
PublicationMany metabolic inhibitors, considered potential antimicrobial or anticancer drug candidates, exhibit verylimited ability to cross the biological membranes of target cells. The restricted cellular penetration ofthose molecules is often due to their highhydrophilicity. One of the possible solutions to this problem is aconjugation of an inhibitor with a molecular organic nanocarrier. The conjugate thus formed should beable to penetrate...
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Pharmaceutical and forensic drug applications of chiral supercritical fluid chromatography
PublicationTHE SUPERCRITICAL FLUID IS AN EXCELLENT CHOICE AS THE CHROMATOGRAPHIC MOBILE PHASE BECAUSE IT ALLOWS RAPID SEPARATION WITH HIGH EFFICIENCY AND APPLICATIONS INVOLVING ENANTIORESOLUTION ARE COMMON. SUPERCRITICAL FLUID CHROMATOGRAPHY (SFC) IS INCREASINGLY USED FOR ANALYTICAL, SEMI-PREPARATIVE AND PREPARATIVE PURIFICATION OF CHIRAL COMPOUNDS, INCLUDING PRODUCTION OF ENANTIOMERS THAT ARE MAINLY ENCOUNTERED DURING DRUG DEVELOPMENT. SFC...
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Diatomaceous earth as a drug-loaded carrier in a glass-ionomer cement
PublicationThe effect of a natural filler (diatomaceous earth [DE], a promising drug-delivery agent) and its content was investigated on the performance of a model glass-ionomer cement (GIC). Three sample series, differing in DE content (0, 2.5 and 5 wt%), were prepared using a commercial GIC as a matrix (3M Ketac Molar Easymix). The resultant surface microhardness and roughness, wear performance, and compressive strength of the samples were...
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Effective Drug Concentration and Selectivity Depends on Fraction of Primitive Cells
PublicationPoor efficiency of chemotherapeutics in the eradication of Cancer Stem Cells (CSCs) has been driving the search for more active and specific compounds. In this work, we show how cell density-dependent stage culture profiles can be used in drug development workflows to achieve more robust drug activity (IC50 and EC50) results. Using flow cytometry and light microscopy, we characterized the cytological stage profiles of the HL-60-,...
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Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies
PublicationA series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9–20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5–8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II,...
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Graphene Production and Biomedical Applications: A Review
PublicationGraphene is a two-dimensional nanomaterial composed of carbon atoms with sp2 hybrid orbitals. Both graphene and graphene-based composite have gained broad interest among researchers because of their outstanding physiochemical, mechanical, and biological properties. Graphene production techniques are divided into top-down and bottom-up synthesis methods, of which chemical vapor deposition (CVD) is the most popular. The biomedical...
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Progress in targeting tumor cells by using drug-magnetic nanoparticles conjugate.
PublicationTo limit the cytotoxicity of anticancer drugs against healthy cells, an appropriate carrier should be synthesized to deliver the drug to the tumor tissue only. A good solution is to anchor a magnetic nanoparticle to the molecule of the drug and to use a properly directed external magnetic field. We have shown that the improved by us synthesis of the conjugate of doxorubicin with iron-oxide magnetic nanoparticles allows a substantial...
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Natural carbon-based quantum dots and their applications in drug delivery: A review
PublicationNatural carbon based quantum dots (NCDs) are an emerging class of nanomaterials in the carbon family. NCDs have gained immense acclamation among researchers because of their abundance, eco-friendly nature, aqueous solubility, the diverse functionality and biocompatibility when compared to other conventional carbon quantum dots (CDs).The presence of different functional groups on the surface of NCDs such as thiol, carboxyl, hydroxyl,...
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublicationHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition
PublicationHeterocyclic pharmacophores such as thiazole and quinoline rings have a significant role in medicinal chemistry. They are considered privileged structures since they constitute several Food and Drug Administration (FDA)-approved drugs for cancer treatment. Herein, we report the synthesis, in silico evaluation of the ADMET profiles, and in vitro investigation of the anticancer activity of a series of novel thiazolyl-hydrazones based...
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublicationAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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Magnetic Silica Nanotubes: Synthesis, Drug Release, and Feasibility for Magnetic Hyperthermia
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Multi‐wall carbon nanotubes – a vehicle for targeted Irinotecan drug delivery
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Antimicrobial peptides (AMPs) as drug candidates: a patent review (2003–2015)
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Disposition of Drugs of Abuse and Their Metabolites in Wastewater as a Method of the Estimation of Drug Consumption
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Natural carbon-based quantum dots and their applications in drug delivery: A review
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The significance of lumican expression in ovarian cancer drug-resistant cell lines
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pH-dependent composite coatings for controlled drug delivery system - Review
PublicationNowadays in case of long-term implants, the most common postoperative complications are bacterial infections, which in consequence may provoke loos- ening of the implants in the primary phase of stabilization. Bacterial infections are currently the most frequent cause of revision surgery of the implants such as hip joint endoprosthesis, knee joint endoprosthesis and dental implants. In order to provide the local and long-term antibacterial...
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The impact of lipophilicity on environmental processes, drug delivery and bioavailability of food components
PublicationLipophilic properties of the compound allow to predict its fate in living organisms and to propose the models of chemicals transport and accumulation in the ecosystem. Lipophilicity is also useful as the characteristic of chemicals in respect to their optimal attributes for specific biological and non-biological tasks. The lipophilicity descriptors define the potency of endo- and xenobiotics to metabolic transformations and their...
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Influence of Escherichia coli on Expression of Selected Human Drug Addiction Genes
PublicationThe impact of enteric microflora on the expression of genes associated with cocaine and amphetamine addiction was described. Human genome-wide experiments on RNA transcripts expressed in response to three selected Escherichia coli strains allowed for significant alteration (p > 0.05) of the linear regression model between HT-29 RNA transcripts associated with the KEGG pathway:hsa05030:Cocaine addiction after 3 h stimulation with...
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In silico design of telomerase inhibitors.
PublicationTelomerase is a reverse transcriptase enzyme involved in DNA synthesis at the end of linear chromosomes. Unlike in most other cells, telomerase is reactivated most cancerous cells and, therefore, has become a promising new anticancer target. Despite extensive research, direct telomerase inhibitors have yet not been introduced to the clinics because of the complexity of this enzyme. Structures of this protein from simple organisms...
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Therapeutic intervention by the simultaneous inhibition of DNA repair and type I or type II DNA topoisomerases: one strategy, many outcomes
PublicationMany anticancer drugs reduce the integrity of DNA, forming strand breaks. This can cause mutations and cancer or cell death if the lesions are not repaired. Interestingly, DNA repair-deficient cancer cells (e.g., those with BRCA1/2 mutations) have been shown to exhibit increased sensitivity to chemotherapy. Based on this observation, a new therapeutic approach termed 'synthetic lethality' has been developed, in which radiation...
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Resistance of human prostate carcinoma cells to a new antitumor compound capridine beta is associated with changed drug metabolism combined with both inherent and drug-induced overexpression of ABC transporters
PublicationW pracy charakteryzujemy mechanizm oporności na nową pochodną 1-nitroakrydyny, związku capridine beta (C-1748) o wysokiej aktywności przeciwnowotworowej, znajdującego się w badaniach klinicznych. Nasze dane wskazują, że oporność na ten związek jest wynikiem zmienionego metabolizmu inaktywującego C-1748 oraz wzrostem ekspresji pompy błonowej ABCG2 a także innych białek transportowych typu ABC.