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Smart Pen - new multimodal computer control tool for graphomotorical therapy
PublicationW sytuacji, gdy około 15% populacji uczniów wykazuje cechy dyslektyczne, koniecznością staje się wyposażenie szkół w efektywne narzędzia do diagnozy i terapii tego rodzaju zaburzeń. Dzięki wykorzystaniu tabletu i specjalnie skonstruowanego długopisu wyposażonego w czujniki nacisku uzyskano możliwość monitorowania wielu parametrów, które do tej pory były dla terapeutów całkowicie niedostępne (np. pomiar nacisku na podłoże czy ścisku...
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Badanie procederu fałszowania mięsa – poważny problem analityczny
PublicationFałszowanie żywności, w tym produktów mięsnych, stanowi problem ogólnoświatowy. Analitycy ze zdwojonym wysiłkiem pracują nad metodami badawczymi, które umożliwią zarówno weryfikację jakości jak i określenie autentyczności danego produktu żywnościowego. Dotychczas, w celu określenia autentyczności mięsa wykorzystywano najczęściej techniki oparte na elektroforezie żelowej oraz testy immunoenzymatyczne. Równie popularne, stały się...
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Planowanie testów wspomagane analizą ryzyka
PublicationTestowanie wciąż pozostaje jednym z głównych sposobów zapewniania jakości oprogramowania. Testowanie pochłania znaczne zasoby, które w praktyce mogą się okazać zbyt kosztowne. Należy więc testy planować i to w taki sposób, by skontrolować efekty wynikające z testowania oraz nakłady ponoszone na testowanie dążąc do maksymalizacji współczynnika efektów-do-nakładów. Jedną z kluczowych decyzji w tym zakresie jest decyzja o wyborze...
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Analiza możliwości automatycznego rozpoznawania zachowań zwierząt doświadczalnych
PublicationAutomatyzacja analizy zachowań zwierząt laboratoryjnych umożliwia szybką i obiektywną ocenę obserwacji. Rozwiązania w istniejących systemach skupiają się na detekcji prostych aspektów zachowań, która jest możliwa dzięki pomiarowi parametrów motorycznych zwierząt, ich punktów charakterystycznych czy kształtu ciała. Jednym z istotnych problemów w dziedzinie rozpoznania zachowań są zachowania złożone, dla których trudno jest zdefiniować...
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Modelling of Capillary Pressure-driven Water Flow in Unsaturated Concrete Using Coupled DEM/CFD Approach.
PublicationSformułowano nowatorskie, połączone podejście do modelowania dwufazowego przepływu wody napędzanego kapilarami w nienasyconym betonie. Dzięki połączeniu metody elementów dyskretnych (DEM) z obliczeniową dynamiką płynów (CFD) w warunkach izotermicznych proces został zbadany numerycznie w mezoskali w warunkach dwuwymiarowych. Niewielkie próbki betonu o uproszczonej mezostrukturze cząstek poddano w pełni sprzężonym hydromechanicznym...
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Two highly thermostable paralogous single-stranded DNA-binding proteins from Thermoanaerobacter tengcongensis
PublicationThe thermophilic bacterium Thermoanaerobacter tengcongensis has two single-stranded DNA-binding (SSB) proteins, designated TteSSB2 and TteSSB3. In a SSB complementation assay in Escherichia coli, only TteSSB3 took over the in vivo function of EcoSSB. We have cloned the ssb genes obtained by PCR and have developed E. coli overexpression systems. The TteSSB2 and TteSSB3 consist of 153 and 150 amino acids with a calculated molecular...
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Mechanics of mesh implanted into abdominal wall under repetitive load. Experimental and numerical study
PublicationThere are a number of papers discussing medical and mechanical aspects of ventral hernia management. Despite intensive work on the problem understanding, recurrences of the sickness still happen too often. For that reason new aspects of the problem must be considered. In this paper, a change in the abdominal implant’s stiffness is discussed, which is caused by cyclic loading. Such loading influence abdominal implant e.g. while...
