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Wyniki wyszukiwania dla: MURAMYL DIPEPTIDE, MURAMYL DIPEPTIDE ANALOGS, ANTICANCER COMPOUNDS, ANTICANCER ACTIVITY, NOD2 RECEPTOR, ADJUVANT THERAPY
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Batracylina (BAT) - potencjalny lek przeciwnowotworowy. Batracylin (BAT) - potential of anticancer drug
PublikacjaOpisano działanie potencjalnego leku przeciwnowotworowego - batracyliny(BAT). Batracylina została wyselekcjonowana przez National Cancer Institute (NCI, Bethesda, USA) w 1978 roku jako efekt programu poszukiwań nowych leków chemioterapii.Związek ten w badaniach in vivo u myszy okazał się bardzo aktywny przeciw nowotworowi okrężnicy 38 (colon 38), trudnemu do wyleczenia przez znane leki przeciwnowotworowe. Okazała się ona skuteczna...
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In Search of Panacea—Review of Recent Studies Concerning Nature-Derived Anticancer Agents
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Anticancer properties of low molecular weight oat beta-glucan – An in vitro study
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Dysfunctional prefrontal cortical network activity and interactions following cannabinoid receptor activation.
PublikacjaCoordinated activity spanning anatomically distributed neuronal networks underpins cognition and mediates limbic-cortical interactions during learning, memory, and decision-making. We used CP55940, a potent agonist of brain cannabinoid receptors known to disrupt coordinated activity in hippocampus, to investigate the roles of network oscillations during hippocampal and medial prefrontal cortical (mPFC) interactions in rats. During...
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Synthesis of new antrapyridazone derivatives - a novel group of anticancer agents active on a multidrugresistant(MDR) tumor cell lines
PublikacjaNovel antrapyridazone derivatives were synthesized and biologically evaluated in order tobroaden the data on structure-activity relationship of this class of cytostatics. Recent literaturedata prove that acetamides react better with aryl chlorides. A new approach based onintroduction of other amides form into aromatic ring in Ullmann was tested. This new methodcould give better yields and make purification step more convenient.
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Anticancer and antimicrobial properties of novel η6-p-cymene ruthenium(ii) complexes containing a N,S-type ligand, their structural and theoretical characterization
PublikacjaRuthenium(II) complexes are lately of great scientific interest due to their chemotherapeutic potential asanticancer and antimicrobial agents. Here we present the synthesis of new pyrazole carbothioamidederivatives and their four arene–ruthenium complexes. The title compounds were characterized with theapplication of IR, NMR, mass spectrometry, elemental analysis and X-ray diffraction. Additionally, for newcomplexes DFT calculations...
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Deltorphin analogs restricted via a urea bridge: structure and opioid activity
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Deltorphin analogs restricted via a urea bridge: structure and opioid activity
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Tuftsin-Properties and Analogs
PublikacjaImmunomodulation is one of the significant therapeutic strategies. It includes both stimulation or suppression of the immune system by a variety of substances called immunomodulators, designed to regulate the immune response of the organism to infections of varying etiology. An example of such a substance is tuftsin (TKPA) 3 (Fig. (1)). Tuftsin is an endogenous immunomodulator of a wide spectrum of biological activity. Tetrapeptide...
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Synthesis and Characterization of Size- and Charge-Tunable Silver Nanoparticles for Selective Anticancer and Antibacterial Treatment
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Cisplatin filled multiwalled carbon nanotubes – a novel molecular hybrid of anticancer drug container
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Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)
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A novel source of the cardiac glycoside digoxin from the endophytic fungus Epicoccum nigrum : isolation, characterization, production enhancement by gamma irradiation mutagenesis and anticancer activity evaluation
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Regioselective synthesis of novel 4,5-diaryl functionalized 3,4-dihydropyrimidine-2(1H)-thiones via a non-Biginelli-type approach and evaluation of their in vitro anticancer activity
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Comparison of the content of phenolic compounds and antioxidant activity of white, red and black currants (Ribes sp.) extracts
PublikacjaThe aim of this study was to compare the content of antioxidant compounds and the antioxidant activity of extracts from white, red and black currants (Ribes sp.). The chemical properties verified included determinations of anthocyanins and other phenols by HPLC-DAD-MS, total antioxidant activity by standard spectrophotometric tests (ABTS, DPPH and FCR), and profiles of antioxidants by TLC with visualization reagents (ABTS, DPPH,...
