Дисертації з теми "Biological Active Molecules"
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Strawbridge, Sharon Mary. "Redox-active sensors for molecules of biological interest." Thesis, University of Exeter, 2004. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.414263.
Повний текст джерелаLu, Biao. "Evaluation of physico-chemical properties of biorefinery-derived amphiphilic molecules and their effects on multi-scale biological models." Thesis, Compiègne, 2015. http://www.theses.fr/2015COMP2218/document.
Повний текст джерелаNowadays, a wide variety of new molecules can derive from biomass. Among them, the family of sugar-based surfactants, which are considered as alternatives to fossil-based surfactants, due to their relatively high biodegradability and biocompatibility, exhibit interesting properties both in terms of their self-assembly and their ability to induce biological responses. In the study, for the purpose to analyse these properties, different methodologies have been established. In this work, physico-chemistry and cellular biology methodologies are associated to analyse the properties of pre-selected molecules characterized by gradua) structure modifications. Firstly, we have screened synthesized sugar-based surfactants according to their solubility and their ability to reduce surface tension of water. Four pre-selected molecules, with a C8 chain linked to a glucose or maltose head through an amide functional group, either under the form of carbamoyl (carbohydrate scaffold bearing the carbonyl) or alkylcarboxamide (the alkyl chain bearing the carbonyl), were then dissolved in water/ cell culture media for surface tension measurements. Their behaviors in solutions were characterized by Krafft points, Critical Micellar Concentrations or self-assembling properties through different methods. To evaluate the cytotoxic/ irritant effects of these molecules on cells and tissues, 3 in-vitro models were established: I) 2D cell culture mode! (L929 cell monolayer) II) 3D ce!! culture mode! (L929 cells embedded in collagen gel) and III) Reconstituted human epidermis (differentiated human keratinocytes). Corresponding experiments were carried out on these models with increasing complexity. Results show that the synthesized sugar-based surfactants, GlulamideC8, Glu6amideC8, Glu6amideC8' and MallamideC8 can reduce the surface tension of water solution to the came level as standard surfactants (Tween 20 and Hecameg). In the meantime, GlulamideC8, Glu6amideC8' and MallamideC8 present Iess cytotoxicity effects on L929 cells both in the monolayer model and the 3D mode! than Tween 20 and Hecameg. All synthesized and standard surfactants (GlulamideC8, Glu6amideC8, Gu6amideC8', MallamideC8, Tween 20 and Hecameg) have no significant cytotoxic/ irritant effects on reconstituted human epidermis at 1000 ig/mL after 48 h of topical application. Discussions have been made according to the results of experiments to establish possible structures/ physico-chemical properties - cytotoxicity relationships of these surfactants
Shortt, Marie Fiona. "Synthetic approaches to biologically active molecules." Thesis, Bangor University, 1994. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.282267.
Повний текст джерелаFinn, P. W. "Computer studies on biologically active molecules." Thesis, University of Manchester, 1985. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.374793.
Повний текст джерелаd'Ippolito, Giuliana. "Biologically active molecules from marine microalgae." Thesis, Open University, 2005. http://oro.open.ac.uk/54203/.
Повний текст джерелаTunbridge, Gemma Ann. "Efficient synthesis of biologically active small molecules." Thesis, University of Bath, 2012. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.571862.
Повний текст джерелаGutierrez, Mauricio R. (Mauricio Roberto). "Size adjustable separation of biologically active molecules." Thesis, Massachusetts Institute of Technology, 2004. http://hdl.handle.net/1721.1/34150.
Повний текст джерелаIncludes bibliographical references (p. 92-96).
Separation of biologically active molecules (BAM's) is a problem for the pharmaceutical and biotechnology industries. Current technologies addressing this problem require too many techniques, toxic additives, and time to filter desired materials. As a result, a new technology is needed. The objective of this thesis is to contribute towards the development of a new method for separating biologically active molecules in the size range of 0.5 nanometers to 500 nanometers. A normally open diaphragm valve is proposed that can control a gap formed by two flat surfaces. For accurate control of gap height, the valve was designed to ensure that the flat surfaces remain parallel during operation . Modularity was also part of design considerations to address issues of eventual biocompatibility breakdown specifically protein adsorption. Control of the gap has been achieved to increments of 1.8 nanometers.
by Mauricio R. Gutierrez.
S.M.
Perez-Powell, Isabel Rose. "From fragments of prostanoids to biologically active molecules." Thesis, University of Bristol, 2016. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.707737.
Повний текст джерелаJiang, Xiaohui. "Computational and NMR studies of biologically active molecules /." Diss., Connect to a 24 p. preview or request complete full text in PDF format. Access restricted to UC campuses, 1998. http://wwwlib.umi.com/cr/ucsd/fullcit?p9906482.
Повний текст джерелаMuller, Christophe. "The synthesis of biologically active molecules using organocobalt complexes." Thesis, Kingston University, 1997. http://eprints.kingston.ac.uk/20608/.
Повний текст джерелаGiacomini, Elisa <1983>. "Innovative Strategies for the Synthesis of Biologically Active Small Molecules." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2013. http://amsdottorato.unibo.it/5537/.
Повний текст джерелаIanni, Cristina <1980>. "Synthesis of Biologically Active Small Molecules: Different Approaches to Drug Design." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2014. http://amsdottorato.unibo.it/6403/.
