Dissertations / Theses on the topic 'Bisphosphonate'
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Roelofs, Anke. "Anti-tumour mechanisms of action bisphosphonates and bisphosphonate analogues." Thesis, University of Oxford, 2006. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.436994.
Full textDebbabi, M., M. Othmani, and A. Aissa. "Nanocrystalline Hydroxyapatite-Bisphosphonate Composites." Thesis, Sumy State University, 2013. http://essuir.sumdu.edu.ua/handle/123456789/35199.
Full textSharma, Chakrabhavi Gundurao Dileep. "Role of Inflammation and Angiogenesis in Aetiology of Bisphosphonate-related Osteonecrosis of the Jaws." Thesis, Griffith University, 2016. http://hdl.handle.net/10072/367505.
Full textThesis (PhD Doctorate)
Doctor of Philosophy (PhD)
School of Dentistry and Oral health
Griffith Health
Full Text
Duan, Ke. "Bisphosphonate-containing coatings for bone implants." Thesis, University of British Columbia, 2007. http://hdl.handle.net/2429/31288.
Full textApplied Science, Faculty of
Materials Engineering, Department of
Graduate
Stewart, Charlotte. "Structure activity relationships of bisphosphonate analogues." Thesis, University of Aberdeen, 2010. http://digitool.abdn.ac.uk:80/webclient/DeliveryManager?pid=128207.
Full textBenford, Helena L. "Molecular pathways of bisphosphonate-induced apoptosis." Thesis, University of Aberdeen, 2000. http://digitool.abdn.ac.uk/R?func=search-advanced-go&find_code1=WSN&request1=AAIU602025.
Full textWhite, Courtney Ellen. "Characteristics of bisphosphonate elution from orthopaedic implants." Thesis, McGill University, 2006. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=99121.
Full textDuan, Xuchen. "Physiological and biological mechanisms of bisphosphonate action." Thesis, University of Oxford, 2011. http://ora.ox.ac.uk/objects/uuid:36b0439d-2f89-4c1e-8bb3-941b4e6ee847.
Full textRoberts, Jacintha. "Studies on bisphosphonate elution from orthopaedic implants." Thesis, McGill University, 2008. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=112582.
Full textPhoebe, Erin, Jeff Pasteur, Marion Slack, and Jeannie Lee. "Fracture Risk with Bisphosphonate Use versus Concurrent Proton Pump Inhibitor and Bisphosphonate Use: A Systematic Review and Meta- Analysis." The University of Arizona, 2013. http://hdl.handle.net/10150/614271.
Full textSpecific Aims: To determine whether concurrent use of a proton pump inhibitor (PPI) and a bisphosphonate represent an additional fracture risk compared with bisphosphonate use alone and to identify an increased risk of any particular fracture type. Methods: This study was a systematic review and meta-analysis of data collected from PubMed, Cochrane, OVID Medline, Google Scholar, and IPA. The authors utilized the search terms: bisphosphonate, fractures and proton pump inhibitors. Studies which met criteria of being English-language with adults 18 years of age and older were included. Main Results: The studies were cohort studies and primarily evaluated older adults. The summary effect was that use of a PPI with a bisphosphonate showed a slight increase in fracture risk when compared to bisphosphonate-only therapy (odds ratio [OR] 1.12, 95% confidence interval [CI], 1.06-1.18). Systematic review of similar studies showed varied results, making difficult any conclusion regarding fracture risk among the treatments. Conclusion: In this analysis, PPI + bisphosphonate demonstrated a slight increase in fracture rate without inference to an increase in any particular fracture type compared with bisphosphonate only. However, there is minimal data on the association or causal effect of this increase. The few studies available offered contradictory results. Additionally, database studies are subject to the possibility of residual confounding. Further research using randomized control trial (RCT) design evaluating long term use of bisphosphonates with or without PPI and their impact on fractures is needed to determine if there is an additional degree of fracture risk from the concurrent use.