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H2AX phosphorylation, its role in DNA damage response and cancer therapy
PublikacjaDouble-strand breaks (DSBs) are the most deleterious DNA lesions, which, if left unrepaired, may have severe consequences for cell survival, as they lead to chromosome aberrations, genomic instability, or cell death. Various physical, chemical, and biological factors are involved in DSB induction. Cells respond to DNA damage by activating the so-called DNA damage response (DDR), a complex molecular mechanism developed to detect...
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Evaluation and cellular responses of modulators of TRF1/TRF2 protein’s function as potential anticancer drugs interfering with telomeric shelterin’s function
PublikacjaA number of proteins that interact with telomeres have been identified in human cells, indicating the high plasticity of human nucleoprotein complex organization. The most important complex is the "shelterin" complex, which consists of six proteins: TRF1, TRF2, TIN2, POT1, TPP1. The TRF1 and TRF2 directly bind to telomeric double-stranded DNA and the TIN2 protein. The TIN2 protein also binds to the TPP1 protein, stabilizing the...
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New Chalcones Derivatives With Potent Antitumor Activity And Their Metabolism In Vitro
PublikacjaChalcone derivatives exhibit a broad range of biological activities, with antioxidant and cytotoxic properties among the most studied. Despite numerous reports on chalcones as cytotoxic, and potentially anticancer agents, very little is know on their actual mechanism of activity. Generally, chalcones are considered as antimitotic agents, which interfere with tubulin assembly.We have recently developed a new class of chalcones with...
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Using Flavonoid Substitution Status to Predict Anticancer Effects in Human Melanoma Cancers: An In Vitro Study
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Biosynthesis of zinc oxide nanoparticles with antimicrobial, anticancer, antioxidant and photocatalytic activities by the endophytic Alternaria tenuissima
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Modulation of cellular response to anticancer treatment by caffeine:inhibition of cell cycle checkpoints, DNA repair and more
PublikacjaKofeina i inne metyloksantyny wywołują bardzo różne efekty fizjologiczne w organizmie człowieka. W pracy przedstawiamy, które z tych efektów mogą wpływać na skuteczność terapii przeciwnowotworowych. Kofeina może bezpośrednio wpływać na transport oraz aktywację metaboliczną cząsteczek leków do komórki, poprzez tworzenie kompleksów z lekami zawierającymi układy poliaromatyczne. Kofeina hamuje aktywność kinaz ATM/ATR co prowadzi do...
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Enzymatic cleavage of specific dipeptide conjugated with ferrocene as a flexible ultra-sensitive and fast voltammetric assay of matrix metalloproteinase-9 considered a prognostic cancer biomarker in plasma samples
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Chemical and biological evaluation of antioxidant activity of endogenous redox-active compounds compared to plant-derived exogenous antioxidants
PublikacjaThe research conducted so far has shown that endogenous antioxidants, despite being regarded as the first line of antioxidant defense, may not be sufficient to maintain redox homeostasis in cells exposed to oxidative stress. The results obtained in the doctoral dissertation show that endogenous redox-active compounds were moderate or weak scavengers of ABTS and DPPH radicals, while in cellular setting, their impact on the reducing...