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Active IR-Thermal Imaging in Medicine
PublicationIn this paper we summarize results of several research projects devoted to development of new diagnostic methods and procedures based on quantitative infrared thermography in medical applications. First, basics of active dynamic thermography are presented. Described are both, instrumentation and software comprising measurement procedures including collection of series of IR-images after external excitation, data treatment with...
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Bioactivities of Phenolic Compounds from Kiwifruit and Persimmon
PublicationFruit used in the common human diet in general, and kiwifruit and persimmon particularly, displays health properties in the prevention of heart disease. This study describes a combination of bioactivity, multivariate data analyses and fluorescence measurements for the differentiating of kiwifruit and persimmon, their quenching and antioxidant properties. The metabolic differences are shown, as well in the results of bioactivities...
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Determinants of the primary stability of cementless acetabular cup implants: A 3D finite element study
PublicationPrimary stability of cementless implants is crucial for the surgical success and long–term stability. However, primary stability is difficult to quantify in vivo and the biomechanical phenomena occurring during the press–fit insertion of an acetabular cup (AC) implant are still poorly understood. The aim of this study is to investigate the influence of the cortical and trabecular bone Young's moduli Ec and Et, the interference...
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Dissection of σE‐dependent cell lysis in Escherichia coli: roles of RpoE regulators RseA, RseB and periplasmic folding catalyst PpiD
PublicationTo understand the mechanism of sigma(E)-dependent cell lysis, we examined the consequences of deletion derivatives of rpoE regulators rseA, rseB and rseC on sigma(E) transcription, on levels of free versus membrane-bound sigma(E) and on OMP-biogenesis limiting factor(s) that could impact cell lysis. RT-PCR showed that individual nonpolar DeltarseA and DeltarseB increased the rpoE expression to varying extents, with pronounced induction...
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Solid Phase Synthesis and Biological Activity of Tuftsin Conjugates
PublicationNew tuftsin/retro-tuftsin conjugates were designed and synthesized using a classical fluorenylmethoxycarbonyl (Fmoc) solid phase procedure. All the peptide conjugates were divided into three series: 1,4-dihydroxyanthraquinone (type A), 1-nitroacridine (type B), and 4-carboxyacridone (type C) derivatives. In type A conjugates, the N-terminal group of the peptide chain is directly connected to the anthraquinone ring at C1 (Scheme...
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Response of a New Low-Coherence Fabry-Perot Sensor to Hematocrit Levels in Human Blood
PublicationIn this paper, a low-coherence Fabry-Perot sensor with a spectrally measured signal processing response to the refractive index of liquids is presented. Optical fiber sensors are potentially capable of continuous measuring hematocrit levels in blood. Low-coherence Fabry-Perot interferometric sensors offer a robust solution, where information about the measurand is encoded in the full spectrum of light reflected from the sensing...
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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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Antibacterial Porous Systems Based on Polylactide Loaded with Amikacin
PublicationThree porous matrices based on poly(lactic acid) are proposed herein for the controlled release of amikacin. The materials were fabricated by the method of spraying a surface liquid. Description is given as to the possibility of employing a modifier, such as a silica nanocarrier, for prolonging the release of amikacin, in addition to using chitosan to improve the properties of the materials, e.g., stability and sorption capacity....
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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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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublicationRational drug design and in vitro pharmacology profiling constitute the gold standard in drug development pipelines. Problems arise, however, because this process is often dicult due to limited information regarding the complete identification of a molecule’s biological activities. The increasing aordability of genome-wide next-generation technologies now provides an excellent opportunity to understand a compound’s diverse eects...
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Gelatin and gelatin/starch-based films modified with sorbitol for wound healing
PublicationGelatin-based films modified with sorbitol were produced from gelatin solution or gelatin/starch blends using a simple and low-cost solvent casting method, and subsequently, their physicochemical, mechanical, and biocompatibility properties were characterized. This work focused on developing and optimizing a biopolymeric blend to improve the pure biopolymers’ properties for potential biomedical applications such as wound dressing....
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Hyaluronic acid/tannic acid films for wound healing application
PublicationIn this study, thin films based on hyaluronic acid (HA) with tannic acid (TA) were investigated in three different weight ratios (80HA/20TA, 50HA/50TA, 20HA/80TA) for their application as materials for wound healing. Surface free energy, as well as their roughness, mechanical properties, water vapor permeability rate, and antioxidant activity were determined. Moreover, their compatibility with blood and osteoblast cells was investigated....