Vassiliadou, Athiná. "Humane Osteoblasten und Bisphosphonate eine In-vitro-Studie des Verhaltens von humanen Osteoblasten unter dem Einfluss von Bisphosphonaten verschiedener Generationen /." [S.l.] : [s.n.], 2003. http://deposit.ddb.de/cgi-bin/dokserv?idn=969815018.
Full textWermelin, Karin. "Surface bound bisphosphonate for implant fixation in bone." Doctoral thesis, Linköpings universitet, Ortopedi och idrottsmedicin, 2008. http://urn.kb.se/resolve?urn=urn:nbn:se:liu:diva-15310.
Full textMorgado, Maria isabel Afonso de Passos. "Studies on potential cellular targets for bisphosphonate drugs." Thesis, University of Sheffield, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.268270.
Full textSavaridas, Terence. "The effects of bisphosphonate on direct fracture healing." Thesis, University of Edinburgh, 2011. http://hdl.handle.net/1842/25158.
Full textWang, Ling. "Syntheses and applications of bisphosphonate-based biomaterials and nanomaterials /." View abstract or full-text, 2007. http://library.ust.hk/cgi/db/thesis.pl?CHEM%202007%20WANG.
Full textMcKenzie, Kimberly. "Skeletal distribution of bisphosphonate after elution from porous implants." Thesis, McGill University, 2010. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=86584.
Full textA porous tantalum implant coated with hydroxyapatite and 14C-labelled zoledronic acid was implanted into the left femur of three dogs. After one year bone samples were taken from sites near to and distant from the implant. The amount of drug in each sample was determined using liquid scintillation counting and its distribution in peri-implant bone was additionally demonstrated using autoradiography.
All distant skeletal bone samples contained 11.8 ng/g zoledronic acid or less whereas bone immediately adjacent to the implant contained 388 ng/g. There was a 10-fold to 100-fold decrease in zoledronic acid content in bone just 1 or 2 cm away from the implant. Autoradiographs of thin bone-implant sections and bone sections revealed the highest concentration of zoledronic acid within and immediately adjacent to the implant. These data demonstrated for the first time that zoledronic acid eluted from an implant remained mainly local, with minimal systemic distribution.
L'attachement squelettique à un implant peut être amélioré en apportant de l'acide zoledronique de bisphosphonate de façon locale depuis l'implant. Le but de la présente étude était d'évaluer la distribution squelettique de l'acide zoledronique localement généré.
Un implant poreux de tantale enduit d'hydroxyapatite et d'acide 14C zoledronique a été implanté dans le fémur gauche de trois chiens. Après un an, plusieurs échantillons d'os, proches et éloignés de l'implant, ont été prélevés. La quantité de médicament dans chaque échantillon a ensuite été déterminée en utilisant un comptage par scintillation liquide; la distribution dans l'os autour de l'implant a aussi été demontré par autoradiographie.
Tous les échantillons prélevés loin de l'implant contenaient 11.8 ng/g d'acide zoledronique ou moins alors que ceux prélevés immédiatement à côté de l'implant contenaient 388 ng/g. Une diminution de 10 à 100 fois dans la teneur en acide zoledronique a été notée dans l'os situé seulement à 1 ou 2 cm de l'implant. Les autoradiographies des sections minces d'os-implant et des sections d'os ont indiqué que la concentration la plus élevée en acide zoledronique se situait dans l'implant et immédiatement à côté. Ces données démontrent, pour la première fois, que l'acide zoledronique élué d'un implant reste principalement local, avec une distribution systémique minimale.
Thompson, Keith. "Novel insights into the molecular pharmacology of bisphosphonate drugs." Thesis, University of Aberdeen, 2003. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.288395.
Full textDudakovic, Amel. "Geranylgeranyl diphosphate synthase as a novel cancer therapeutic target." Diss., University of Iowa, 2010. https://ir.uiowa.edu/etd/795.
Full textKoivukangas, A. (Antti). "Effects of long-term clodronate administration on bone and on fracture healing in rat, with special reference to methodological aspects." Doctoral thesis, University of Oulu, 2002. http://urn.fi/urn:isbn:9514267052.
