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Wyniki wyszukiwania dla: EC50
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Determination of EC50 toxicity data of selected heavy metals toward heterocypris incongruens and their comparison to "direct-contact" and microbiotests
PublikacjaW artykule omówiono czułość organizmu Heterocypris incongruens wobec metali ciężkich. Pomimo iż test Ostracodtoxkit F jest dostępny hadlowo na rynku od wielu lat to brak jest danych na temat czułości i selektywności tego organizmu, a dane na ten temat są niezbędne podczas interpretowania wyników oznaczeń toksyczności chronicznej próbek gleb i osadów. Wyniki LC50 oraz EC50 zostały też porównane z danymi innych handlowo dostępnych...
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Determination of Toxicological Parameters of Selected Bioactive Organic Chemicals Using the Ostracodtoxkit FTM
PublikacjaAssessment of the impact of pharmaceutical residues on living organisms is very complex subject. Apart from taking into account the toxicity of individual compounds also their presence in mixtures should be taken into account. In this work, attempts were made to assess the ecotoxicity of biologically active substances (with 50 % effective concentration (EC50) values growing from fluoxetine (EC50 = 4.431 nM) >> gemfibrozil ≈ 17α-ethinylestradiol...
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Amberlyst-15 catalysed synthesis of novel indole derivatives under ultrasound irradiation: Their evaluation as serotonin 5‑HT2C receptor agonists
PublikacjaA series of indole based novel Schiff bases was designed as potential agonists of 5‑HT2C receptor that was supported by docking studies in silico. These compounds were synthesized via Amberlyst-15 catalysed condensation of an appropriate pyrazole based primary amine with the corresponding indole-3-aldehyde under ultrasound irradiation at ambient temperature. A number of target Schiff bases were obtained...
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Effective Drug Concentration and Selectivity Depends on Fraction of Primitive Cells
PublikacjaPoor 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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Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives
PublikacjaNew conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2′,3′-O-isopropylidene protected and free hydroxyl...
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Assessing ecotoxicity and the endocrine potential of selected phthalates, BADGE and BFDGE derivatives in relation to environmentally detectable levels
PublikacjaThere is no doubt that the subject area of plasticmaterials (e.g., production of epoxy resins or polyesters) is inherently connected to issues concerning bisphenol A (BPA) and its analogues. Unfortunately, much less attention has been given to other compounds, which are also used for the production of these materials. Bisphenol A diglycidyl ether (BADGE) is a synthetic industrial compound obtained by a condensation reaction between...
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Aromatic heptaene antibiotics as an alternative for synthetic triazole fungicides in plant protection
PublikacjaAn in vitro antifungal activity of candicidin and ascosin antibiotics (0,01-10 μg/mL) towards representative strains of phytopathogenic fungi was detd. Both compds. exhibited similar half max. effective concns. inhibiting growth of the fungi as that of tebuconazole used for comparison.
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Application of bioassays in studies on the impact of pharmaceuticals on the environment
PublikacjaDrug interactions are often desirable particularly in medicine, when treatment of a patient requires using a mixture of drugs in specific doses to produce the adequate therapeutic effect. Unfortunately, interactions between drugs in the environment are not as desirable, despite the fact that drugs are present in the environment at low concentration levels [1]. Pharmaceuticals are present in the environment in a mixture of compounds,...
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Relationship between heavy metal distribution in sediment samples and their ecotoxicity by the use of the Hasse diagram technique
PublikacjaOpisane badania wskazują, że istnieje nowe podejście oszacowywania ryzyka zanieczyszczenia określonych przedziałów środowiska morskiego dzięki równoczesnemu monitorowaniu zawartości metali ciężkich i parametrów ekotoksykologicznych. Rutynowe podejście stosuje oddzielnie wskaźniki zawartości metali ciężkich i wskaźniki ekotoksykologiczne w celu wykrycia zależności między poziomami zawartości metali ciężkich a mierzalnymi parametrami...
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Ecotoxicity and chemical sediment data classification by the useof self-organising maps
PublikacjaArtykuł dotyczy przedstawiania nowej interpretacji szacowania jakości osadów. To oryginalne podejście bada powiązania między parametrami ekotoksyczności (ostrej i chronicznej) i składnikami chemicznymi (zanieczyszczenia takie jak polichlorowane bifenyle, pestycydy, wielopierścieniowe węglowodory aromatyczne, metale ciężkie) próbek osadów Jeziora Turawskiego (Polska) poprzez zastosowanie samoorganizujących się map (SOM) wobec badanego...
