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Search results for: MDRUG DELIVERY
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Operation, Administration, Maintenance in Carrier Grade Ethernet
PublicationOAM (Operation, Administration and Maintenance) plays a crucial role in carrier networks. OAM functionality ensures that network operators and service providers can maintain the quality of the services they offer. One of its major tasks is the detection of anomalies in the network before they become a problem. This enables network operators and service providers to deliver services that come up to a predetermined level of quality...
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Multistage generalized adaptive notch filter with improved accuracy
PublicationGeneralized adaptive notch filters (GANFs) are estimators of coefficients of quasi-periodically time-varying systems. Current state of the art GANFs can deliver highly accurate estimates of system variations’ frequency, but underperform in terms of accuracy of the coefficient estimates. The paper proposes a novel multistage GANF with accuracy improved in this aspect. The processing pipeline consists of three stages. The preliminary...
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Synthesis, characterization, and interactions of single-walled carbon nanotubes modified with doxorubicin with Langmuir–Blodgett biomimetic membranes
PublicationThe synthesis, characterization, and the influence of single-walled carbon nanotubes (SWCNTs) modified with an anticancer drug doxorubicin (DOx) on the properties of model biological membrane as well as the comparison of the two modes of modification has been presented. The drug was covalently attached to the nanotubes either preferentially on the sides or at the ends of the nanotubes by the formation of hydrazone bond. The efficiency...
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Targeting Spike‐ACE2 Interface of SARS‐CoV‐2 and its Omicron Variant: A Comparative Screening of Potential Inhibitors for Existing and Anticipating Variants Using Molecular Modelling Approach
PublicationThe recent COVID pandemic has shown major impact on public health and economic crisis. Despite the development of many vaccines and drugs against the severe acute respiratory syndrome (SARS) coronavirus 2, the pandemic still persists. The continued spread of the virus is largely driven by the emergence of viral variants such as α, β, γ, delta, epsilon spike, omicron and its subvariants (BA.1,2,3) which can evade the current vaccines...
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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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In vivoevaluation of the CB1allosteric modulator LDK1258 reveals CB1-receptor independent behavioral effects
PublicationIn the present study, we examined whether LDK1258, which produces strong CB1receptor allosteric effects ininvitroassays, would elicitin vivoeffects consistent with allosteric activity. In initial studies, LDK1258 reducedfood consumption and elicited delayed antinociceptive effects in the chronic constrictive injury of the sciaticnerve (CCI) model of neuropathic pain, which unexpectedly emerged 4 h post-injection. UPLC-MS/MS analysisquantified...
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Influence of Parameters of Laser Beam Welding on Structure of 2205 Duplex Stainless Steel
PublicationLaser welding is used in modern industry, having many advantages comparing to traditional welding technologies. Nowadays, industry sectors such as shipbuilding, automotive and aviation can’t be imagined without laser processing technologies. Possibility of increase of welded joint properties, autogenous welding and high level of process automation makes the technology of laser welding perspective part of the industry. Physical...
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Chitosan-based electrospun nanofibers for encapsulating food bioactive ingredients: A review
PublicationToday, society has been more aware of healthy food products and related items containing bioactive compounds, which potentially contribute to human health. Unfortunately, the long-term stability and bioactivity of biologically active compounds against environmental factors compromise their target and effective action. In this way, lab-designed vehicles, such as nanoparticles and nanofibers, provide enough properties for their preservation...
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Amphotericin B and Its New Derivatives - Mode of Action
PublicationAmphotericin B (AmB) is a well known antifungal and antiprotozoal antibiotic used in the clinic for several decades. Clinicalapplications of AmB, however, are limited by its nephrotoxicity and many other acute side effects which are not acceptable by patientswhen their life is not threaten. In order to improve the therapeutic index of this drug, lipid formulations have been introduced and manyefforts have been made to obtain less...
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Development of different methods for drugs and psychoactive substances extraction from hair samples and their identification based on HPLC-ESI-QTOF analysis
PublicationOver the past decade, the use of non-controlled designer drugs and drug of abuse has rapidly increased. Hair, as a human matrix, enables detection of drugs incorporated into its structure. Studies of presence and identification of drug metabolites in human hair samples has been performed using liquid chromatography electrospray ionization quadrupole time of flight mass spectrometry (HPLC-ESI-QTOF-MS) with steady alternation of...
