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Search results for: UNSYMMETRICAL BISACRIDINE DERIVATIVES, AG-IN-ZN-S NANOCRYSTALS, LUNG AND COLON CANCER CELLS, DRUG-CARRIER DEGRADATION PATHWAY, CYTOTOXIC ACTIVITY, IN VIVO ANTITUMOR EFFICACY, PH-DEPENDENT RELEASE, CELLULAR UPTAKE
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Selected symmetrically substituted carbazoles: Investigation of anticancer activity and mechanisms of action at the cellular and molecular levels
PublicationDNA topoisomerases play a critical role as essential enzymes in controlling alterations in the topology of DNA. They achieve this by orchestrating the coordinated process of breaking and rejoining DNA strands, which is crucial for maintaining the proper structure of DNA during regular cellular development. The search for and development of new potential anticancer drugs is a challenging yet immensely important area of research...
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Antitumor potential of new low molecular weight antioxidative preparations from the white rot fungus Cerrena unicolor against human colon cancer cells
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IN VIVO DEGRADATION OF BIOMATERIALS
PublicationThe material designed to be introduced into the human tissue should be biocompatible and biofunctional. Unless it is so, the body may respond to the implant in different ways. An inflammation reaction may appear such as: parting of items of the implant surface resulting from fraction or pressure. The condition of the surface has an important influence on the usefulness of the implant. The required values depend on the implant function...
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Interleukin 12 and indomethacin exert a synergistic, angiogenesis-dependent antitumor activity in mice
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Synthesis and antitumor activity of conjugates of muramyldipeptide or normuramyldipeptide with hydroxyacridine/acridone derivatives
PublicationOpisano syntezę analogów MDP oraz nor-MDP modyfikowanych w części peptydowej pochodnymi hydroksyakrydyny/akrydonu i dwóch analogów modyfikowanych pochodnymi 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny. Tylko związki zawierające pochodne 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny wykazały wysoką aktywność cytotoksyczną badaną na 60 liniach ludzkich komórek nowotworowych, na nowotwór prostaty i AIDS-related lymphoma (ARL). Związek...
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Exploring the Reactivity of Unsymmetrical Diphosphanes toward Heterocumulenes: Access to Phosphanyl and Phosphoryl Derivatives of Amides, Imines, and Iminoamides
PublicationWe present a comprehensive study on the diphosphanation of iso(thio)cyanates by unsymmetrical diphosphanes. The reactions involving unsymmetrical diphosphanes and phenyl isocyanate or phenyl thioisocyanate gave rise to phosphanyl, phosphoryl, and thiophosphoryl derivatives of amides, imines, and iminoamides. The structures of the diphosphanation products were confirmed through NMR spectroscopy, IR spectroscopy, and single-crystal...
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Release of selected chemical elements from shale drill cuttings to aqueous solutions of different pH
PublicationThe effect of pH changes on leachability of light and heavy metals from shale drill cuttings generated from unconventional shale gas production was investigated. Cuttings, being the primary byproduct generated from drilling operations, belong to the potentially hazardous type of wastes due to presence of heavy and radioactive elements and remains of drilling fluid. In this regard, assessment of potentially dangerous components...
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Vimentin immunoexpression and its prognostic activity in colon cancer among Caucasian patients
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Aminopropyl-functionalized mesoporous silica SBA-15 as drug carrier for cefazolin: adsorption profiles, release studies, and mineralization potential
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Chemopreventive activity of bioactive fungal fractions isolated from milk-supplemented cultures of Cerrena unicolor and Pycnoporus sanguineus on colon cancer cells
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The influence of different expression of CYP3A4 izoenzymes on metabolic pathway derivatives in human hepatoma cells
PublicationCelem przeprowadzonych badań było określenie różnic w metabolizmie pochodnych C-857 i C-1748 w komórkach ludzkiego nowotworu wątroby HepG2 oraz określenie wpływu na ich biotransformację w podwyższonej ekspresji izoenzymu CYP3A4 w tejże linii. Uzyskane wyniki wskazały, że związek C-857, jak również C-1748 metabolizuje w komórkach HepG2 oraz Hep3A4 do wielu reaktywnych, niestabilnych metabolitów. Różnice w biotransformacji były bardzo...