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Modified Peptide Molecules As Potential Modulators of Shelterin Protein Functions; TRF1
PublicationIn this work, we present studies on relatively new and still not well-explored potential anticancer targets which are shelterin proteins, in particular the TRF1 protein can be blocked by in silico designed "peptidomimetic" molecules. TRF1 interacts directly with the TIN2 protein, and this protein-protein interaction is crucial for the proper functioning of telomere, which could be blocked by our novel modified peptide molecules....
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A Comparative Study on the Toxicity of Chlorides and Tri-tert-butoxysilanethiolates of Zinc(II), Cadmium(II) and Mercury(II) Towards Candida albicans and Escherichia coli.
PublicationMetale przejściowe, czyli cynk, kadm i rtęć należą do XII grupy układu okresowego. Cynk jako element strukturalny białek odgrywa zróżnicowaną rolę biologiczną i jest pierwiastkiem niezbędnym do zachowania funkcji życiowych. W odróżnieniu od niego kadm i rtęć są metalami wykazującymi działanie toksyczne i podejrzanymi o działanie rakotwórcze. Kadm w szkodliwy sposób wpływa na uprawy oraz organizm ludzki. Toksyczne działanie rtęci...
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Algorytm i program sterowania układem samoczynnego załączania rezerwy zasilania z funkcją odciążania
PublicationW artykule omówiono układ samoczynnego załączania rezerwy (SZR) zasilania z jednym transformatorem i jednym generatorem przy rezerwie jawnej, z ośmioma grupami odbiorów i funkcją odciążania. W systemie sterowania tego układu SZR założono wykorzystanie sterownika programowalnego, graficznego dotykowego panelu operatorskiego i analizatorów parametrów sieci. Funkcja odciążania służy do realizacji przełączania wyłączników grup odbiorów...
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Zastosowanie immobilizowanego białka MutS do wychwytywania fragmentów DNA zawierających niesparowane zasady
PublicationBiałko MutS wiąże DNA zawierające błędnie sparowane oraz niesparowane zasady w DNA. Podjęto szereg prób wykorzystania tego białka jako narzędzia do detekcji nieznanych mutacji lub zagęszczania frakcji DNA z niesparowaną zasadą. Dotychczas żadna z metod oparta na użyciu białka MutS nie została wdrożona powszechnie do praktyki laboratoryjnej. Głównym powodem takiego stanu rzeczy jest stosunkowo silne powinowactwo MutS do DNA w pełni...
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Identification, cloning, expression, and characterizationof a highly thermostable single-stranded-DNA-binding protein (SSB) from Deinococcus murrayi
PublicationZidentyfikowano i scharakteryzowano białko SSB-podobne, pochodzące z Deinococcus murrayi (DmuSSB). Otrzymany w reakcji PCR fragment zawierający kompletny gen ssb sklonowano w systemie ekspresyjnym Escherichia coli. Gen składa się z 826 nt, kodujących 276 reszt aminokwasowych z wyliczoną teoretycznie masą cząsteczkową monomeru równą 30,14 kDa. DmuSSB zawiera dwie domeny wiążące jednoniciowe DNA OBna monomer I funkcjonuje jako homodimer....
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Role for chitin and chitooligomers in the capsular architecture of Cryptococcus neoformans
PublicationW pracy opisano wyniki badań nad rolą struktur zawierających N-acetylo-D-glukozaminę (GlcNAc) w tworzeniu kapsuły otaczającej komórki patogennych dla człowieka grzybów Cryptococcus neoformans. Ekspresja w warunkach in vivo chitooligomerów łączących polisacharydy kapsuły ze ścianą komórkową jest różna, w zależności od rodzaju zainfekowanej tkanki, co określono poprzez wykazanie różnej reaktywności komórek form drożdżowych C. neoformans...
