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Computer-aided drug design and ADMET predictions for identification and evaluation of novel potential farnesyltransferase inhibitors in cancer therapy

SILVA, Carlos Henrique Tomich de Paula da; SILVA, Vinicius Barreto da; RESENDE, Jonathan; RODRIGUES, Patricia Franco; BONONI, Fernanda Cristina; BENEVENUTO, Carolina Gomes; TAFT, Carlton Anthony
Fonte: ELSEVIER SCIENCE INC Publicador: ELSEVIER SCIENCE INC
Tipo: Artigo de Revista Científica
ENG
Relevância na Pesquisa
35.93%
We have used various computational methodologies including molecular dynamics, density functional theory, virtual screening, ADMET predictions and molecular interaction field studies to design and analyze four novel potential inhibitors of farnesyltransferase (FTase). Evaluation of two proposals regarding their drug potential as well as lead compounds have indicated them as novel promising FTase inhibitors, with theoretically interesting pharmacotherapeutic profiles, when Compared to the very active and most cited FTase inhibitors that have activity data reported, which are launched drugs or compounds in clinical tests. One of our two proposals appears to be a more promising drug candidate and FTase inhibitor, but both derivative molecules indicate potentially very good pharmacotherapeutic profiles in comparison with Tipifarnib and Lonafarnib, two reference pharmaceuticals. Two other proposals have been selected with virtual screening approaches and investigated by LIS, which suggest novel and alternatives scaffolds to design future potential FTase inhibitors. Such compounds can be explored as promising molecules to initiate a research protocol in order to discover novel anticancer drug candidates targeting farnesyltransferase, in the fight against cancer. (C) 2009 Elsevier Inc. All rights reserved.; CNPq; CAPES; FAPESP; FAPERJ

DERIVATIVE SPECTROPHOTOMETRIC METHOD FOR DEYERMINATION OF ACYCLOVIR IN POLYMERIC NANOPARTICLES

Tavares, Guilherme Diniz; Ishikawa, Gisele Miki; Monteiro, Talita Ferreira; Zanolini, Carolina; Kedor-Hackmann, Erika Rosa Maria; Bou-Chacra, Nádia Araci; Consiglieri, Vladi Olga
Fonte: SOC BRASILEIRA QUIMICA; SAO PAULO Publicador: SOC BRASILEIRA QUIMICA; SAO PAULO
Tipo: Artigo de Revista Científica
ENG
Relevância na Pesquisa
35.98%
A derivative spectrophotometric method was validated for quzintification of acyclovir in poly (n-butylcyanoacrylate) (PBCA) nanoparticles. Specificity, linearity. precision, accuracy, recovery. detection (LOD) and quantification (LOQ) Inuits were established for method validation. First-derivative it 295.2 nm eliminated interferences from nanoparticle ingredients and presented linearity for acyclovir concentrations ranging front 1.25 to 40.0 mu g/mL. (r = 0.9999). Precision and accuracy data demonstrated good reproducibility. Recovery ranged from 99.3 to 101.2. LOD) was 0.08 mu g/mL and LOQ. 0.25 mu g/mL. Thus. the proposed method proved to be easy. low cost. and accurate, and therefore, an useful alternative to quantify acyclovir in nanoparticles.; CNPq; CNPq; CAPES; CAPES

Doseamento da vitamina B6 por espectrofotometria derivada no ultravioleta; Derivative spectrophotometric determination of vitamin B6 in pharmaceutical preparations

Consiglieri, Vladi Olga
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 18/11/1992 PT
Relevância na Pesquisa
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Uma metodologia rápida e seletiva foi desenvolvida para a quantificação da piridoxina em medicamentos. O método foi padronizado para aplicação da espectrofotometria derivada no ultravioleta na análise direta da vitamina em preparações multivitamínicas sólidas (cápsulas) e líquidas (solução oral e injetável). As interferências do espectro UV convencional devidas aos excipientes (veículos) e demais fármacos presentes foram eliminados. As retas de calibração foram calculadas, obtendo-se, para a derivada de 1ª ordem, o coeficiente de correlação linear de 0.99997. Os resultados foram estatisticamente estudados e determinaram-se o desvio padrão, coeficiente de variação e intervalo de confiança. O método foi empregado na análise de amostras comerciais e simuladas e os resultados, quando comparados com aqueles provenientes da aplicação do método da Farmacopéia Americana XXII rev., evidenciaram nítidas vantagens quanto à exatidão e precisão, além da facilidade operacional.; A rapid and selecrive method for rhe dererminarion of pyridoxine in pharmaceuticals has been described. The procedure has been developed using direct UV first-derivative spectrofotometry in solid and liquid preparations (tablets...