Full textSmits, Jacqueline Patricia. "Synthesis and evaluation of novel bis-and trisphosphonates." Diss., University of Iowa, 2011. https://ir.uiowa.edu/etd/2772.
Full textGrodde, Katharina. "Bisphosphonat- assoziierte Kiefernekrose (BONJ) im Dental- CT." Doctoral thesis, Universitätsbibliothek Leipzig, 2016. http://nbn-resolving.de/urn:nbn:de:bsz:15-qucosa-215530.
Full textChan, Ka Lok. "Synthesis and bioactivites of new conjugates of bisphosphonate and porphyrin /." View abstract or full-text, 2007. http://library.ust.hk/cgi/db/thesis.pl?CHEM%202007%20CHAN.
Full textZhu, Yinghua, and 朱穎華. "Establishment of osteolysis model in rabbit and evaluation of bisphosphonate intervention." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2004. http://hub.hku.hk/bib/B31246369.
Full textLi, Chunlei, and 李春蕾. "Role of periodontal diseases in bisphosphonate-related osteonecrosis of the jaws." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2014. http://hdl.handle.net/10722/208556.
Full textSaoji, Nachiket A. "Effect of bisphosphonate on osteogenic differentiation of pulp and PDL cells." Thesis, Birmingham, Ala. : University of Alabama at Birmingham, 2008. https://www.mhsl.uab.edu/dt/2009r/saoji.pdf.
Full textPfannkuchen, Nina [Verfasser]. "Chelator-konjugierte Bisphosphonate : Synthese, Radiomarkierung und in vivo-Evaluierung / Nina Pfannkuchen." Mainz : Universitätsbibliothek Mainz, 2018. http://d-nb.info/1149977523/34.
Full textKamble, Sumedh. "Bisphosphonates for Bone Targeting and Cancer Therapy." Thesis, The University of Sydney, 2020. https://hdl.handle.net/2123/22013.
Full textLinderbäck, Paula. "Improved titanium and steel implants : Studies on bisphosphonate, strontium and surface treatments." Doctoral thesis, Linköpings universitet, Institutionen för fysik, kemi och biologi, 2011. http://urn.kb.se/resolve?urn=urn:nbn:se:liu:diva-71289.
Full textConners, Christopher. "Bisphosphonate Functionalized Gold Nanoparticles for the Study and Treatment of Osteoporotic Disease." Scholar Commons, 2017. http://scholarcommons.usf.edu/etd/6818.
Full textGirard, Bruno. "Exploring high dose effects of a bisphosphonate, HEBP, on osteogenesis in vitro." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 2000. http://www.collectionscanada.ca/obj/s4/f2/dsk1/tape4/PQDD_0018/MQ53412.pdf.
Full textStürmer, Stephanie [Verfasser]. "Immunhistochemische Untersuchungen zur Differenzierung unterschiedlicher Knochenreaktionen auf Bisphosphonate in Humanpräparaten / Stephanie Stürmer." Bonn : Universitäts- und Landesbibliothek Bonn, 2013. http://d-nb.info/1043699953/34.
Full textEichelberg, Anne-Christine [Verfasser]. "Bisphosphonate in der Therapie von Patienten mit Multiplem Myelom / Anne-Christine Eichelberg." Berlin : Medizinische Fakultät Charité - Universitätsmedizin Berlin, 2015. http://d-nb.info/1067098887/34.
Full textYamazaki, Toru. "Incidence, risk and risk factors of bisphosphonate-related osteomyelitis of the jaw." Kyoto University, 2013. http://hdl.handle.net/2433/180463.
Full textGardina, Christopher. "Bone Mass Preservation and Fracture Risk Assessment with Bisphosphonate Therapy During Spaceflight." DigitalCommons@CalPoly, 2008. https://digitalcommons.calpoly.edu/theses/5.
Full textSilva, Jonathan Ribeiro da [UNESP]. "Prevenção da Osteonecrose dos Maxilares Induzida por Medicamentos com a utilização de enxerto Xenógeno e β- trifosfato de cálcio (β-TCP)." Universidade Estadual Paulista (UNESP), 2018. http://hdl.handle.net/11449/154852.