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Kwas mykofenolowy i jego analogi. Synteza i aktywność biologiczna = Mycophenolic acid (MPA) and its analogues. Synthesis and biological activity
PublicationW artykule opisano kwas mykofenolowy (MPA)oraz jego analogi. Kwas MPA został odkryty ponad 100 lat temu i nadal pozostaje atrakcyjnym celem badań biologicznych. Z uwagi na bardzo dużą tendencję do ulegania glukuronidyzacji in vivo, ograniczone są jego możliwości zastosowań jako potencjalnego chemoterapeutyka. Otrzymane dotychczas analogi m.in. zawierające różne cykliczne ugrupowania, monocykliczne fenole i niefenolowe analogi oraz...
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Multi-layered tissue head phantoms for noninvasive optical diagnostics
PublicationExtensive research in the area of optical sensing for medical diagnostics requires development of tissue phantoms with optical properties similar to those of living human tissues. Development and improvement of in vivo optical measurement systems requires the use of stable tissue phantoms with known characteristics, which are mainly used for calibration of such systems and testing their performance over time. Optical and mechanical...
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Imidazoacridinone-dependent lysosomal photodestruction: a pharmacological Trojan horse approach to eradicate multidrug-resistant cancers
PublicationMultidrug resistance (MDR) remains a primary hindrance to curative cancer therapy. Thus, introduction of novel strategies to overcome MDR is of paramount therapeutic significance. Sequestration of chemotherapeutics in lysosomes is an established mechanism of drug resistance. Here, we show that MDR cells display a marked increase in lysosome number. We further demonstrate that imidazoacridinones (IAs), which are cytotoxic fluorochromes,...
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LC-MS/MS dtermination of isoprostanes in plasma samples collected from mice exposed to doxorubicin or tert-butyl hydroperoxide
PublicationIsoprostanes are stable products of arachidonic acid peroxidation and are regarded as the most reliable markers of oxidative stress in vivo. Here we describe the LC-MS/MS procedure enabling simultaneous determination of four regioisomers (8-iso prostaglandin F2α, 8-iso-15(R)-prostaglandin F2α, 11β-prostaglandin F2α, 15(R)-prostaglandin F2α) in plasma samples collected from mice. The four plasma isoprostanes are determined by LC–ESI-MS/MS...
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Noise in biological Raman spectroscopy
PublicationRaman spectroscopy is a widely used method to investigate chemical molecules by analyzing their vibrational transitions. It utilizes inelastic scattering of the laser light irradiating the investigated object. The scattered light requires appropriate filtering to reduce dominant laser light and expose much weaker components having shifted wavelengths of a characteristic spectral pattern. These components are measured by dispersing...
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A highly thermostable, homodimeric single-stranded DNA-binding protein from Deinococcus radiopugnans
PublicationWe report the identification and characterization of the single-stranded DNA-binding protein (SSB) from the mesophile and highly radiation-resistant Deinococcus radiopugnans (DrpSSB). PCR-derived DNA fragment containing the complete structural gene for DrpSSB protein was cloned and expressed in Escherichia coli. The gene consisting of an open reading frame of 900 nucleotides encodes a protein of 300 amino acids with a calculated...
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Functionalized Peptide Fibrils as a Scaffold for Active Substances in Wound Healing
PublicationTechnological developments in the field of biologically active peptide applications in medicine have increased the need for new methods for peptide delivery. The disadvantage of peptides as drugs is their low biological stability. Recently, great attention has been paid to self-assembling peptides that can form fibrils. Such a formulation makes bioactive peptides more resistant to enzymatic degradation and druggable. Peptide fibrils...
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Synthesis of green benzamide-decorated UiO-66-NH2 for biomedical applications
PublicationMetal-organic frameworks (MOFs) biocompatible systems can host enzymes/bacteria/viruses. Herein we synthesized a series of fatty acid amide hydrolase (FAAH)-decorated UiO-66-NH2 based on Citrus tangerine leaf extract for drug delivery and biosensor applications. Five chemically manipulated FAAH-like benzamides were localized on the UiO-66-NH2 surface with physical interactions. Comprehensive cellular and molecular analyses were...
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Is mesh fixation necessary in laparoendoscopic techniques for M3 inguinal defects? An experimental study.