Повний текст джерелаPaula, Da Cunha Denise. "Application of MOFs in adsorption and release of biologically active molecules." Versailles-St Quentin en Yvelines, 2012. http://www.theses.fr/2012VERS0050.
Повний текст джерелаThe last class of porous materials, organic-inorganic hybrid solids crystalline also commonly called Metal-Organic Frameworks (MOFs) has many advantages for biomedical applications, such as large pore sizes, biodegradability and properties of medical imaging. However, it was proposed to evaluate the cytotoxicity of MOFs with different composition and structure in two different cell lines. We found that MOFs present no or very low cytotoxicity and that depends on the cell line, metal and particle size. Regarding MOFs as controlled drugs release systems, we perfomed a systematic study of the encapsulation and release of model compounds such as caffeine (cosmetics), from a series of MOFs with low toxicity, compositions and topologies different. Results showed that encapsulation and kinetics release of caffeine can be modulated by changing the composition and structure of MOFs. The last approach of this work consisted in forming patches consisting of organic-inorganic hybrid mixtures with the MIL-100 loaded with caffeine and biocompatible polymers for transdermal drug delivery. In vitro release studies showed that the hybrid patches are more effective for slow release caffeine. Studies ex vitro carried out in Ussing chamber showed a greater absorption of caffeine on the skin patch and Gel-CAF somewhat similar in the case of MIL-100-CAF-Gel compared with commercial cream caffeine
Gutowski, Mariusz. "Molecular detection and characterisation of biologically relevant free radicals during surgical ischaemia-reperfusion." Thesis, University of South Wales, 2011. https://pure.southwales.ac.uk/en/studentthesis/molecular-detection-and-charcaterisation-of-biologically-relevant-free-radicals-during-surgical-ischaemiareperfusion(016f6447-5d02-45f7-a543-8b880148dc23).html.
Повний текст джерелаThe I-R has got a major influence on the muscle oxygenation to increased ROS and the return of values towards baseline period in reperfusion stage appears to coincide with increased oxidative stress. Using the state-of-the-art molecular techniques that include Electron Paramagnetic Spectroscopy (EPR) for the direct detection of free radicals and Near Infrared Spectroscopy (NIRS) for the direct detection of muscle oxygenation these studies have attempted to translate the basic mechanisms associated with free radical formation during I-R and have provided unique insight into the basic mechanisms responsible for the oxidative stress with the ultimate objective of developing novel antioxidant interventions that can provide effective prophylaxis.
Fitzsimmons, C. M. "Biologically active domains in collagen important in its haemostatic function." Thesis, University of Cambridge, 1987. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.377902.
Повний текст джерелаDickinson, Niall. "The application of iminium ions to the synthesis of biologically active molecules." Thesis, University of Southampton, 2013. https://eprints.soton.ac.uk/354554/.
Повний текст джерелаZaki, Afroditi Maria. "Molecular dynamics study of biomembrane interactions with biologically active polymers." Thesis, University of Manchester, 2018. https://www.research.manchester.ac.uk/portal/en/theses/molecular-dynamics-study-of-biomembrane-interactions-with-biologically-active-polymers(0e61623d-d73c-4f84-a1ef-6698026c4aa2).html.
Повний текст джерелаDavidson, Louise. "Synthesis and evaluation of solid supported receptors for biologically active steroids." Thesis, University of Reading, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.250678.
Повний текст джерелаAleksandra, Cvetanović. "Оптимизација савремених екстракционих поступака за изоловање апигенина из цвета камилице (Chamomilla recutita L.) и карактеризација биолошке активности добијених екстраката". Phd thesis, Univerzitet u Novom Sadu, Tehnološki fakultet Novi Sad, 2016. http://www.cris.uns.ac.rs/record.jsf?recordId=101724&source=NDLTD&language=en.
Повний текст джерелаU okviru ove doktorske disertacije izvedeno jeispitivanje različitih ekstrakcionih postupaka zaizolovanje apigenina iz cveta kamilice, kao i evaluacijabiološke aktivnosti dobijenih ekstrakata. Polaznibiljni materijal sačinjavale su dve grupe laticakamilice: fermentisane i nefermentisane (nativne).Ekstrakcija fermentisanih cvetova je izvođena primenomultrazvučne ekstrakcije koristeći etanol kao ekstragens,a dobijeni ekstrakti su se odlikovali izuzetno visokimsadržajem apigenina. Optimizacija ekstrakcije je bilaizvedena primenom metode odzivne površine. Primenomelektron-spin rezonance ispitana je antiradikalskaaktivnost ekstrakata. Dodatno, farmakološka vrednostdobijenih ekstrakata je potvrđena i određivanjem njihovogantimikrobnog i antiproliferativnog potencijala.Nativni cvetovi kamilice su ekstrahovani primenomrazličitih ekstarkcionih tehnika: mikrotalasne,ultrazvučne, Soxhlet ekstrakcije kao i ekstrakcijesubkritičnom vodom. Ekstrakcija vodom u subkritičnomstanju se pokazala superiornijom u odnosu na sve ostaletehnike u pogledu sadržaja ukupnih fenola i flavonoida.U cilju dobijanja ekstrakata sa maksimalnim sadržajemapigenina izvedena je optimizacija ovog ekstrakcionogprocesa. Izolovanje čistog apigenina je izvedeno izekstrakta dobijenog pod optimalnim ekstrakcijomuslovima (odnos droga:rastvarač 1:30, brzina mešanja 3 Hz,pritisak 45 bar, temperatura 115ºC, vreme 30 min,koncentracija modifikatora 0,001 M) primenom postupkakolonske hromatografije na stubu poliamida. Hemijskiprofil kao i sadržaj pojedinačnih polifenolnihkomponenata u ekstraktima dobijenim na različitimpritiscima, temperaturama i uz prisustvo modifikatorarazličitih koncentracija određen je primenom UHPLCDAD-HESI-MS/MS. U svim analiziranim ekstraktimadetektovan je veliki broj polifenolnih komponenata, dokje apigenin u svima bio dominantno jedinjenje. Sadržajapigenina u ekstraktu dobijenom pod optimalnimekstrakcionim uslovima je iznosio 1.700,34 mg/kg.Primenom sedam različitih testova izvršena jeevaluacija antioksidativnog i antiradikalskogpotencijala ekstrakata. Antimikrobni potencijalekstrakata je određen za osam različitih mikrobnihlinija. in vitro testovima ispitana je sposobnostinhibicije α-amilaze, α-glukozidaze i tirozinaze.Delovanjem na rast tri histološki različite ćelijskelinije, ispitana je antiproliferativna aktivnostekstrakata dobijenih subkritičnom vodom.Antimotilitetna aktivnost obe grupe ekstrakata(fermentisanih i nefermentisanih cvetova) određena je uin vitro uslovima.