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Outra
Objetivo: Avaliar a prevenção da OMIM em ratos em risco de desenvolvimento de osteonecrose na região em que foi realizada a exodontia utilizando apenas coágulo, enxerto de osso xenógeno, e enxerto de β- trifosfato de cálcio (β-TCP). Métodos: Foram utilizados 20 Ratos Wistar machos com 3 meses de idade, pesando 350 – 450g, submetidos a indução da Osteonecrose por uso de ácido zoledrônico (0,04mg/kg) durante 05 semanas. Na 7a semana foi realizado a cirurgia de exodontia dos molares superiores direito e preenchimento do alvéolo com coágulo (controle), enxerto xenógeno (Grupo 2), e β- trifosfato de cálcio (β-TCP) (Grupo 3). A eutanásia foi realizada na 15a semana. Foram realizadas análises morfométrica, estereológica, e imunohistoquímica, onde aplicou-se os testes estatísticos ANOVA e Tukey, considerando-se um nível de significância de 5%. Resultados: Durante a análise macroscópica não houve manifestação clínica da OMIM nos grupos experimentais. A análise quantitativa demonstrou que o Grupo 3 (BTCP) apresentou menor formação de lacunas ósseas e maior formação de tecido ósseo sadio quando comparado com os grupos 1 e 2 (p<0,05). Não houve diferença estatística entre os grupos durante análise de formação de tecido epitelial. Na análise imunohistoquimica, o grupo experimental apresentou maior atividade de remodelação óssea. Conclusão: Os resultados deste trabalho demonstraram que os grupos experimentais apresentaram maior atividade de remodelação óssea, e ausência de manifestação clínica da OMIM. O grupo BTCP ainda demonstrou menor quantidade de lacunas e maior quantidade de osso formado durante analise histológica. No entanto, mais estudos necessitam ser realizados até o desenvolvimento de um protocolo de prevenção desta complicação
Objective: To evaluate the bone formation in rats with osteonecrosis in the region where the extraction was performed using only clot, xenogen bone graft, and calcium β-triphosphate (β-TCP) graft. METHODS: Twenty male Wistar rats weighing 350-450 g were submitted to osteonecrosis induction for the use of zoledronic acid (0.2 mg / kg) for 5 weeks. In the 7th week, the maxillary right molar extraction and filling of the alveolus with clot (control), xenogene graft (Group 2) and calcium β-triphosphate (β-TCP) were performed (Group 3). Euthanasia was performed in the 15th week. Morphometric and stereological analyzes were performed. The ANOVA and Tukey statistical tests were used, considering a level of significance of 5%. Results: During the macroscopic analysis there was no clinical manifestation of the OMIM in the experimental groups. Quantitative analysis showed that Group 3 (BTCP) presented less bone formation and greater formation of healthy bone tissue when compared to groups 1 and 2 (p <0.05). There was no statistical difference between groups during analysis of epithelial tissue formation. In the immunohistochemical analysis no difference was found in the bone remodeling process between the groups. Conclusion: The results of this work were favorable for the use of BTCP for guided bone regeneration and prevention of the clinical manifestation of OMIM in rats. However, more studies need to be performed until the development of a protocol to prevent this complication
Zhang, Rui. "Ionic Copolymer-Magnetite Complexes for Magnetic Resonance Imaging and Drug Delivery." Thesis, Virginia Tech, 2015. http://hdl.handle.net/10919/73648.
Full textMaster of Science
Neudert, Marcus, Christian Fischer, Burkhard Krempien, Markus J. Seibel, and Frieder Bauss. "A Rapid Histological Score for the Semiquantitative Assessment of Bone Metastases in Experimental Models of Breast Cancer." Saechsische Landesbibliothek- Staats- und Universitaetsbibliothek Dresden, 2014. http://nbn-resolving.de/urn:nbn:de:bsz:14-qucosa-134931.