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The neuroprotective activity of new phenylalanine-based AMPA receptor antagonists
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The thermostability, bioactive compounds and antioxidant activity of some vegetables subjected to different durations of boiling: investigation in vitro
PublikacjaThis research was performed in order to compare the water and acetone extracts of raw and boiled for 10, 20, 40 and 60 min Korean lotus roots (KLR) and Polish white onion (PWO) in the contents of theirbioactive compounds, antioxidant activity and thermostability.It was found that polyphenols (mg GAE/g), flavanols (mg GAE/g), flavonoids (mg CE/g), anthocyanins (mg CGE/kg) and tannins (mg CE/g) in water extract of raw lotus roots...
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The termostability, bioactive compounds and antioxidant activity of some vegetables subjected to different durations of boiling: investigation in vitro.
PublikacjaThis research was performed in order to compare the water and acetone extracts of raw and boiled for 10, 20, 40 and 60 min Korean lotus roots (KLR) and Polish white onion (PWO) in the contents of theirbioactive compounds, antioxidant activity and thermostability. It was found that polyphenols (mg GAE/g), flavanols (mg GAE/g), flavonoids (mg CE/g), anthocyanins(mg CGE/kg) and tannins (mg CE/g) in water extract of raw lotus roots...
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Effect of new bisacridines IKE16, IKE18 and IE10 on the yeast topoisomerase II relaxation activity
Dane BadawczeThe datasets contain the results of new bisacridines IKE16, IKE18 and IE10 inhibition activity against yeast topoisomerase II. DNA topoisomerases (Topo) are enzymes that catalyze changes in the spatial structure of DNA and play an important role in replication, transcription and recombination. Beyond their normal functions, DNA topo are significant...
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DNA-reactive anticancer imidazoacridinone C-1311 is a new inhibitor of hypoxia-inducible factor 1 alpha, vascular endothelial growth factor and tumor angiogenesis
PublikacjaHypoxia-inducible factor 1 (HIF-1) plays a critical role for tumor adaptation to hypoxia and promotes angiogenesis. Antitumor imidazoacridinone C-1311 is a DNA reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor selected for phase II clinical trials for breast cancer. Here, we demonstrate the new mechanism of C-1311 action involving HIF-1a, vascular endothelial growth factor (VEGF) and angiogenesis as additional...
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Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cell
PublikacjaThe main activity of mycophenolic acid (MPA) and its analogs is the inhibition of proliferation of T cells. Here, we hypothesized that MPA and its conjugates inhibits also the activity of antigen-presenting cells (APC) including dendritic cells (DCs). We tested the effect of novel amino acid derivatives of MPA and conjugates of MPA with acridines/acridones on DCs by flow cytometry, ELISA and MLR assay. Both acridines/acridone derivatives...
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CYP3A4 overexpression enhances apoptosis induced by anticancer agent imidazoacridinone C-1311, but does not change the metabolism of C-1311 in CHO cells
PublikacjaWe examine whether CYP3A4 overexpression influences the rate and pattern of antitumor imidazoacridinone C-1311 metabolism, in relation to the impact of this overexpression on cell cycle progression and final cellular response of CHO cells following C-1311 treatment. Methods: Three CHO cell lines: CHO-WT, wild type, CHO-HR, overexpressing cytochrome P450 reductase (CPR) and CHO-HR-3A4, coexpressing CPR and CYP3A4 were applied....
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Targeting shelterin proteins for cancer therapy.
PublikacjaAs a global health challenge, cancer prompts continuous exploration for innovative therapies that are also based on new targets. One promising avenue is targeting the shelterin protein complex, a safeguard for telomeres crucial in preventing DNA damage. The role of shelterin in modulating ataxia- telangiectasia mutated (ATM) and ataxia-telangiectasia and Rad3-related (ATR) kinases, key players in the DNA damage response (DDR),...
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Inhibitory and antimicrobial activities of OGTI and HV-BBI peptides, fragments and analogs derived from amphibian skin
PublikacjaA series of linear and cyclic fragments and analogs of two peptides (OGTI and HV-BBI) isolated from skin secretions of frogs were synthesized by the solid-phase method. Their inhibitory activity against several serine proteinases: bovine beta-trypsin, bovine alpha-chymotypsin, human leukocyte elastase and cathepsin G from human neutrophils, was investigated together with evaluation of their antimicrobial activities against Gram-negative...