Candidatos a leishmanicidas, antichagásicos e tuberculostáticos: estudo da síntese de fármacos dirigidos de hidroximetilnitrofural com manana para liberação específica em macrófagos; Leishmanicidal, antichagasic and tuberculostatic candidates: synthesis study of hydroxymethylnitrofurazone drug targeted with mannan for macrophages.

Primi, Marina Candido
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 26/08/2013 PT
Relevância na Pesquisa
36.08%
As doenças negligenciadas infectam mais de um bilhão de pessoas no mundo, no entanto, uma fração ínfima dos fármacos registrados nos últimos anos é direcionada a essas patologias. Entre as doenças negligenciadas consideradas prioridade, encontram-se doença de Chagas e leishmaniose. A tuberculose, que recentemente não é mais classificada como negligenciada pela Organização Mundial da Saúde, também está entre as prioridades do Ministério da Saúde no Brasil. O arsenal terapêutico disponível para o tratamento destas enfermidades compreende fármacos com toxicidade elevada e resistência crescente, entre outros inconvenientes. Dessa forma, verifica-se a importância no desenvolvimento de novos fármacos para as referidas doenças. Para este fim, o presente trabalho objetivou a síntese de um fármaco dirigido de hidroximetilnitrofural (NFOH) com manana para a liberação específica em macrófagos. O processo de latenciação foi utilizado para a consecução desse objetivo por meio da estratégia de fármacos dirigidos, buscando elevar seletividade e potência do NFOH. Este composto protótipo possui ação potencial tripanomicida, leishmanicida e tuberculostática. O transportador utilizado foi a manana, polímero de manose...

Synthesis, ex Vivo and in Vitro Hydrolysis Study of an Indoline Derivative Designed as an Anti-Inflammatory with Reduced Gastric Ulceration Properties

Chung, Man Chin; dos Santos, Jean Leandro; Oliveira, Ednir Vizioli; Blau, Lorena; Menegon, Renato Farina; Peccinini, Rosangela Goncalves
Fonte: Molecular Diversity Preservation International-mdpi Publicador: Molecular Diversity Preservation International-mdpi
Tipo: Artigo de Revista Científica Formato: 3187-3197
ENG
Relevância na Pesquisa
35.96%
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES); Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); Processo FAPESP: 07/56115-0; The compound 1-(2,6-dichlorophenyl)indolin-2-one (1), planned as a pro-drug of diclofenac (2), was easily synthesized in 94% yield by an intramolecular reaction in the presence of coupling agent (i.e., EDC). Compound 1 showed anti-inflammatory and analgesic activity without gastro-ulcerogenic effects. The chemical and enzymatic hydrolysis profile of the lactam derivative 1 does not indicate conversion to diclofenac (2). This compound is a new non-ulcerogenic prototype for treatment of chronic inflammatory diseases.

Development and Validation of an UV-Derivative Spectrophotometric Method for Determination of Glimepiride in Tablets

Bonfilio, Rudy; de Araujo, Magali B.; Salgado, Hérida Regina Nunes
Fonte: Soc Brasileira Quimica Publicador: Soc Brasileira Quimica
Tipo: Artigo de Revista Científica Formato: 292-299
ENG
Relevância na Pesquisa
35.98%
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq); Glimepiride is an oral antidiabetic drug widely used in treatment of type 2 diabetes. This work proposed the development and validation of a derivative UV spectrophotometric method for determination of glimepiride in tablets. The quantification of glimepiride in 5x10(-3) mol L(-1) NaOH was performed by using a wavelength interval of 8 nm in the range of 220-300 nm. The amplitude values obtained in the second-derivative spectra were arbitrary units of the peak height from the central zero base line to the signals obtained at 279.0, 257.5 and 256.3 nm for quantification of Amaryl (R) tablets 1 mg, Amaryl (R) tablets 2 mg and Amaryl (R) tablets 4 mg, respectively. The method was completely validated according to the International Conference on Harmonization (ICH) guidelines, showing accuracy, precision, selectivity, robustness and linearity. The validated method is suitable for quality control applications, since it does not use polluting reagents, it is simple and has low-cost.