In the frame of this thesis different extraction approaches forapigenin isolation from chamomile ligulate flowers wereexamined and biological activity of obtained extracts wasevaluated. Starting plant samples included fermented andnonfermented (native) flowers.Extraction of fermented flowers was performed by usingultrasound-assisted extraction with ethanol. The concentrationof apigenin was high in obtained extracts. Optimization of theextraction procedures was performed by response surfacemethodology. Antiradical activity of observed extracts wasexamined by electron-spin resonance spectroscopy.Furthermore, pharmacological potential of obtained extractswas confirmed by determining their antimicrobial andantiproliferative activity.Native chamomile flowers were extracted by differentextraction techniques: microwave, ultrasound, Soxhlet andsubcritical water extraction. Subcritical water extractionshowed to be superior in comparison to other applied techniquesin respect to total phenols and flavonoids content. Optimizationof the subcritical water extraction was directed to maximizationof apigenin content. Isolation of pure apigenin from extractsobtained under optimal extraction conditions (sample-tosolventratio 1:30, agitation rate 3 Hz, temperature 115ºC,pressure 45 bar, extraction time 30 min) was performed bypreparative chromatography. Chemical profiles and content ofindividual polyphenolic components in extracts obtained atdifferent pressures, temperatures, and with differentconcentrations of a modifier was determined by UHPLC-DADHESI-MS/MS. In all analyzed extracts the great number ofpolyphenolic components was detected while apigenin was thedominant compound in all extracts. Content of apigenin in theextract obtained under optimal extraction condition was1,700.34 mg/kg. Antioxidant and antiradical potential ofextracts was evaluated according to different mechanisms.Antimicrobial potential of extracts was determined against eightdifferent microbial strains. Ability of extracts to inhibit α-amylase, α-glucosidase and tyrosinase was determined by invitro assays. Antiproliferative activity of subcritical waterextracts was defined by testing their influence on the growth ofthree histologically different cell lines.Anti-intestinal motility activity of both group of extracts (nativeand fermented) was determined by in vivo experiments.
Donaldson, Lauren Rona. "New methods for the synthesis of biologically active phenanthridine-based libraries." Thesis, University of Edinburgh, 2009. http://hdl.handle.net/1842/5736.
Повний текст джерелаSpáčil, Zdeněk. "Mass Spectrometry of Biologically Active Small Molecules : Focusing on polyphenols, alkaloids and amino acids." Doctoral thesis, Stockholms universitet, Institutionen för analytisk kemi, 2010. http://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-33233.
Повний текст джерелаAt the time of the doctoral defense, the following papers were unpublished and had a status as follows: Paper 4: In press. Paper 5: Manuscript.
Patel, Pratiq A. "Functionalization of Nitrogen-Containing Heterocycles in the Synthesis of Biologically Active Molecules." The Ohio State University, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=osu1382064973.
Повний текст джерелаSpáčil, Zdeněk. "Mass spectrometry of biologically active small molecules focusing on polyphenols, alkaloids and amino acids /." Stockholm : Department of analytical chemistry, Stockholm University, 2010. http://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-33233.
Повний текст джерелаAt the time of the doctoral defense, the following papers were unpublished and had a status as follows: Paper 4: In press. Paper 5: Manuscript. Härtill 5 uppsatser.
Orlando, Michele. "Modification of proteins and low molecular weight substances with hydroxyethyl starch (HES) HESylation - a new technology for polymer conjugation to biologically active molecules /." [S.l.] : [s.n.], 2003. http://deposit.ddb.de/cgi-bin/dokserv?idn=96981545X.
Повний текст джерелаHill, David Brooks. "Changes in the number of molecular motors driving vesicle transport in PC12 /." Electronic thesis, 2003. http://dspace.zsr.wfu.edu/jspui/handle/10339/206.