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Myrosinase activity in different plant samples; optimisation of measurement conditions for spectrophotometric and pH-stat methods
PublicationMyrosinase found in Brassicaceae plants, is the enzyme responsible for hydrolysis of glucosinolates. As a result a variety of biologically active metabolites are liberated, whose importance in crop protection and especially in cancer chemoprevention is rapidly gaining recognition. The growing practical application of glucosinolate degradation products requires that sensitive and reliable methods of myrosinase activity determination...
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Cell Density-Dependent Cytological Stage Profile and Its Application for a Screen of Cytostatic Agents Active Toward Leukemic Stem Cells
PublicationProliferation and expansion of leukemia is driven by leukemic stem cells (LSCs). Multidrug resistance (MDR) of LSCs is one of the main reasons of failure and relapses in acute myeloid leukemia (AML) treatment. In this study, we show that maintaining HL-60 at low cell culture density or applying a 240-day treatment with anthrapyridazone (BS-121) increased the percentage of primitive cells, which include LSCs determining the overall...
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Influence of the electrosynthesis conditions on the spontaneous release of anti-inflammatory salicylate during degradation of polypyrrole coated iron for biodegradable cardiovascular stent
PublicationIn this work, the spontaneous release of anti-inflammatory salicylate from polypyrrole (PPy) coated iron has been studied during degradation of the material in phosphate buffer saline at 37 C. The sodium salicylate was incorporated into PPy in a one-step electropolymerization process. The influence of the synthesis conditions such as sodium salicylate concentration, pyrrole concentration and deposition charge on drug release profile...
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The Influence of the Co-Dopant Dexamethasone Phosphate on the Electrodeposition Process and Drug-Release Properties of Polypyrrole-Salicylate on Iron
PublicationIn this work, the influence of incorporation of two anti-inflammatory drugs dexamethasone phosphate and sodium salicylate on the electrodeposition process of polypyrrole (PPy) film on iron has been studied. The incorporation of the agents into PPy has been carried out in a one-step electropolymerization process on oxidizable iron. The role of each drug agent during the deposition process has been discussed. The morphological and...
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Ag modified ZnO microsphere synthesis for efficient sonophotocatalytic degradation of organic pollutants and CO2 conversion
PublicationThe synthesis and design of non-precious and efficient sonophotocatalyts by an environment friendly technique are requisites for solar energy conversion and environmental remediation. This work reports the preparation of Ag/ZnO microspheres with different Ag contents through deposition–precipitation method for pollutant degradation and CO2 conversion. Detail structural investigation reveals that ZnO microspheres and Ag-ZnO microspheres...
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Synthesis, crystal structure and cytotoxic activity of ruthenium(II) piano-stool complex with N,N-chelating ligand
PublicationA mononuclear compound of the general formula [(η6-p-cymene)RuIICl(2,2′-PyBIm)]PF6 has been synthesized from a bidentate N,N-donor ligand, viz. 2,-(2′-pyridyl)benzimidazole (2,2′-PyBIm) and the corresponding chloro-complex [(η6-p-cymene)Ru(μ-Cl)Cl]2 (precursor). The isolated coordination compound was characterized by IR, UV–vis and 1H, 13C NMR spectroscopies. The single crystal X-ray analysis of the complex reveals that the asymmetric...
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Novel chalcone-derived pyrazoles as potential therapeutic agents for the treatment of non-small cell lung cancer
PublicationLung cancer is considered to account for approximately one-fifth of all malignant tumor-related deaths worldwide and is therefore one of the most lethal malignancies. Pyrazole scaffold possesses a wide range of biological and pharmacological activities, which play important roles in medicinal chemistry. The present study reports the synthesis and in vitro biological characterization of nine pyrazoles derived from chalcones as potential...
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The Chemometric Evaluation of Antitumor Activity of Novel Benzensulfonamide Derivatives Based on their Physiochemical Properties
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Novel composite of Zn/Ti-layered double hydroxide coupled with MXene for the efficient photocatalytic degradation of pharmaceuticals
PublicationIn the present study, a hybrid photocatalyst of Zn/Ti layered double hydroxide (LDH) coupled with MXene – Ti3C2 was synthesized for the first time and applied in photocatalytic degradation of acetaminophen and ibuprofen, two commonly present in the natural environment and prone to accumulate in the aquatic ecosystem pharmaceuticals. The effect of MXene content (0.5 wt%, 2.5 wt%, and 5 wt%) on the photocatalytic activity of LDH/MXene...