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Self-Association of Amphotericin B: Spontaneous Formation of Molecular Structures Responsible for the Toxic Side Effects of the Antibiotic
PublicationAmphotericin B (AmB) is a lifesaving antibiotic used to treat deep-seated mycotic infections. Both the pharmaceutical activity and highly toxic side effects of the drug rely on its interaction with biomembranes, which is governed by the molecular organization of AmB. In the present work we present detailed analysis of self-assembly of AmB molecules in different environments, interesting from the physiological standpoint, based...
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Data, Information, Knowledge, Wisdom Pyramid Concept Revisited in the Context of Deep Learning
PublicationIn this paper, the data, information, knowledge, and wisdom (DIKW) pyramid is revisited in the context of deep learning applied to machine learningbased audio signal processing. A discussion on the DIKW schema is carried out, resulting in a proposal that may supplement the original concept. Parallels between DIWK pertaining to audio processing are presented based on examples of the case studies performed by the author and her collaborators....
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Analiza wielokryterialna wariantów systemu zaopatrzenia w wodę zespołu padów
PublicationJednym z istotnych problemów decyzyjnych na etapie potencjalnej eksploatacji gazu z formacji łupkowych jest wybór sposobu zaopatrzenia w wodę kopalni gazu łupkowego. Z uwagi na duże zapotrzebowanie na wodę do procesu szczelinowania kolejno przekazywanych do eksploatacji odwiertów wydobywczych, należy poszukiwać systemu zaopatrzenia w wodę, który zagwarantuje wymaganą jej ilość, a jednocześnie nie będzie zbyt dużym obciążeniem dla...
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Wpływ ścieków przemysłowych na energochłonność i efektywność procesów technologicznych w komunalnej oczyszczalni ścieków
PublicationW artykule skupiono się na przedstawieniu wpływu jakości i ilości ścieków przemysłowych wprowadzanych do sieci kanalizacyjnej PEWIK GDYNIA Sp. z o. o. na stabilność procesów technologicznych. Określono również wpływ ścieków przemysłowych na energochłonność i efektywność oraz na wzrost kosztów oczyszczania ścieków komunalnych w Grupowej Oczyszczalni Ścieków „Dębogórze” w latach 2012-2015.
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Postawy osób starszych wobec tradycyjnych i innowacyjnych kanałów dystrybucji usług finansowych
PublicationRosnący udział osób starszych w strukturze populacji stawia nowe wyzwania przed przedsiębiorstwami oferującymi produkty do nich skierowane. Przykładem takich produktów są usługi finansowe. Przedmiotem niniejszego tekstu są usługi ubezpieczeniowe i bankowe oferowane osobom starszym z wykorzystaniem tradycyjnych i nowoczesnych kanałów dystrybucji. Na podstawie przeglądu literatury sformułowano dwie hipotezy badawcze: H1: Cechy społeczno-demograficzne...
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MACHINE LEARNING SYSTEM FOR AUTOMATED BLOOD SMEAR ANALYSIS
PublicationIn this paper the authors propose a decision support system for automatic blood smear analysis based on microscopic images. The images are pre-processed in order to remove irrelevant elements and to enhance the most important ones - the healthy blood cells (erythrocytes) and the pathologic (echinocytes). The separated blood cells are analyzed in terms of their most important features by the eigenfaces method. The features are the...
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EXPERIMENTAL EVALUATION OF DLC/STEEL SLIDING CONTACTS’ OPERATIONAL ENVELOPE
PublicationIn an industrial project concerning sliding bearings, a sliding pair was selected of high alloy steel vs. industrial grade DLC coated high alloy steel as a basis for an innovative design of high performance sliding bearings lubricated with a synthetic oil for use in geared transmission units. The development process required credible data on the ultimate resistance of the sliding pair to very high contact stress. An experimental...
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Performance Models of a Multidomain IMS/NGN Service Stratum
PublicationThis paper quantifies call processing performance (CPP) of a multidomain IMS/NGN architecture, which was proposed to deliver current and future telecommunication services with strict quality requirements, independently of the transport network technologies. A realistic simulation model is used as a reference for evaluation of the analytical results, in which vari-ous types of queuing systems are applied to model the opera-tion...
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Role of public space in designing complex urban structures
PublicationThe aim of this article is to present the main assumptions about design studios as held in the Faculty of Architecture at Gdańsk University of Technology (FA-GUT), Gdańsk, Poland, adapted to the development of key competencies in the urban planning of complex urban structures. One of these competencies is the design of public spaces. The main goal of the studios was to deliver knowledge of the role of public spaces in the design...