Повний текст джерелаAlli, Zaman. "Expression of biologically active human granulocyte macrophage colony stimulating factor in the seeds of transgenic tobacco." Thesis, University of Ottawa (Canada), 2001. http://hdl.handle.net/10393/9046.
Повний текст джерелаRandhawa, Sukanya. "Active control of surface plasmons in hybrid nanostructures." Doctoral thesis, Universitat Politècnica de Catalunya, 2012. http://hdl.handle.net/10803/124095.
Повний текст джерелаLas nanoestructuras plasmónicas han adquirido una importante relevancia como herramientas capaces de manipular los fotones en la nanoescala, y pueden llegar a revolucionar un amplio abanico de aplicaciones tales como los circuitos ópticos integrados, la fotovoltaica o los dispositivos biosensores. Dichas estructuras hacen posible la miniaturización de los componentes ópticos más allá del “límite de difracción” de la luz, ya que convierten la radiación óptica en campos electromagnéticos fuertemente confinados en la proximidad de estructuras metálicas de tamaño inferior a la longitud de onda mediante la excitación de plasmones de superficie (SPs). Estos campos electromagnéticos tan intensos generados en los llamados “puntos calientes” plasmónicos brindan perspectivas muy interesantes para la generación de efectos no lineales en medios activos. El área de investigación denominado plasmónica activa busca la modulación de los SPs sostenidos por la intercara entre un metal y un material no lineal mediante una señal de control externa. El índice de refracción del material no lineal cambia bajo la aplicación de la señal de control, lo cual da lugar a la modificación de la respuesta plasmónica. Estas nanoestructuras híbridas también hacen posible la aparición de nuevos tipos de estados híbridos, lo cual proporciona tanto herramientas para diseñar dispositivos plasmónicos activos como mecanismos que permiten re-examinar las reglas convencionales de la interacción luz materia. Por lo tanto, es necesario el estudio de dichas nanoestructuras plasmónicas híbridas de manera teórica y experimental. En este trabajo de tesis se analiza el control de los SPs excitados en sistemas híbridos que combinan materiales activos y nanoestructuras metálicas mediante una señal óptica externa o un voltaje aplicado. Se han investigado distintos tipos de geometrías plasmónicas utilizando herramientas de simulación basadas en métodos en el dominio de la frecuencia, y posteriormente se han caracterizado experimentalmente dichas geometrías mediante técnicas de campo cercano y de campo lejano tales como la microscopía óptica de campo cercano y la microscopía basada en pérdidas radiativas, respectivamente. En primer lugar se estudiaron elementos plasmónicos pasivos, en particular espejos plasmónicos dieléctricos que demuestran la capacidad que tienen las redes periódicas de caballones de material dieléctrico colocados sobre una superficie metálica plana para abrir intervalos prohibidos en la relación de dispersión de los plasmones de superficie propagantes o plasmones-polaritones de superficie (SPPs). Los resultados muestran que dichos espejos poseen muy buenas propiedades reflectantes para SPPs cuya energía está en el intervalo prohibido. Otra configuración pasiva analizada fueron los resonadores plasmónicos basados en anillos de guía de onda plasmónica fabricada a partir de estructuras dieléctricas sobre metal (WRR, del inglés waveguide ring resonator ). Asimismo, se propone una versión más robusta de resonador plasmónico, basada en la sustitución del anillo del WRR por un disco (WDR, del inglés waveguide disk resonator). Se ha evaluado el funcionamiento de los WDRs en términos de selectividad en longitud de onda y de eficiencia, y los resultados obtenidos presentan un buen acuerdo con las predicciones numéricas. Pasando a las configuraciones activas, se demuestra el control de la señal plasmónica en configuración WRR por medios tanto electro-ópticos como completamente ópticos. En el caso del control electro-óptico, el material dieléctrico que compone el WRR estaba dopado con un componente electro-óptico y a la estructura pasiva se le añadió un conjunto de electrodos planos. Bajo la aplicación de un campo eléctrico externo, se midió un cambio relativo en la transmisión a través de la guía plasmónica del 16%. En cuanto al control puramente óptico, se utilizó la no linealidad de un material polimérico con origen en una isomerización trans-cis. En este caso se detectó un factor 3 entre los estados de alta y baja transmisión del dispositivo con potencias de control del orden de milivatios (intensidad del haz óptico de control de unos 100W/cm2 aproximadamente). Además del control activo de los plasmones de superficie propagantes, la utilización de nanoestructuras plasmónicas que poseen resonancias plasmónicas localizadas puede dar lugar a nuevos fenómenos. En esta tesis también se han estudiado las interacciones entre las excitaciones moleculares en un polímero pi-congujado con las polarizaciones plasmónicas en nanocavidades plasmónicas híbridas. Utilizando espectroscopia de tipo bombeo-sonda con pulsos ultrarrápidos, se han analizado diversos aspectos del aumento en la interacción luz-materia para estructuras híbridas de dimensiones inferiores a la longitud de onda sometidas a concentraciones de luz muy altas. Por último, esta tesis también proporciona una visión general de los desafíos y posibilidades que las funcionalidades plasmónicas híbridas ofrecen en el campo de la nano-óptica basada en plasmones de superfície.
Yam, Noymi. "Molecular interactions of biologically active derivatives of sulfamide with pharmaceutical polymers in solid state." Scholarly Commons, 2009. https://scholarlycommons.pacific.edu/uop_etds/2398.