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Fluorescent analogs of trypsin inhibitor SFTI-1 isolated from sunflower seeds-synthesis and applications
PublikacjaThis article describes the synthesis and enzymatic study of newly synthesized analogs of trypsin inhibitors SFTI-1 that were fluorescent labeled on their N-terminal amino groups. Two fluorescent derivatives of benzoxazole (3-[2-(4-diphenylaminophenyl) benzoxazol-5-yl]-L-alanine[(4NPh(2)) Ph] Box-Ala and 3-[2-(2', 4', 5'-trimethoxyphenyl) benzoxazol-5-yl]-l-alanine-[2,4,5-(OMe)3Ph] Box-Ala) were used as efficient fluorescent labels....
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An In Vitro Anticancer, Antioxidant, and Phytochemical Study on Water Extract of Kalanchoe daigremontiana Raym.-Hamet and H. Perrier
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Sandwich-like mesoporous silica flakes for anticancer drug transport—Synthesis, characterization and kinetics release study
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In vitro and in vivo evaluation of sandwich-like mesoporous silica nanoflakes as promising anticancer drug delivery system
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Isoform-specific inhibition of DNA topoisomerase II as the mechanism of action of novel anticancer agent C-1305
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Anticancer potential of acetone extracts from selected Potentilla species against human colorectal cancer cells
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In Vitro Anticancer Potential of Jasione montana and Its Main Components against Human Amelanotic Melanoma Cells
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Discovery of the anticancer drug vinblastine from the endophytic Alternaria alternata and yield improvement by gamma irradiation mutagenesis
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Strain improvement and immobilization technique for enhanced production of the anticancer drug paclitaxel by Aspergillus fumigatus and Alternaria tenuissima
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Sonochemical synthesis of rosuvastatin based novel 3-methyleneisoindolin-1-one derivatives as potential anticancer agents
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Thromboelastometric Analysis of Anticancer Cerrena unicolor Subfractions Reveal Their Potential as Fibrin Glue Drug Carrier Enhancers
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Selective detection of F- by chromogenic tetrazole receptor
PublikacjaA chromogenic anion host 4, containing two amide functionalities linked to azo dye and tetrazole rings was synthesized and its complexes with various anions were investigated. The results show that receptor 4 can recognize selectively biologically important F- ion. The binding affinity for F- was investigated by naked-eye colour change, UV-Vis and 1H NMR spectroscopy. Addition F- ion in CH3CN and DMSO to receptor 4 cause a colour...
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Towards β-selectivity in functional estrogen receptor antagonists
PublikacjaBased on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques. It was found that the introduction of a BSC in these systems brings about a decrease of affinity for both estrogen receptors α and β in an in vitro competitive...
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Superconductivity and superconducting compounds
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Evaluation of Receptor Affinity, Analgesic Activity and Cytotoxicity of a Hybrid Peptide, AWL3020
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New clicked full agonists of the estrogen receptor β
PublikacjaA click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists...
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Synthesis and molecular structure of novel 2-(alkylthio)-4-chloro-N-(4,5-dihydro-5-oxo-1H-1,2,4-triazol-3-yl)-5-methylbenzenesulfonamideswith potential anticancer activity
PublikacjaOtrzymano 15 nowych związków: 2-(alkilotio)-4-chloro-N-(4,5-dihydro-5-oxo-1H-1,2,4-triazol-3-yl)-5-metylobenzenosulfonamidów, dla których opracowano nową metodę syntezy. Dla jednej pochodnej wyznaczono strukturę rentgenowską. Związek nr 36 wykazuje wysoką aktywność przeciwnowotworową w stosunku do 13 linii komórek nowotworowych o poziomie GI_50 w zakresie stężeń 1,9-3,0 μM.