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Design and Experimental Validation of a Metamaterial-Based Sensor for Microwave Imaging in Breast, Lung, and Brain Cancer Detection
PublicationThis study proposes an innovative geometry of a microstrip sensor for high-resolution microwave imaging (MWI). The main intended application of the sensor is early detection of breast, lung, and brain cancer. The proposed design consists of a microstrip patch antenna fed by a coplanar waveguide with a metamaterial layer-based lens implemented on the back side, and an artificial magnetic conductor (AMC) realized on as a separate...
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Derivatives of 1-nitroacridine induce apoptosis only in a limited number of human colon adenocarcinoma cells
PublicationPraca dotyczy indukcji apoptozy w komórkach ludzkich raków okrężnicy HT29 i HCT8 pod wpływem pochodnych 1-nitroakrydyny: C-857 i C-1748. Wykazano, że związki te w stężeniach biologicznie istotnych (EC90) indukują apoptozę tylko w części populacji komórek. Efekt ten uzależniony był od czasu inkubacji komórek ze związkiem, a nie zależał od stężenia związku.
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Evaluating the antibacterial activity of muramyl dipeptide derivatives, retro-tuftsin derivatives, and anthraquinone oligopeptides against a range of pathogenic bacteria
PublicationSearch for new and efficient antibiotic is crucial because of microbial drug resistance and problems with side effects of the administered medication. In this study, we evaluate the in vitro microbiological activity of muramyl dipeptide derivatives, retro-tuftsin derivatives (i.e., tuftsin with reversed amino acid sequences), and combinations of retro-tuftsin derivatives with substituted anthraquinones. The potency of the investigated...
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Lipid mediators involved in the oxidative stress and antioxidant defence of human lung cancer cells
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Potent antitumor 4-methyl-1-nitroacridine C-1748 induces apoptosis only in part of colon cells
PublicationCelem przedstawionej pracy było zbadanie zdolności pochodnej 1-nitroakrydyny C-1748 do indukcji apoptozy komórek raka jelita grubego HCT8 i HT29 pochodzenia ludzkiego. Śmierć komórek była badana przez określony czas inkubacji komórek ze związkiem w stężeniach odpowiadających wartościom EC90 lub ich wielokrotnościom przez czas od 3 do 72 godzin. Uzyskane wyniki wskazują, że C-1748 indukuje apoptozę zależną od czasu tylko w części...
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Potent antitumor 4-methyl-1-nitroacridine C-1748 induces apoptosis only in part of colon cells
PublicationZbadaliśmy zdolność pochodnej 4-metylo-1-nitroakrydyny C-1748 do indukcji apoptozy w ludzkich komórkach nowotworów jelita grubego HCT-8 i HT29 w stężeniach biologicznie istotnych. Zjawisko apoptozy określiliśmy na podstawie zmian morfologicznych jak i biochemicznych tj. fragmentacji DNA, aktywacji kaspazy-3, spadku potencjału mitochondrialnego, eksternalizacji fosfatydyloseryny i pojawiania się frakcji sub-G1. Wykazaliśmy, że pochodna...
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Highly effective degradation of selected groups of organic compounds by cavitation based AOPs under basic pH conditions
PublicationCavitation has become on the most often applied methods in a number of industrial technologies. In the case of oxidation of organic pollutants occurring in the aqueous medium, cavitation forms the basis of numerous advanced oxidation processes (AOPs). This paper presents the results of investigations on the efficiency of oxidation of the following groups of organic compounds: organosulfur, nitro derivatives of benzene, BTEX, and...
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Lung cancer survival and comorbidities in lung cancer screening participants of the Gdańsk screening cohort
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Meiothermus ruber cells as β-galactosidase activity biocatalyst
PublicationThe current study allowed to establish the possibility of using whole cells of thermophilic bacteria Meiothermus ruber as a biocatalyst with β-galactosidase activity. β-galactosidases are used for hydrolysis of lactose as well as for oligosaccharides synthesis. The advantages of using whole bacterial cells catalysis is not only elimination of tedious, expensive protein isolation and/or purification but also stabilization of enzymes...