Повний текст джерелаYamamura, Ei-tora. "Biochemical and molecular biological studies on enzymatic synthesis of vitamin B6 derivatives and optically active carboxylic acids." Kyoto University, 2020. http://hdl.handle.net/2433/245820.
Повний текст джерела0048
新制・論文博士
博士(農学)
乙第13305号
論農博第2880号
新制||農||1074(附属図書館)
学位論文||R2||N5242(農学部図書室)
富山大学大学院理工学研究科生命環境科学専攻
(主査)教授 小川 順, 教授 阪井 康能, 教授 栗原 達夫
学位規則第4条第2項該当
Ng, Sean. "Regioselective copper(I)-NHC-catalysed allylic oxidation reactions : application towards the total syntheses of biologically active molecules." Thesis, University of Liverpool, 2011. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.577144.
Повний текст джерелаMerrifield, Jonathan David. "Development of novel sensors for biologically active molecules based on the selective modification of supported phospholipid monolayers." Thesis, University of Leeds, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.446053.
Повний текст джерелаTiao, Jim Yu-Hsiang. "The neuregulin-3 intracellular domain is biologically active : molecular and functional characterisation of protein interactions." University of Western Australia. School of Medicine and Pharmacology, 2006. http://theses.library.uwa.edu.au/adt-WU2006.0083.
Повний текст джерелаFriesen, Sergej [Verfasser], and Richard [Akademischer Betreuer] Buchner. "Hydration and Ion Binding of Small Biologically Active Molecules: The Case of Neurotransmitters / Sergej Friesen ; Betreuer: Richard Buchner." Regensburg : Universitätsbibliothek Regensburg, 2020. http://d-nb.info/1203875258/34.
Повний текст джерелаSánchez, Mirna Inés Mosquera. "Interação de moléculas biologicamente ativas com filmes de Langmuir de fosfolipídios." Universidade de São Paulo, 2000. http://www.teses.usp.br/teses/disponiveis/76/76132/tde-08112013-102613/.
Повний текст джерелаThe interaction of various bioactive substances with phospholipids monolayers has been investigated using surface pressure and surface potential isotherms, which include the pharmaceutical drugs dipyridamole (DIP), chlorpromazine (CPZ) and trifluoperazine (TFP), in addition to melatonin (MEL) and cholesterol (COL). The phospholipids employed were the zwitterionic dipalmitoyl phosphatidyl choline (DPPC) and the anionic dipalmitoyl phosphatidyl glycerol (DPPG) spread onto ultra pure water surfaces, where the monolayers served as simple model membrane systems. Cooperativity in the interaction between phospholipid and bioactive molecules was essential to account for the large effects of expansion (up to 10% increase in area in relation to the pure phospholipid monolayer for the DIP/DPPC mixture) of the monolayers and changes in dipole moment, which occurred at very low concentrations, e.g. 0.2 - 0.4 mol% of the substance. Such large effects were observed for all 5 substances investigated, at all surface pressure regimes. At higher concentrations, the interaction behavior depended on the type of molecule and also on whether the host monolayer was DPPC or DPPG. For DPPC, the pharmaceutical drugs were expelled at varying degrees from the interface at high surface pressures, and there was a maximum drug concentration above which the effects saturated, probably because the molecules in excess were lost to the subphase. These critical concentrations were 2mol% for DIP and CPZ and 5mol% for TFP. For DIP, in particular, the results from isotherm were correlated with in situ FTIR spectroscopy and fluorescent microscopy experiments, carried out by collaborators, which allowed the precise location of the drug to be determined. There is no insertion of DIP into the hydrophobic tail region of the DPPC monolayer, with interaction taking place with the phosphate group in the zwitterion, whose small changes in orientation induced by DIP lead to the large changes in dipole moment. Because DPPG is negatively charged on a pure water surface monolayer, there is no saturation of the expansion effects with the increase in drug concentration. The increase in the effective dipole moment of the mixed monolayers are attributed to alterations in the surface charge density by adsorption of the cationic drugs, which then reduces the negative contribution of the double-layer potential as compared to the pure DPPG monolayer. The results for COL and MEL must be considered separately owing to their distinct nature, even though a cooperative behavior was also observed with large effects at low concentrations. Both COL and MEL induce changes in the DPPC monolayers up to the highest concentration employed, viz. 20mol%. For COL, a condensation effect was observed at low concentrations, which was followed by monolayer expansion at high concentrations, thus confirming previous results in the literature. All COL/DPPG monolayers were more expanded than pure DPPG, also confirming previous results from the literature. While the interaction of MEL with DPPC was essentially similar to that of COL, in spite of the fact that MEL does not form stable monolayers on its own, its interaction with DPPG was somewhat peculiar in that the effects it induced saturate at 5mol%. This also differs from the behavior of the pharmaceutical drugs. MEL is neutral over a wide range of pHs, and therefore its interaction with DPPC and DPPG monolayers must occur via dipole interaction. The same applies to COL, and this explains why the behavior of these two substances is different from the drugs (DIP, CPZ and TFP) that are charged on the water surface, in the interaction with DPPC and DPPG.
Tatarski, Miloš. "Molecular mechanism of dBigH1 action." Doctoral thesis, Universitat de Barcelona, 2018. http://hdl.handle.net/10803/663021.