Efficacy and Tolerability of the Combination Valsartan/Hydrochlorothiazide Compared with Amlodipine in a Mild-to-moderately Hypertensive Brazilian Population

Franco, Roberto J.S.; Goldflus, Suely; McQuitty, Mari; Oigman, Wille
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 41-47
ENG
Relevância na Pesquisa
36.12%
Most hypertensive patients need more than one drug to reach recommended blood-pressure targets. We investigated the effects on 24-h ambulatory blood pressure (ABP) of the angiotensin-receptor blocker, valsartan, in combination with hydrochlorothiazide (HCTZ), compared with the calcium-channel blocker amlodipine in a Brazilian population in a multicentre, double-blind, double-dummy, parallel group, controlled study in 373 patients with essential hypertension. After a 2-week washout period, patients with a mean sitting systolic blood pressure (SBP) of 160-190 mmHg were randomized to receive either valsartan 160 mg o.d., or amlodipine 5 mg o.d. for 2 weeks and subsequently force-titrated to valsartan 160 mg/HCTZ 25 mg o.d. or amlodipine 10 mg o.d. This regimen was continued until the end of the study at week 8. The primary efficacy parameter was the change from baseline to week 8 in mean 24-h SBP. Secondary endpoints were change in mean 24-h diastolic blood pressure (DBP), tolerability and safety of treatments. Valsartan/HCTZ achieved a mean reduction in systolic ABP of -19.1 ± 11.3 mmHg compared with -20.7 ± 12.0 mmHg with amlodipine (p = 0.324 for the comparison) and in diastolic ABP by -11.1 ± 7.4 mmHg vs -11.6 ± 7.2 mmHg by amlodipine (p = 0.853 for the comparison). The valsartan/HCTZ group exhibited markedly lower rates of adverse events and discontinuations than the amlodipine group. Peripheral oedemas were far more frequent with amlodipine than with valsartan/HCTZ (1.6% with valsartan/HCTZ; 16.8% with amlodipine). Thus...

Liposomes and micro/nanoparticles as colloidal carriers for nasal drug delivery

Mainardes, Rubiana Mara; Cocenza Urban, Maria Cristina; Cinto, Priscila Oliveira; Chaud, Marco Vinícius; Evangelista, Raul Cesar; Daflon Gremião, Maria Palmira
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Revisão Formato: 275-285
ENG
Relevância na Pesquisa
36.23%
The use of the nasal route for drug delivery has attracted much interest in recent years in the pharmaceutical field. Local and principally systemic drug delivery can be achieved by this route of administration. But the nasal route of delivery is not applicable to all drugs. Polar drugs and some macromolecules are not absorbed in sufficient concentration due to poor membrane permeability, rapid clearance and enzymatic degradation into the nasal cavity. Thus, alternative means that help overcome these nasal barriers are currently in development. Absorption enhancers such as phospholipids and surfactants are constantly used, but care must be taken in relation to their concentration. Drug delivery systems including liposomes, cyclodextrins, micro- and nanoparticles are being investigated to increase the bioavailability of drugs delivered intranasally. This review article discusses recent progress and specific development issues relating to colloidal drug delivery systems in nasal drug delivery. © 2006 Bentham Science Publishers Ltd.

Chorismate synthase: An attractive target for drug development against orphan diseases