Publicationrepairs, in case of large direct hernias (M3) mesh fixation is recommended to reduce recurrence risk. Despite lack of highquality evidence, the recommendation was upgraded to strong by expert panel. The authors conducted a research experiment to verify the hypothesis that it is possible to preserve the mesh in the operating field in large direct hernias (M3) without the need to use fixing materials. Method The authors conducted...
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Keratin-Butyrate Scaffolds Promote Skin Wound Healing in Diabetic Rats Through Down-Regulation of IL-1β and Up-Regulation of Keratins 16 and 17
PublicationImpaired wound healing particularly in diabetics creates a significant healthcare burden. The study aimed to evaluate the effect of keratin-butyrate fibers (FKDP +0.1%NaBu) in a full-thickness skin wound model in 30 diabetic rats. Physicochemical examination showed that the obtained dressing possesses a heterogeneous structure and butyrate was slowly released into the wound. Moreover, the obtained dressing is nontoxic and supports...
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Cu-HKUST-1 and Hydroxyapatite–The Interface of Two Worlds toward the Design of Functional Materials Dedicated to Bone Tissue Regeneration
PublicationA novel composite based on biocompatible hydroxyapatite (HA) nanoparticles and Cu-HKUST-1 (Cu-HKUST-1@HA) has been prepared following a layer-by-layer strategy. Cu-HKUST-1 was carefully selected from a group of four Cu-based metal−organic frameworks as the material with the most promising antimicrobial activity. The formation of a colloidal Cu- HKUST-1 layer on HA nanoparticles was confirmed by various techniques, e.g., infrared...
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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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Synthesis, molecular structure, and metabolic stability of new series of N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1 H -pyrazol-1-yl)amidine as potential anti-cancer agents
PublicationA series of new N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1H-pyrazol-1-yl)amidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The studied compounds display selective activity mainly against HCT-116 and HeLa cells. Thus, five compounds show selective cytotoxic...
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Antibacterial Activity and Cytocompatibility of Bone Cement Enriched with Antibiotic, Nanosilver, and Nanocopper for Bone Regeneration
PublicationBacterial infections due to bone replacement surgeries require modifications of bone cement with antibacterial components. This study aimed to investigate whether the incorporation of gentamicin or nanometals into bone cement may reduce and to what extent bacterial growth without the loss of overall cytocompatibility and adverse effects in vitro. The bone cement Cemex was used as the base material, modified either with gentamicin...
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Novel fused pyran derivatives induce apoptosis and target cell cycle progression in anticancer efficacy against multiple cell lines.
PublicationNitrogen-based heterocycles such as pyrazole, imidazole, 1,2,4-triazole, benzimidazole, and benzotriazole substituted fused pyran derivatives (6a–e, 8a–e, 10a–e, 12a–e,&14a–e) have been synthesized and tested for their in vitro anticancer efficacies against MCF7, A549, and HCT116 cancer cell lines. Among the compounds, 6e, 14b, and 8c were identified as the most potent against MCF7, A549, and HCT116, with IC50 values of 12.46 2.72...
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Biocompatibility and potential functionality of lanthanum-substituted cobalt ferrite spinels
PublicationBulk and nanostructurized lanthanum-cobalt spinels have attracted a lot of interest from researchers, due to their unique physical and chemical properties as well as functionalities, which are interesting for biomedical and electronic industries. In this manuscript we show that introducing small lanthanum (La3+) content can tune magnetic, electronic and cytotoxic properties of the CoFe2− xLaxO4 system (x ≤ 0.1). The mechanisms...
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Analiza przydatności wybranych systemów transmisji danych w systemie RSMAD
PublicationW pracy dokonano analizy przydatności wybranych systemów radiokomunikacyjnych, aktualnie wykorzystywanych lub możliwych do wykorzystania w przyszłości, do transmisji danych w Radiowym Systemie Monitorowania i Akwizycji Danych z Urządzeń Fotoradarowych (RSMAD). Przedstawiono wady i zalety każdego z systemów, zwracając szczególną uwagę na cechy, które w sposób bezpośredni decydują o przydatności danego rozwiązania w systemie RSMAD....