Повний текст джерелаIkeda, Yasunori. "Synthesis and molecular imprinting studies of small analogues of heparan sulfates : preparation and characterization of biologically active oligosaccharides." Paris 12, 2007. http://www.theses.fr/2007PA120052.
Повний текст джерелаWhite, Colin P. "Molecular Microbial Ecology and Operational Evaluation of a Full-scale and Pilot-scale Biologically Active Filter for Drinking Water Treatment." University of Cincinnati / OhioLINK, 2010. http://rave.ohiolink.edu/etdc/view?acc_num=ucin1277154047.
Повний текст джерелаYing, Jinfa. "Studies of biologically active peptides by NMR and molecular dynamics simulations: From structure and dynamics to design and synthesis." Diss., The University of Arizona, 2004. http://hdl.handle.net/10150/280667.
Повний текст джерелаRuiz, Carmona Sergio. "Virtual screening for novel mechanisms of action: applications and methodological developments." Doctoral thesis, Universitat de Barcelona, 2017. http://hdl.handle.net/10803/400297.
Повний текст джерелаLa motivación principal de esta tesis ha sido validar, mejorar y desarrollar nuevos métodos con relación a los disponibles hoy en día en el área del desarrollo de fármacos, para en un futuro poder estudiar dianas que actualmente están fuera de nuestro alcance. Debido a que la productividad de la industria farmacéutica está disminuyendo durante los últimos años, una mejora en los métodos disponibles sería un gran paso adelante. Esta tesis se ha centrado en diferentes métodos computacionales, como el docking o la dinámica molecular. En la primera de las partes, trabajé en el cribado virtual (Virtual Screening) basado en docking. Concretamente, participé en la validación del programa de docking rDock mediante la comparación con dos programas muy usados hoy en día de su capacidad de predecir correctamente el modo de unión de un ligando con su proteína diana y de sus resultados en el cribado virtual de posibles fármacos. En la segunda parte de la tesis, participé en el desarrollo de un método computacional novedoso en el diseño de fármacos que complementase y mejorase los métodos actualmente disponibles. Éste método, bautizado en inglés como “Dynamic Undocking”, consiste en una implementación específica de dinámica molecular mediante la cual somos capaces de detectar si un ligando puede ser activo o inactivo de manera rápida y eficiente. Se validó el método de manera retrospectiva y posteriormente se aplicó en otro proyecto con el objetivo de encontrar nuevos posibles fármacos para una proteína relacionada con cáncer. Gracias a una colaboración con una empresa del Reino Unido, encontramos nuevos ligandos de manera que aumentamos la tasa de éxito con relación a un método estándar en casi 10 veces. Por último, participé en el “D3R Grand Challenge 2015”, un experimento a escala mundial donde los participantes aplicaron diferentes métodos y compararon sus resultados respecto a dos métricas distintas: la predicción del modo de unión y la capacidad de ordenar los ligandos proporcionados por la organización por su afinidad respecto a la proteína diana. En nuestro caso, aplicamos una combinación de docking y “Dynamic Undocking” con unos resultados excelentes.
Enzinger, Monika [Verfasser], and Sabine [Akademischer Betreuer] Amslinger. "Reactivities of biologically active small molecules: Kinetic assessment of electrophilic enones and characterization of a photoactive phosphoantigen probe / Monika Enzinger ; Betreuer: Sabine Amslinger." Regensburg : Universitätsbibliothek Regensburg, 2020. http://d-nb.info/1218299029/34.
Повний текст джерелаTeixeira, Lúcia de Fátima Moreira. "Role and mechanism of action of human immunoregulatory iNKT cells in Leishmania infection: new approaches for vaccination?" Doctoral thesis, Faculdade de Farmácia da Universidade do Porto, 2010. http://hdl.handle.net/10216/63808.
Повний текст джерелаTeixeira, Lúcia de Fátima Moreira. "Role and mechanism of action of human immunoregulatory iNKT cells in Leishmania infection: new approaches for vaccination?" Tese, Faculdade de Farmácia da Universidade do Porto, 2010. http://hdl.handle.net/10216/63808.
Повний текст джерелаBergamini, Fernando Rodrigues Goulart 1988. "Síntese, caracterização, modelagem molecular e ensaios antibacterianos de novos complexos de Ag(I) com ligantes biologicamente ativos." [s.n.], 2013. http://repositorio.unicamp.br/jspui/handle/REPOSIP/249125.