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Adenylate kinase immobilized on graphene oxide impairs progression of human lung carcinoma epithelial cells through adenosinergic pathway
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Electroporation and lipid nanoparticles with cyanine IR-780 and flavonoids as efficient vectors to enhanced drug delivery in colon cancer
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Electrochemistry/mass spectrometry (EC/MS) for fast generation and identification of novel reactive metabolites of two unsymmetrical bisacridines with anticancer activity.
PublicationThe development of a new drug requires knowledge about its metabolic fate in a living organism, regarding the comprehensive assessment of both drug therapeutic activity and toxicity profiles. Electrochemistry (EC) coupled with mass spectrometry (MS) is an efficient tool for predicting the phase I metabolism of redox-sensitive drugs. In particular, EC/MS represents a clear advantage for the generation of reactive drug transformation...
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The effect of Ag, Au, Pt, and Pd on the surface properties, photocatalytic activity and toxicity of multicomponent TiO2-based nanomaterials
PublicationMulticomponent TiO2-based nanomaterials (MC-NMs) show better physicochemical properties than their individual components or bulk materials. However, the same unique properties that offer innovative applications might also pose unknown risks to human health and the environment. In this context, TiO2- based nanomaterials with a mixture of noble metal precursors (Ag, Au, Pt, and Pd) for large-scale technological applications in air...
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Successive cytotoxicity control by evolutionary surface decorated electronic push-pull green ZnCr-LDH nanostructures: Drug delivery enlargement for targeted breast cancer chemotherapy
PublicationThe reason for the increasing bioavailability and biocompatibility of the porous nanomaterials in the presence of different (bio)molecules is still unknown. The role of difference functional groups and their interactions with the potential bioavailability and biocompatibility is of great importance. To investigate the potential contribution of the electronic effects (especially on the surface of the porous nanomaterials) on their...
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Mass spectrometry based identification of geometric isomers during metabolic stability study of a new cytotoxic sulfonamide derivatives supported by quantitative structure-retention relationships
PublicationA set of 15 new sulphonamide derivatives, presenting antitumor activity have been subjected to a metabolic stability study. The results showed that besides products of biotransformation, some additional peaks occurred in chromatograms. Tandem mass spectrometry revealed the same mass and fragmentation pathway, suggesting that geometric isomerization occurred. Thus, to support this hypothesis, quantitative structure-retention relationships...
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Safe-by-Design Ligand-Coated ZnO Nanocrystals Engineered by an Organometallic Approach: Unique Physicochemical Properties and Low Toxicity toward Lung Cells
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(1→3)-α-d-Glucooligosaccharides Increase the Killing Capacity of NK Cells against Selected Human Colon Cancer Cells
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Role of size scale of ZnO nanoparticles and microparticles on toxicity toward bacteria and osteoblast cancer cells
PublicationThe specific role of size scale, surface capping, and aspect ratio of zinc oxide (ZnO) particles on toxicity toward prokaryotic and eukaryotic cells was investigated. ZnO nano and microparticles of controlled size and mor- phology were synthesized by wet chemical methods. Cytotoxicity toward mammalian cells was studied using a human osteoblast cancer cell line and antibacterial activity using Gram-negative bacteria (Escherichia...
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In vivo degradation of short-term implants
PublicationStan powierzchni wywiera istotny wpływ na właściwości użytkowe implantu. Stawiane wymagania, zależą od funkcji jakie ma spełniać wszczep oraz rodzaju implantowanego materiału. W przypadku implantów krótkotrwałych wymagana jest przede wszystkim odpowiednia odporność korozyjna, nie powinno tworzyć się trwałe połączenie pomiędzy wszczepem a tkanką kostną.Wszystkie biomateriały ulegają degradacji. Ważne jest to, aby produkty tej degradacji...
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Synthesis and antimicrobial activity of 6-sulfo-6-deoxy-D-glucosamine and its derivatives
Publication6-Sulfo-6-deoxy-D-glucosamine (GlcN6S), 6-sulfo-6-deoxy-D-glucosaminitol (ADGS) and their N-acetyl and methyl ester derivatives have been synthesized and tested as inhibitors of enzymes catalyzing reactions of the UDP-GlcNAc pathway in bacteria and yeasts. GlcN6S and ADGS at micromolar concentrations inhibited glucosamine-6-phosphate (GlcN6P) synthase of microbial origin. The former was also inhibitory towards fungal GlcN6P N-acetyl...