Full textHintergrund: Mit Hilfe eines etablierten Tiermodells zur Erzeugung lokalisationsspezifischer Knochenmetastasen in der Nacktratte wurde ein semiquantitatives histologisches Graduierungssystem zur schnellen Bewertung osteolytischer Knochenmetastasen entwickelt. Das Graduierungssystem liefert hinsichtlich der Metastasenlokalisation, deren Ausmaß und Infiltrationsmuster wertvolle Zusatzinformationen zu den konventionellen histologischen Untersuchungsmethoden. Damit kann beispielsweise auch die pharmakologische Wirkung von Bisphosphonaten auf die Knochenmetastasierung beurteilt werden. Material und Methoden: Männlichen Nacktratten (n = 12 pro Gruppe) wurden Zellen der humanen Brustkrebszellinie MDA-MB-231 in die Oberschenkelarterie inokuliert. Ab dem Auftreten radiologisch erkennbarer Osteolysen 18 Tage nach Inokulation erhielten die Tiere bis zum Studienende (Tag 30) täglich entweder eine subkutane Applikation einer Phosphat-Puffer-Lösung (Kontrollgruppe) oder Ibandronat (IBN, 10 µg P/kg; Behandlungsgruppe). Konventionelle Röntgenaufnahmen wurden an den Tagen 18 und 30 nach Tumorinokulation angefertigt und die Osteolysenflächen mittels Computerauswertung bestimmt. Nach Studienende wurde der Metastasenbefall in beiden Tibiae sowohl konventionell histologisch als auch mittels des neuen Graduierungssystems ausgewertet. Ergebnisse: Die Metastasenfläche korrelierte mit der kummulativen Punktsumme des Graduierungssystems sowohl in der Kontrollgruppe (r = 0,762; p < 0,001) als auch in der Ibandronat- Gruppe (r = 0,951; p < 0,001). Ebenso war die Osteolysenfläche eng mit der Punktesumme in beiden Gruppen korreliert (r = 0,845 und 0,854; p < 0,001). Schlussfolgerung: Die signifikante Reduktion von Knochenmark- und Kortikalisbefall durch IBN deuten auf eine gute lokale Kontrolle des Metastasenwachstums hin
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Kelley, Leslie K. "Effectiveness of Statin and Bisphosphonate Treatment in a 3NP model of Huntington’s Disease." ScholarWorks@UNO, 2015. http://scholarworks.uno.edu/td/1993.
Full textHuikko, Katri. "Capillary electrophoresis- and microchip-mass spectrometry interfaces and their utilization in bisphosphonate analysis." Helsinki : University of Helsinki, 2003. http://ethesis.helsinki.fi/julkaisut/mat/farma/vk/huikko/.
Full textWills, Veronica Sue. "Synthesis of geminal bisphosphonates as potential inhibitors of GGDPS." Diss., University of Iowa, 2015. https://ir.uiowa.edu/etd/1933.
Full textCallard, Jason Scott. "Effect of Zoledronic Acid on Maxillary Alveolar Bone Coverage in Rice Rats With and Without Dental Trauma." The Ohio State University, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=osu1366108637.
Full textFrith, Julie C. "Studies into the mechanism of action of clodronate." Thesis, University of Sheffield, 1998. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.299577.
Full textGardina, Christopher Hazelwood Scott James. "Bone mass preservation and fracture risk assessment with bisphosphonate therapy during spaceflight : a thesis /." [San Luis Obispo, Calif. : California Polytechnic State University], 2008. http://digitalcommons.calpoly.edu/theses/5/.
Full textMajor professor: Scott Hazelwood, Ph.D. "Presented to the faculty of California Polytechnic State University, San Luis Obispo." "In partial fulfillment of the requirements for the degree [of] Master of Science in Engineering with a specialization in Biomedical Engineering." "June 2008." Includes bibliographical references (leaves 46-49). Also available online. Also available on microfiche (2 sheets).