Повний текст джерелаDissertação (mestrado) - Universidade Estadual de Campinas, Instituto de Química
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Resumo: Neste trabalho, são descritas a síntese e a caracterização de três complexos inéditos de prata com os ligantes L-butionina sulfoximina (BSO), ácido 2-tiazolidina carboxílico (2-TC) e ácido 4-tiazolidina carboxílico (4-TC). O complexo de prata com BSO foi caracterizado por um conjunto de análises químicas e espectroscópicas, a saber: análise elementar, análise térmica, espectroscopia na região do infravermelho (IV), espectroscopia Raman, espectroscopia de ressonância magnética no estado sólido de C (C-RMN), estudos por DFT e ensaios biológicos. Os complexos de prata(I) com 2-TC e 4-TC, por sua vez, foram caracterizados por análise elementar, análise térmica, espectroscopia na região do infravermelho (IV), espectroscopia de ressonância magnética no estado sólido de C-RMN e N-RMN, estudos por DFT e ensaios biológicos. O complexo de prata com BSO, [Ag2(BSO)], apresenta uma composição 2:1 metal/ligante, sendo que a coordenação do ligante a um dos átomos de prata ocorre através dos grupamentos amino e carboxilato, enquanto que a coordenação ao segundo átomo de prata ocorre através do nitrogênio da sulfoximina. Os complexos de prata com 2-TC e 4-TC também apresentam proporção 2:1 metal/ligante, com um átomo de prata coordenado através do nitrogênio e o segundo átomo de prata coordenado através do carboxilato. As análises biológicas revelaram que os complexos [Ag2(BSO)], [Ag2(2-TC)] e [Ag2(4-TC)] são efetivos sobre cepas patogênicas Gram-positivas de Staphylococcus aureus, e cepas Gram-negativas de Escherichia coli e Pseudomonas aeruginosa
Abstract: This work deals with the synthesis and characterization of three new silver(I) complexes with the ligands Lbuthionine sulfoximine (BSO), thiazolidine-2 carboxylic acid (2-TC) and thiazolidine-4 carboxylic acid (4-TC). The silver complex with BSO was characterized by elemental and thermal analyses, infrared and Raman spectroscopies, C nuclear magnetic resonance in the solid-state (C-NMR), DFT studies and biological assays. The silver(I) complexes with 2-TC and 4-TC were characterized by elemental and thermal analyses, infrared spectroscopy, C and N nuclear magnetic resonance in the solid-state, DFT studies and biological assays. The silver-BSO complex, [Ag2(BSO)], presents a 2:1 metal/ligand ratio. One of the silver(I) ion was shown to be coordinated through the amine nitrogen atom and the oxygen of carboxylate, while the second ion was shown to be coordinated through the nitrogen atom of the sulfoximine group. The silver(I) complexes with 2-TC and 4-TC also presented a 2:1 metal/ligand ratio, and are coordinated by the nitrogen and the oxygen atom of the carboxylate group. The biological assays revealed that the [Ag2(BSO)], [Ag2(2-TC)] and [Ag2(4-TC)] complexes are active against Gram-positive pathogenic strains of Staphylococcus aureus and Gramnegative pathogenic strains of Escherichia coli and Pseudomonas aeruginosa
Mestrado
Quimica Inorganica
Mestre em Química
Matkar, Smita S. "Mechanism of action of potential anticancer drugs." Scholarly Commons, 2008. https://scholarlycommons.pacific.edu/uop_etds/2368.
Повний текст джерелаGonzález, Abuín Noemí. "Modulation of active glucagon-like peptide-1 (glp-1) levels by grape-seed procyanidins." Doctoral thesis, Universitat Rovira i Virgili, 2013. http://hdl.handle.net/10803/128942.
Повний текст джерелаSans, i. Duran Cristina. "Millora de soques i estudi d’estratègies de procés per a la producció de Fuculosa-1-fosfat aldolasa recombinant activa en Escherichia coli." Doctoral thesis, Universitat Autònoma de Barcelona, 2011. http://hdl.handle.net/10803/84008.
Повний текст джерелаQuesada, Vázquez Helena. "Dietary proanthocyanidins: their effectiveness in dyslipidemic nutritional models and the role of liver and intestine in their hypotriglyceridemic action." Doctoral thesis, Universitat Rovira i Virgili, 2010. http://hdl.handle.net/10803/8689.
Повний текст джерелаProanthocyanidins have been shown to exert advantageous actions on several metabolic disorders that are risk factors of cardiovascular diseases. Lipoprotein metabolism plays an important role in altered lipid states. Therefore, the aims of this Thesis were: To assess the contribution of the liver and the intestine in the hypolipidemic response triggered by proanthocyanidins and to evaluate the short-term effect of an oral intake of proanthocyanidins in dyslipidemic nutritional models. For these purposes, three experimental models have been used: Rats, mice and human Caco2 cells. The obtained results are: In a fat tolerance test, both chylomicrons and VLDL contribute to the hypotriglyceridemic action of proanthocyanidins but their influence depends on time. Moreover, proanthocyanidins repress TG secretion by the liver in vivo and by the intestine in vitro. Furthermore, ACSL manifests as their target gene in intestinal cells. Finally, proanthocyanidins correct dyslipidemia but not the weight gain induced by diet though these have a bimodal effect on energy retention in vivo.
Murakami, Mario Tyago. "Estratégias de inibição, mecanismos moleculares e interações intermoleculares em complexos macromoleculares /." São José do Rio Preto : [s.n.], 2006. http://hdl.handle.net/11449/100483.
Повний текст джерелаBanca: Antônio Carlos Martins Camargo
Banca: Nilson Ivo Tonin Zanchin
Banca: Beatriz Gómez Guimarães
Banca: Roberto da Silva
Abstract: This work presents some features of essential biological processes such as the haemostatic system, integrity of biological membranes and thermostability of proteins. Crystallographic, spectroscopic and in silico tools have been used to obtain information at the molecular level of macromolecular complexes, action mechanisms and inhibition pathways. Worms, snakes, ticks, leeches and spiders produce a variety of proteins, which interfere in the regulation of these systems. Different toxins isolated from these organisms were characterized providing necessary information for the development of a new anti-myonecrotic molecule and reveal a new factor Xa exosite that is important for macromolecular substrates recognition and inhibition. The first crystal structure of a member of the sphingomyelinases D family was determined by the "quick cryo-soaking" technique and the catalytic mechanism was proposed, which involves a magnesium-binding site and two catalytic histidines. An alternative activation of the protein C pathway that does not require thrombomodulin was structurally characterized and revealed the dual role of the elestrotatic surface charge around the active site and the three strategically positioned carbohydrate moieties in the approach, recognition and activation of protein C.