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Mechanisms positioned in a neighbourhood of their singular positions - velocity amplification in the electromagnetic damping. Part 2. Numerical Verification
PublicationPraca prezentuje zagadnienia występujące podczas elektromagnetycznego tłumienia drgań układów mechanicznych. Analizowano zachowania układu ciągłego i jego drgania. Aby przyśpieszyć tłumienie, wprowadzono specjalny dwuramienny mechanizm umieszczony pomiędzy elementem drgającym i elementem tłumiącym drgania. Mechanizm ustawiony jest w pobliżu swojego ustawienia osobliwego. Aby określić potencjalny kierunek zmian prowadzący do poprawić...
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Zastosowanie bajtowo adresowanej pamięci NVRAM do zwiększenia wydajności wybranych aplikacji równoległych wykorzystujących MPI I/O
PublicationObecnie wiele badań podejmuje temat rosnącego problemu wydajności operacji na plikach w środowiskach klastrowych. Jednocześnie, według ostatnich doniesień związanych z rozwojem technologii pamięci komputerowych, w najbliższej przyszłości na rynku powinny pojawić się układy trwałej pamięci o dostępie swobodnym, adresowanej bajtowo. Niniejsza rozprawa pokazuje, że przy użyciu takiej pamięci można zwiększyć wydajność wybranych...
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Optymalizacja doboru prawa konstytutywnego membrany o strukturze plecionej
PublicationCelem niniejszej dysertacji jest opracowanie zagadnienia optymalizacyjnego pozwalającego dobrać model konstytutywny opisujący mechaniczne zachowanie membrany technicznej. Do analizy wybrano membrany plecione, stosowane w medycynie, tzw. siatki chirurgiczne. W celu wykonania identyfikacji praw konstytutywnych, wykonano dwuosiowe rozciąganie próbek materiałów, otrzymując wskazanie na nieliniowe anizotropowe zachowanie materiałów....
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Image Classification Based on Video Segments
PublicationIn the dissertation a new method for improving the quality of classifications of images in video streams has been proposed and analyzed. In multiple fields concerning such a classification, the proposed algorithms focus on the analysis of single frames. This class of algorithms has been named OFA (One Frame Analyzed).In the dissertation, small segments of the video are considered and each image is analyzed in the context of its...
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A comparative analysis of phenotypic and genotypic methods for the determination of the biofilm-forming abilities of Staphylococcus epidermidis
PublicationThe collection of 146 Staphylococcus epidermidis strains isolated from the nasopharynx of lung cancer patients has been studied for the ability of slime secretion and biofilm formation using the Congo red agar (CRA) test and the microtiter plate (MtP) method, respectively. The prevalence of the icaAD and the aap genes was also analyzed. Some isolates (35.6%) were biofilm positive by the MtP method, while 58.9% of isolates exhibited...
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Novel N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives: synthesis and anticancer activity evaluation
PublicationA new series of N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives 4-21 have been synthesized, and evaluated at the National Cancer Institute (USA) for their in vitro activities against a panel of 60 different human cancer cell lines. Among them, compounds 16, 20 and 21 exhibited remarkable cytotoxic activity against numerous human cancer cell lines. We found that sulfonamide derivative 21 appeared to be more selective...
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Detoxification of the tricyclic antidepressant opipramol and its analog – IS-noh by UGT enzymes before and after activation by phase I enzymes in rat liver microsomes
PublicationThe present studies were carried out to evaluate the simultaneous one-pot metabolism of opipramol (IS-opi) and analog (IS-noh) by phase I and phase II enzymes present in rat liver microsomes (RLM) as an alternative to separate testing with recombinant enzymes. This approach allows for more time-saving and cost-effective screening of the metabolism of newly discovered drugs. We also considered that the lack of results for phase...
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DNA methylation as a mediator of HLA-DRB1*15:01 and a protective variant in multiple sclerosis
PublicationThe human leukocyte antigen (HLA) haplotype DRB1*15:01 is the major risk factor for multiple sclerosis (MS). Here, we find that DRB1*15:01 is hypomethylated and predominantly expressed in monocytes among carriers of DRB1*15:01. A differentially methylated region (DMR) encompassing HLA-DRB1 exon 2 is particularly affected and displays methylation-sensitive regulatory properties in vitro. Causal inference and Mendelian randomization...