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Interstrand crosslinking of DNA by C-1311 (Symadex) and other imidazoacridinones
PublikacjaImidazoakrydony, w tym pochodna C-1311 (Symadex) znajdująca się w pierwszej fazie badań klinicznych prowadzonych w USA, należą do grupy bardzo aktywnych związków przeciwnowotworowych zsyntetyzowanych w Katedrze Technologii Leków i Biochemii PG. Za pomocą zmodyfikowanej metody Parsons'a wykazaliśmy, że C-1311 indukuje, w sposób zależny od stężenia, międzyłańcuchowe wiązania sieciujące w komórkach różnych nowotworów ludzkiego pochodzenia...
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Rapid test for ionic liquids toxicity evaluation
PublikacjaW literaturze przedmiotu dostępne są dane na temat toksyczności cieczy jonowych, szczególności tych mających zastosowanie przemysłowe, gdzie toksyczność wyrażana jest jako EC50 mierzone względem konkretnego organizmu np. Vibrio fischeri, Daphnia magna itp. Z uwagi na taksonomiczne zróżnicowanie osadu czynnego nie jest możliwe bezpośrednie wnioskowanie na temat toksyczności cieczy jonowych w stosunku do osadu czynnego na podstawie...
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4-methyl-1-nitroacridine derivative C-1748 induces apoptosis, mitotic catastrophe or senescence in human colon carcinoma HCT116 cells depending on p53 status
PublikacjaPrzeprowadzone badania miały na celu określenie zdolności pochodnej 4-metylo-1-nitroakrydyny C-1748 do uruchomienia apoptozy, katastrofy mitotycznej lub procesu starzenia komórek ludzkiego raka okrężnicy HCT116 posiadających dziki gen p53 oraz podlinii nie posiadającej tego genu. Wykazano, że pochodna C-1748 indukuje apoptozę w komórkach obu linii HCT116 w sposób zależny od czasu inkubacji, przy czym komórki HCT116 p53+/+ wykazują...
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Study of the effect of residues of pharmaceuticals on the environment on the example of bioassay Microtox®
PublikacjaResidues of pharmaceuticals present in the aqueous environment can be found in a mixture of different substances wherein drugs not remain inert with respect to each other. In such mixtures a phenomenon of synergism or antagonism may occur, which can contribute to increase or decrease the overall toxicity of the mixture of drugs. Pharmaceuticals namely: diclofenac (sodium salt), oxyteracycline hydrochloride, fluoxetine hydrochloride,...
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Assessing ecotoxicity, synergic and antagonistic actions of commonly used components of polymerization mixture in molecularly imprinted polymers preparation process
PublikacjaIncreasingly, the challenge is the optimal process of developing a suitable MIP-type sorptive material (taking into account its final form and application area), which is mainly related to the efficiency/effectiveness of the polymerization process. The lack of reaction or its low efficiency generates additional waste and puts it into the environmental cycle. The main aim of the performed research was the estimation of ecotoxicity,...
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Phenolic compounds from Nerium oleander leaves: microwave assisted extraction, characterization, antiproliferative and cytotoxic activities
PublikacjaA microwave-assisted extraction (MAE) method was used for the extraction of phenolic compounds from Nerium oleander leaves. The influence of variables such as ethanol concentration, microwave power, irradiation time and liquid/solid ratio on polyphenol extraction was modelled using a second-order regression equation based on response surface methodology (RSM). The optimal conditions for MAE were: extraction solvent 35% ethanol...
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Cyclodextrin polymers as efficient adsorbents for removing toxic non-biodegradable pimavanserin from pharmaceutical wastewaters
PublikacjaPresence of even small amount of active pharmaceutical ingredients in the environment carries risks tohuman and animal health, presenting an important issue. The paper presents issues related to the newdrug - pimavanserin (PMV). Biological treatment efficiency of pimavanserin (PMV) was evaluated usinglab-scale Sequencing Batch Reactor (SBR). It has been shown to have a negative effect on aquatic or-ganisms by classifying it as...
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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.
PublikacjaBackground 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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In silico modelling for predicting the cationic hydrophobicity and cytotoxicity of ionic liquids towards the Leukemia rat cell line, Vibrio fischeri and Scenedesmus vacuolatus based on molecular interaction potentials of ions
PublikacjaIn this study we present prediction models for estimating in silico the cationic hydrophobicity and the cytotoxicity (log [1/EC50]) of ionic liquids (ILs) towards the Leukemia rat cell line (IPC-81), the marine bacterium Vibrio fischeri and the limnic green algae Scenedesmus vacuolatus using linear free energy relationship (LFER) descriptors computed by COSMO calculations. The LFER descriptors used for the prediction model (i.e....