Doutor
Salazar, Montoya Vivian Angélica. "Exploring the mechanism of action of human antimicrobial ribonucleases." Doctoral thesis, Universitat Autònoma de Barcelona, 2015. http://hdl.handle.net/10803/310611.
Повний текст джерелаHuman ribonucleases are a heterogeneous group of proteins belonging to the superfamily of RNase A. These proteins are characterized by their ability to hydrolyse ribonucleic acids and the presence of antimicrobial activity against various pathogens including bacteria, fungi, parasites and viruses. The first objective of this doctoral study is focused on the antimicrobial characterization of native Ribonuclease 3 forms purified from eosinophils. Native forms present posttranslational modifications giving different glycosylation grades that modulate their activity during inflammatory processes. This study aims to establish the antimicrobial properties of native forms purified from eosinophils and their activity in a membrane model system. Results indicate that post-translational modifications contribute to the the protein biological activities, suggesting a related physiological role. As a second objective, we evaluated for the first time the antifungal activity of the antimicrobial RNase 3 and RNase 7 against Candida albicans, an eukaryotic pathogen selected as a simple model to test the antimicrobial mechanism of action. Both human ribonucleases displayed a high antifungal activity. Results highlighted a dual mechanism of action, where cell lysis takes place at high protein concentration, while depolarization, cell internalization and cellular RNA degradation is achieved at sublethal doses. Finally, the last objective is focused on the characterization of ribonuclease 8, also called the placental RNase, the most recent human ribonuclease described. RNase 8 has gained and lost one cysteine residue in non-conserved positions in a mechanism called "disulphide shuffling". The protein tendency to aggregate required the design of an alternative purification protocol. We analysed its antimicrobial abilities, suggesting a possible role in innate defence. The results of this study confirmed the high antimicrobial activity of several human ribonucleases from the RNase A superfamily suggesting an ancestral role in the host immune defence response. The study contributed to the understanding of their mechanism of action and set the basis for applied drug design.
Arimany, Nardi Cristina. "Impact of membrane transporters polymorphisms on nucleoside-derived drug bioavailability and action = Impacte dels polimorfismes en transportadors de membrana en la biodisponibilitat i acció de fàrmacs anàlegs de nucleòsids." Doctoral thesis, Universitat de Barcelona, 2013. http://hdl.handle.net/10803/129630.
Повний текст джерелаLos fármacos derivados de nucleósidos son ampliamente utilizados en el tratamiento de enfermedades hematológicas, infecciones virales y enfermedades autoinmunes o inflamatorias. Estos fármacos necesitan de transportadores para ser internalizados en la célula y así, ser activos. Los transportadores implicados en la internalización de los nucleósidos y sus derivados son: los transportadores de nucleósidos concentrativos (CNTs) codificados por SLC28 y, los transportadores de nucleósidos equilibrativos (ENTs) codificados por SLC29. Otros transportadores, como los transportadores de cationes orgánicos (OCTs) codificados por SLC22, están implicados también en el transporte de algunos análogos usados en el tratamiento del SIDA. Los transportadores de nucleósdios y hOCT1 han sido detectados en células de sistema inmune, así como también, en epitelio polarizado donde se encuentran distribuidos asimétricamente mediando un flujo neto de nucleósidos y de sus derivados. Los transportadores de membrana pueden presentar polimorfismos alterando su habilidad de interacción con el sustrato. De todos los transportadores estudiados, hOCT1 es el más polimórfico, estando relacionadas sus variantes con la farmacocinética y farmacodinámica de algunos fármacos, como la metformina. En esta tesis mostramos la importancia que tienen estas variantes polimórficas, no solamente en la internalización de lamivudina, sino también en las interacciones de ésta con otros fármacos co-administrados. La infección de PBMCs con VIH mostró un aumento en la expresión de hOCT1, convirtiéndolos en mejor diana. Se descartó también la posibilidad de que los polimorfismos localizados en el loop extracelular, pudieran afectar la oligomerización del transportador. hOCT1 se ha identificado también como transportador de bendamustina, observándose a su vez, que sus variantes polimórficas modificaban la sensibilidad al fármaco. La sensibilidad de células de CLL ex vivo puede ser debida, en parte, a las variantes polimórficas que presentan. En el caso de los inhibidores de la ADN metiltransferasa (DNMT), observamos que los transportadores de nucleósidos son los responsables de la captación de zebularina pero no de decitabina, mediando un flujo de esta apical-basolateral en un modelo de epitelio polarizado. hOCT1 es capaz de mediar la extrusión de zebularina, en cambio, no lo son las variantes polimórficas estudiadas. Estos resultados estarían indicando que los polimorfismos serían responsables de la sensibilidad al tratamiento con zebularina. Para poder entender mejor la interacción transportador-sustrato, se generó un modelo preliminar de hCNT3 basado en el cristal de CNT de V. cholerae. En resumen, esta tesis muestra la importancia que tienen los transportadores y sus variantes polimórficas, en la biodisponibilidad y acción de los fármacos.