Dias, Marcio V.B.; Ely, Fernanda; Palma, Mario Sergio; Azevedo Jr., Walter F. de; Basso, Luiz A.; Santos, Diógenes S.
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Revisão Formato: 437-444
ENG
Relevância na Pesquisa
35.98%
The increase in incidence of infectious diseases worldwide, particularly in developing countries, is worrying. Each year, 14 million people are killed by infectious diseases, mainly HIV/AIDS, respiratory infections, malaria and tuberculosis. Despite the great burden in the poor countries, drug discovery to treat tropical diseases has come to a standstill. There is no interest by the pharmaceutical industry in drug development against the major diseases of the poor countries, since the financial return cannot be guaranteed. This has created an urgent need for new therapeutics to neglected diseases. A possible approach has been the exploitation of the inhibition of unique targets, vital to the pathogen such as the shikimate pathway enzymes, which are present in bacteria, fungi and apicomplexan parasites but are absent in mammals. The chorismate synthase (CS) catalyses the seventh step in this pathway, the conversion of 5-enolpyruvylshikimate-3-phosphate to chorismate. The strict requirement for a reduced flavin mononucleotide and the anti 1,4 elimination are both unusual aspects which make CS reaction unique among flavin-dependent enzymes, representing an important target for the chemotherapeutic agents development. In this review we present the main biochemical features of CS from bacterial and fungal sources and their difference from the apicomplexan CS. The CS mechanisms proposed are discussed and compared with structural data. The CS structures of some organisms are compared and their distinct features analyzed. Some known CS inhibitors are presented and the main characteristics are discussed. The structural and kinetics data reviewed here can be useful for the design of inhibitors. © 2007 Bentham Science Publishers Ltd.

Sistemas biodegradáveis contendo acetato de prednisolona para administração orbitária

Duarte Byrro, Ricardo Martins; Miyashita, Denise; de Albuquerque, Verônica Batista; Velascoe Cruz, Antônio Augusto; da Silva Cunha Júnior, Armando
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 444-450
POR
Relevância na Pesquisa
35.98%
Purpose: The present study aimed to evaluate an injectable extended-release formulation of prednisolone acetate (PA) for orbital administration. Methods: Microspheres (MEs) of poly-ε-caprolactone (PCL) containing PA were developed by the method of solvent evaporation. The MEs obtained were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), encapsulation efficiency and in vitro release profile. The in vivo release profile was evaluated in rabbits after periocular injection of an aqueous suspension of MEs. The local biocompatibility of the system was verified by histopathologic analysis of the deployment region. Results: After MEs preparation, morphological analysis by SEM showed the feasibility of the employed method. The content of PA encapsulated was 43 ± 7% and can be considered as satisfactory. The system characterization by DSC technique, in addition to confirm the system stability, did not indicate the existence of interaction between the drug and the polymer. The in vitro release study showed the prolonged-release features of the developed system. Preliminary in vivo study showed the absence of local toxicity and confirmed the prolonged release profile of PA from MEs, suggesting the viability of the developed system for the treatment of orbital inflammatory diseases. Conclusion: The results obtained in this work are relevant and accredit the system developed as a possible alternative to the treatment of inflammatory orbitopathy.

Progesterone-based strategies to induce ovulation in prepubertal Nellore heifers

Rodrigues, A. D P; Peres, R. F G; Lemes, A. P.; Martins, T.; Pereira, M. H C; Day, M. L.; Vasconcelos, J. L M
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 135-141
ENG
Relevância na Pesquisa
35.96%
Four experiments were conducted to evaluate hormonal strategies to induce ovulation in Nellore heifers. In experiment 1, heifers (N = 1039) received a controlled internal drug release (CIDR) of fourth use (CIDR-4) on Day -12 or no CIDR (CIDR-0). The CIDR was removed on Day 0 in the CIDR-4 treatment, and estrus detection and AI were performed from Days 1 to 7. On Day 8, heifers not detected in estrus were evaluated for CL presence and received the same treatment again, followed by estrus detection and AI from Days 21 to 27. All heifers in experiments 2 (N = 896), 3 (N = 839), and 4 (N = 948) received the CIDR-4 treatment on Day -12. In experiment 2, heifers were randomly assigned to a control group (no additional treatment) or to receive equine chorionic gonadotropin (eCG; 200 IU eCG im) on Day 0. In experiment 3, heifers received the same treatments as in experiment 2, or a treatment that included eCG and estradiol cypionate (ECP) (eCG+ECP; 200 IU im eCG plus 0.5 mg ECP im) on Day 0. In experiment 4, heifers received the treatments described in experiment 3 or only ECP (0.5 mg) on Day 0. In experiments 2 and 3, estrus detection and AI was performed from Days 1 to 7 and on Day 8, heifers not detected in estrus were evaluated for CL presence. In experiment 4...