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PROMOWANIE USUGI PRZELEWU NATYCHMIASTOWEGO BLUECASH W BANKACH SPÓŁDZIELCZYCH
PublicationCelem pracy jest prezentacja Systemu Płatności BlueCash, którego operatorem jest firma Blue Media S.A.. Wskazuje on również na charakterystykę usługi szybkiego przelewu. Celem szczegółowym jest wskazanie na formy promocji stosowane przez banki w celu poinformowania klientów o dostępności płatności natychmiastowych. Tytułem zebrania danych na temat form promocji, autor przeprowadził badanie ankietowe pośród banków uczestników systemu płatności.
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Highly Conserved Homotrimer Cavity Formed by the SARS-CoV-2 Spike Glycoprotein: A Novel Binding Site
PublicationAn important stage in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) life cycle is the binding of the spike (S) protein to the angiotensin converting enzyme-2 (ACE2) host cell receptor. Therefore, to explore conserved features in spike protein dynamics and to identify potentially novel regions for drugging, we measured spike protein variability derived from 791 viral genomes and studied its properties by molecular...
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Determination of bromhexine and its metabolites in equine serum samples by liquid chromatography – Tandem mass spectrometry: Applicability to the elimination study after single oral dose
PublicationBromhexine (BH), expectorant used in the treatment of respiratory disorders associated with viscid or excessive mucus, is not permitted for use in the competing horse by many authorities in horseracing and Olympic disciplines. Metabolic studies are of the great importance in anti-doping field because they allow for updating the selection of the most appropriate markers for prohibited substances, such as metabolites present at higher...
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New bulk liquid membrane oscillator composed of two coupled oscillators with diffusion-mediated physical coupling
PublicationA new type of bulk liquid membrane system, which represents the first example of a bulk liquid membrane oscillator characterised by the presence of two coupled oscillators, is described. When the benzyldimethyltetradecylammonium chloride surfactant undergoes an oscillatory mass transfer through a nitromethane liquid membrane, a new liquid layer (phase X) appears between the membrane and the acceptor phase. Kinetic analysis provides...
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The investment process in the power supply industry
PublicationThe basis for power supply industry programming in a market economy should be the principle of sustainable development, which must take into account maintaining an adequate level of energy security on the one hand, and the aim to preserve the maximum degree of non-renewable resources on the other hand. Therefore, the overriding aim should be a strive to meet the current and prospective demand for energy and fuel, in conjugation...
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Estimation of smokers' exposure to mercury from combustible tobacco products, based on the approach used in food consumers’ exposure estimation
PublicationSmoking has been known to mankind for centuries, but it is only in recent decades that much attention has been paid to the harmfulness of this habit. Mercury inhalation is particularly dangerous in this respect and smoking creates extremely favorable conditions for the emission and targeted delivery of this element into the lungs. Despite this fact, a lack of a clear method for estimating the exposure of tobacco consumers to mercury...
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Fault detection in the marine engine using a support vector data description method
PublicationFast detection and correct diagnosis of any engine condition changes are essential elements of safety andenvironmental protection. Many diagnostic algorithms significantly improve the detection of malfunctions.Studies on diagnostic methods are rarely reported and even less implemented in the marine engine industry.To fill this gap, this paper presents the Support Vector Data Description (SVDD) method as applied to thefault detection...
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Teaching management skills to software develop- ment teams through the lean start-up methodology
PublicationIn order for development teams to understand the impact of software development on value delivery it is important that all team members, including software engineers, possess adequate management skills which not always have been acquired during university education. The lean start-up methodology techniques enable new ventures to test hypothesis, gather customer feed- back and create a minimum viable product. The obtained information...
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Extraction and evaluation of gas-flow-dependent features from dynamic measurements of gas sensors array
PublicationGas analyzers based on gas sensors are the devices which enable recognition of various kinds of volatile compounds. They have continuously been developed and investigated for over three decades, however there are still limitations which slow down the implementation of those devices in many applications. For example, the main drawbacks are the lack of selectivity, sensitivity...
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<p>Potential effects of microbial air quality on the number of new cases of diabetes type 1 in children in two regions of Poland: a pilot study</p>
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Potential of Liquid Biopsy in Papillary Thyroid Carcinoma in Context of miRNA, BRAF and p53 Mutation
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Role of Human UDP-Glucuronosyltransferases in the Biotransformation of the Triazoloacridinone and Imidazoacridinone Antitumor Agents C-1305 and C-1311 : Highly Selective Substrates for UGT1A10
Publication5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties than C-1311. Previously published studies showed that these...