Ward, Jonathan Joseph. "RELATIONSHIPS OF LONG-TERM BISPHOSPHONATE TREATMENT WITH MEASURES OF BONE MICROARCHITECTURE AND MECHANICAL COMPETENCE." UKnowledge, 2014. http://uknowledge.uky.edu/cbme_etds/26.
Full textPagano, Stefanie L. "The Effect of Varying Bisphosphonate Treatment on Changes in Bone Microdamage in Osteoporotic Women." UKnowledge, 2016. http://uknowledge.uky.edu/cbme_etds/40.
Full textTardoski, Sophie. "Traitement des métastases osseuses par association d’un bisphosphonate avec des ultrasons de faible intensité." Thesis, Lyon 1, 2015. http://www.theses.fr/2015LYO10162/document.
Full textBone metastases are common complications of advanced breast cancer. They increase morbidity of patients and alter their quality of life. Bisphosphonates (BPs) stop the progression of osteolysis. However, BPs do not affect the tumor burden located inside the bone marrow cavity. Antitumoral effects have been shown but with high doses incompatibles with a clinical use. BPs bind also avidly to bone mineral which limits their bioavailability and reduce their antitumoral potential in vivo. This work is incorporated within the framework of the enhancement of antitumoral effects of BPs. BPs were combined with low intensity ultrasound (LIUS), which are known to induce a mechanical stimulation and a slight increase of temperature without involving cavitationnal effect. Initially, LIUS were found to increase the penetration of BPs inside several mammary tumor cell lines without affecting their viability by increasing endocytosis. In vivo, a daily repeated treatment of LIUS associated with a single and clinical dose of BPs lead to a decrease in osteolysis as well as tumor burden. The accumulation of unprenylated Rap1A form was found in bone marrow of mice suggesting that LIUS promote BPs penetration inside cells of the bone cavity. The effect of BPs and LIUS was evaluated in a subcutaneous mammary tumor xenograft. Tumor growth was slowed during the first days of LIUS treatment. A study was performed using doxorubicin and BPs leading to a better penetration of both compounds when LIUS were used. This last result allows increasing the field of application of LIUS for breast cancer treatment. In conclusion, this work showed that LIUS are an interesting method to enhance the penetration of drugs inside bone and mammary tumors leading to an increase of their antitumoral activity
Mattos, Ana Carolina Lopes. "Osteonecrosis of the jaw in association to bisphosphonates." Thesis, Boston University, 2008. https://hdl.handle.net/2144/41446.
Full textThe use of bisphosphonate has become more widespread for the treatment of bone metastasis, multiple myeloma, osteoporosis, Paget's disease and other bone malignancies. Osteonecrosis of the jaw (ONJ) has been recently recognized as a possible complication of the use of bisphosphonate therapy. This study includes a review of the literature on the mechanism of action of bisphosphonate and its potential association to the development of osteonecrosis of the jaw. The inhibitory effects of bisphosphonates on osteoclasts and its antiangiogenic properties have been examined as possible mechanisms to induce osteonecrosis of the jaw. The incidence of ONJ in osteoporosis patients receiving bisphosphonate treatment is <1 in 100,000, and in between 1% and 10% in patients with malignancy (Hess et al., 2008). The results of this study suggest a higher incidence of osteonecrosis of the jaw in patients under long term use of nitrogen containing bisphosphonate. The incidence of bisphosphonate associated ONJ in the first 4 to 12 months of therapy was of 1.5% and it increased to 7.7% after 37 to 48 months [Bamias] Additional risk factors include dental extractions, invasive dental procedures and trauma. It is not yet clear, however, if other drugs that affect bone turnover may induce similar complications. This study suggests an association of bisphosphonates to the development of osteonecrosis of the jaw. There is no evidence that bisphosphonates cause osteonecrosis of the jaw. An evaluation of the published data indicates that more research is necessary to understand the relationship of bisphosphonates and osteonecrosis of the jaw.
Lecercle, Delphine. "Synthèse et application de composés gem-bisphosphonates, de puissants complexants de métaux." Phd thesis, Université Paris Sud - Paris XI, 2007. http://tel.archives-ouvertes.fr/tel-00359912.