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Theoretical Encapsulation of Fluorouracil (5-FU) Anti-Cancer Chemotherapy Drug into Carbon Nanotubes (CNT) and Boron Nitride Nanotubes (BNNT)
PublicationIntroduction: Chemotherapy with anti-cancer drugs is considered the most common approach for killing cancer cells in the human body. However, some barriers such as toxicity and side effects would limit its usage. In this regard, nano-based drug delivery systems have emerged as cost-effective and efficient for sustained and targeted drug delivery. Nanotubes such as carbon nanotubes (CNT) and boron nitride nanotubes (BNNT) are promising...
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Morphological and cellular alternations of HepG2 cells overexpressing CYP3A4 after treatment with antitumor imidazoacridinone derivative C-1311
PublicationW pracy badano odpowiedź biologiczną komórek nowotworu wątroby HepG2 z nadekspresją izoenzymu CYP3A4 pod wpływem pochodnej imidazoakrydonu C-1311. Wyniki porównywano z odpowiedzią komórek HepG2 z tzw. wektorem zerowym.Izoeznym CYP3A4 jest jednym z izoenzymów cytochromu P450 odpowiedzialnych za przemiany metaboliczne pochodnej C-1311. Wykazano, że pochodna C-1311 indukuje w obu liniach komórkowych blok w fazie G2/M cyklu komórkowego,...
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A novel in vitro assay for assessing efficacy and toxicity of antifungals using human leukaemic cells infected with Candida albicans
PublicationAims: This study describes a novel in vitro assay that simultaneously determines antifungal efficiency and host cell toxicity using suspensions of human leukaemic cells (HL-60) infected with Candida albicans. Methods and Results: The effect of Candida infection on host cell viability was evaluated by the microscopy of trypan blue-stained cells and lactate dehydrogenase (LDH) activity. The in vitro ‘drug potency assay’ utilized...
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Aqueous Extracts of Selected Potentilla Species Modulate Biological Activity of Human Normal Colon Cells
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The response of human colon cancer cells to C-1748 (4-methyl-1-nitroacridine derivative) treatment
PublicationPrzeprowadzone badania miały na celu określenie wpływu pochodnej 4-metylo-1-nitroakrydyny C-1748 na komórki ludzkiego raka okrężnicy HCT8 oraz HT29. Komórki obu linii, traktowane badanym związkiem, ulegały przede wszystkim apoptozie, przy czym liczba komórek apoptotycznych była znacznie większa w przypadku linii HCT8. Ponadto, proliferacja części komórek HCT8, została zahamowana w wyniku uruchomienia procesu starzenia, czego nie...
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Development of Sulfamoylated 4‑(1-Phenyl‑1H‑1,2,3-triazol-4-yl)phenol Derivatives as Potent Steroid Sulfatase Inhibitors for Efficient Treatment of Breast Cancer
PublicationWe present here the advances achieved in the development of new sulfamoylated 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives as potent steroid sulfatase (STS) inhibitors for the treatment of breast cancer. Prompted by promising biological results and in silico analysis, the initial series of similar compounds were extended, appending a variety of m-substituents at the outer phenyl ring. The inhibition profiles of the newly...
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The modulatory effect of green tea catechin on drug resistance in human ovarian cancer cells
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Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems.
PublicationBackground Among the studied antitumor acridinone derivatives developed in our laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) exhibited cytotoxic and antitumor properties against several cancer types and were selected to be evaluated in preclinical and early-phase clinical trials. In the present work, we investigated the impact of C-1305...
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Voltammetric and biological studies of folate-targeted non-lamellar lipid mesophases
PublicationFolate-targeted lipid nanostructures are promising strategies for the development of biocompatible drug delivery systems. The objective of this study was to evaluate the efficacy of drug delivery to cancer cells by folate-targeted lipid mesophases, cubosomes (CUB) and hexosomes (HEX), loaded with doxorubicin (DOX). Three cancer-derived cell lines (KB, HeLa, T98G) exhibiting different expressional levels of folate receptor protein...
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Got a Light? Illuminating Lung Cancer
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