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Genotoxicity of selected pharmaceuticals, their binary mixtures, and varying environmental conditions – study with human adenocarcinoma cancer HT29 cell line
PublicationPharmaceutical residues are present in the environment in mixtures and their adverse effects may also result from interactions that occur between compounds. Studies presented in this work focus on genotoxicity of pharmaceuticals from different therapeutic groups in mixtures and in individual solutions impacted with different environmental conditions assessed using comet assay (alkaline approach). Binary mixtures of pharmaceuticals...
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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublicationIn the present work, we described convenient methods for the synthesis ofN-thiophosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates as steroid sulfatase(STS) inhibitors. To design the structures of the potential STS inhibitors, molecularmodeling techniques were used. A computational docking method was used to deter-mine the binding modes of the synthesized inhibitors as well as to identify potentialinteractions between specified...
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Vitamin D Metabolism Gene Polymorphisms and Their Associated Disorders: A Literature Review
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Prolonged Quercetin Administration Diminishes the Etoposide-Induced DNA Damage in Bone Marrow Cells of Rats
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Acridinone antitumor agents: C-1311, C-1330 and C-1305 are metabolized by flavin-containing monooxygenase isoenzymes: FMO1, FMO3 and FMO5 with different rates
PublicationRekombinantowe ludzkie monooksygenazy flawinowe: FMO1, FMO3, FMO5 indukują przemiany metaboliczne wybranych do badań pochodnych akrydonu. Biotransformacja związków C-1311, C-1330 i C-1305 przez FMO prowadzi do jednego produktu o strukturze N-tlenku. Wyniki badań wskazują, że najbardziej podatna na przemiany wobec FMO jest pochodna triazoloakrydonu C-1305. Wydaje się więc, że głównymi enzymami pierwszej fazy przemian metabolicznych...
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Genetic Determinants of Vitamin D-Related Disorders; Focus on Vitamin D Receptor
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Morphine and methadone pre-exposures differently modify brain regional Fos protein expression and locomotor activity responses to morphine challenge in the rat
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Population analysis to assess the influence of age and body weight on pharmacokinetics and pharmacodynamics of dexmedetomidine in New Zealand White rabbits
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Acute and subacute (28-Day) toxicity studies of ionic liquid, didecyldimethyl ammonium acesulfamate, in rats
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The pharmacokinetics of propofol in ICU patients undergoing long-term sedation
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The quantification of reticulocyte maturation and neocytolysis in normal and erythropoietin stimulated rats
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublicationIn 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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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Human carnosinases: A brief history, medicinal relevance, and in silico analyses
PublicationCarnosine, an endogenous dipeptide, has been found to have a plethora of medicinal properties, such as antioxidant, antiageing, and chelating effects, but with one downside: a short half-life. Carnosinases and two hydrolytic enzymes, which remain enigmatic, are responsible for these features. Hence, here we emphasize why research is valuable for better understanding crucial concepts like ageing, neurodegradation, and cancerogenesis,...
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Targeting shelterin proteins for cancer therapy.
PublicationAs 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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The role of intestine and liver in glucuronidation of the imidazo- and triazoloacridinone antitumor agents, C-1311 and C-1305: High affinity substrates for UGT1A10
PublicationCelem przeprowadzonych badań było określenie roli poszczególnych izoform UDP-glukuronylotransferazy (UGT)oraz mikrosomów jelita(HIM)i wątroby (HLM) wyizolowanych od różnych pacjentów w metabolizmie pochodnych akrydonu, związków C-1311 i C-1305. Wykazano, że rodziną UGT katalizującą przemiany C-1305 i C-1311 jest UGT1A, z najwyższą aktywnością wykazywaną przez pozawątrobowy izoenzym UGT1A10. Rozkład aktywności frakcji mikrosomalnych...
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Biotransformation of abused synthetic cannabinoids, JWH-018 and JWH-073, by human cytochromes P450 and UDP-glucuronosyltransferases
PublicationZwiązki oznaczone symbolami JWH-018 i JWH-073 są syntetycznymi pochodnymi kanabinoidów, obecnymi w preparatach o działaniu psychoaktywnym (K2/Spice). Wcześniejsze badań wykazały, że u osób przyjmujących tzw. ''legalną marihuanę'', głównymi produktami biotransformacji obecnymi w moczu były hydroksylowe pochodne obu związków, jak również ich glukuronidy. W związku z tym celem prowadzonych badań było określenie roli poszczególnych...
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Protective Effect of Aronia Melanocarpa Polyphenols on Cadmium Accumulation in the Body: A Study in a Rat Model of Human Exposure to this Metal
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Aqueous Extracts of Selected Potentilla Species Modulate Biological Activity of Human Normal Colon Cells
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