Full textLa première de ces applications fit suite à des travaux réalisés au sein du laboratoire, ayant montré les fortes propriétés de complexation de ligands bisphosphoniques vis à vis de l.ion uranyle. Les tests in vivo réalisés sur ces composés ayant montré la tendance de ces ligands à entraîner une accumulation hépatique de l'uranium, nous avons voulu remédier à ce problème en modifiant le mode d.ancrage des fonctions bisphosphonates. Pour cela nous avons développé une nouvelle voie d.accès à ces composés utilisant une réaction d.insertion d.espèce métal-carbénoide, portant la fonction bisphosphonate, sur des plates-formes poly-ols et poly-amines.
Concernant la préparation de BPs possédant une activité anticancéreuse, nous avons mis au point une nouvelle voie synthétique utilisant, comme étape clé, une réaction d.á-P-addition d.un pro-nucléophile phosphoré sur un alcyne porteur d.un groupement phosphonate catalysé par une phosphine. Cela nous a permis de préparer une trentaine de composés dont l.activité anti-cancéreuse a été évaluée sur deux lignées cellulaire (A431 et HuH7). Cinq de ces composés possèdent une activité équivalent à celle du composé décrit comme étant le plus actif, le Zolédronate®.
Vanderpoorten, K. J. "Design, synthesis of biologically interesting dinucleotides : ADPR, c ADPR and NAD⺠alkyne (bisphosphonate) analogues." Thesis, Queen's University Belfast, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.426911.
Full textNeudert, Marcus, Christian Fischer, Burkhard Krempien, Markus J. Seibel, and Frieder Bauss. "A Rapid Histological Score for the Semiquantitative Assessment of Bone Metastases in Experimental Models of Breast Cancer." Karger, 2008. https://tud.qucosa.de/id/qucosa%3A27606.
Full textHintergrund: Mit Hilfe eines etablierten Tiermodells zur Erzeugung lokalisationsspezifischer Knochenmetastasen in der Nacktratte wurde ein semiquantitatives histologisches Graduierungssystem zur schnellen Bewertung osteolytischer Knochenmetastasen entwickelt. Das Graduierungssystem liefert hinsichtlich der Metastasenlokalisation, deren Ausmaß und Infiltrationsmuster wertvolle Zusatzinformationen zu den konventionellen histologischen Untersuchungsmethoden. Damit kann beispielsweise auch die pharmakologische Wirkung von Bisphosphonaten auf die Knochenmetastasierung beurteilt werden. Material und Methoden: Männlichen Nacktratten (n = 12 pro Gruppe) wurden Zellen der humanen Brustkrebszellinie MDA-MB-231 in die Oberschenkelarterie inokuliert. Ab dem Auftreten radiologisch erkennbarer Osteolysen 18 Tage nach Inokulation erhielten die Tiere bis zum Studienende (Tag 30) täglich entweder eine subkutane Applikation einer Phosphat-Puffer-Lösung (Kontrollgruppe) oder Ibandronat (IBN, 10 µg P/kg; Behandlungsgruppe). Konventionelle Röntgenaufnahmen wurden an den Tagen 18 und 30 nach Tumorinokulation angefertigt und die Osteolysenflächen mittels Computerauswertung bestimmt. Nach Studienende wurde der Metastasenbefall in beiden Tibiae sowohl konventionell histologisch als auch mittels des neuen Graduierungssystems ausgewertet. Ergebnisse: Die Metastasenfläche korrelierte mit der kummulativen Punktsumme des Graduierungssystems sowohl in der Kontrollgruppe (r = 0,762; p < 0,001) als auch in der Ibandronat- Gruppe (r = 0,951; p < 0,001). Ebenso war die Osteolysenfläche eng mit der Punktesumme in beiden Gruppen korreliert (r = 0,845 und 0,854; p < 0,001). Schlussfolgerung: Die signifikante Reduktion von Knochenmark- und Kortikalisbefall durch IBN deuten auf eine gute lokale Kontrolle des Metastasenwachstums hin.
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