Development and in vitro evaluation of coated pellets containing chitosan to potential colonic drug delivery

Ferrari, Priscileila Colerato; Souza, Fagner Magalhães; Giorgetti, Leandro; Oliveira, Giselle Faria; Ferraz, Humberto Gomes; Chaud, Marco Vinícius; Evangelista, Raul Cesar
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 244-252
ENG
Relevância na Pesquisa
36.01%
In this work pellets containing chitosan for colonic drug delivery were developed. The influence of the polysaccharide in the pellets was evaluated by swelling, drug dissolution and intestinal permeation studies. Drug-loaded pellets containing chitosan as swellable polymer were coated with an inner layer of Kollicoat® SR 30 D and an outer layer of the enteric polymer Kollicoat® MAE 30 DP in a fluidized-bed apparatus. Metronidazole released from pellets was assessed using Bio-Dis dissolution method. Swelling, drug release and intestinal permeation were dependent on the chitosan and the coating composition. The drug release data fitted well with the Weibull equation, indicating that the drug release was controlled by diffusion, polymer relaxation and erosion occurring simultaneously. The film coating was found to be the main factor controlling the drug release and the chitosan controlling the drug intestinal permeation. Coated pellets containing chitosan show great potential as a system for drug delivery to the colon. © 2012 Elsevier Ltd.

Nanotechnology-based drug delivery systems for treatment of hyperproliferative skin diseases - a review

dos Santos, Fernanda Kolenyak; Oyafuso, Marcia Helena; Kiill, Charlene Priscila; Daflon-Gremião, Maria Palmira; Chorilli, Marlus
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 159-167
ENG
Relevância na Pesquisa
36.16%
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq); Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES); The chronic hyperproliferative diseases (CHD) include cancer, precancerous lesions and diseases of unknown etiology such as psoriasis. Various drugs have been used in the treatment of CHD, such as antiproliferative and corticosteroids in general. However, some drugs have properties that limit their effectiveness, such as low solubility in water and low penetration of the skin. Thus, the control of drug release in the skin may improve efficacy and reduce side effects of many drugs used in hyperproliferative diseases. The purpose of this study was to make a systematic review of nanotechnology-based drug delivery systems used against hyperproliferative skin diseases. © 2013 Bentham Science Publishers.

Development and characterization of biocompatible isotropic and anisotropic oil-in-water colloidal dispersions as a new delivery system for methyl dihydrojasmonate antitumor drug

Rolfsen Ferreira da Silva, Gisela Bevilacqua; Scarpa, Maria Virginia; Rossanezi, Gustavo; Tabosa do Egito, Eryvaldo Socrates; Oliveira, Anselmo Gomes de
Fonte: Dove Medical Press Ltd Publicador: Dove Medical Press Ltd
Tipo: Artigo de Revista Científica Formato: 867-876
ENG
Relevância na Pesquisa
35.94%
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES); Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq); Microemulsions (MEs) are colloidal systems that can be used for drug-delivery and drug-targeting purposes. These systems are able to incorporate drugs modifying bioavailability and stability and reducing toxic effects. The jasmonate compounds belong to a group of plant stress hormones, and the jasmonic acid and its methyl ester derivative have been described as having anticancer activity. However, these compounds are very poorly water-soluble, not allowing administration by an intravenous route without an efficient nanostructured carrier system. In this work, biocompatible MEs of appropriate diameter size for intravenous route administration, loaded and unloaded with methyl dihydrojasmonate (MJ), were developed and described in a pseudo-ternary phase diagram. The compositions of the MEs were carefully selected from their own regions in the pseudo-ternary phase diagram. The formulations were analyzed by light scattering, polarized light microscopy, and X-ray diffraction. Also, a study on rheological profile was performed. The results showed that the droplet size decreased with both MJ incorporation and oil phase/surfactant ratio. All compositions of the studied MEs showed rheological behavior of pseudoplastic fluid and amorphous structures. In the absence of MJ...

Development and validation of an UV-derivative spectrophotometric method for determination of glimepiride in tablets

Bonfilio,Rudy; Araújo,Magali B. de; Salgado,Hérida R. N
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/02/2011 EN
Relevância na Pesquisa
35.98%
Glimepiride is an oral antidiabetic drug widely used in treatment of type 2 diabetes. This work proposed the development and validation of a derivative UV spectrophotometric method for determination of glimepiride in tablets. The quantification of glimepiride in 5×10-3 mol L-1 NaOH was performed by using a wavelength interval of 8 nm in the range of 220-300 nm. The amplitude values obtained in the second-derivative spectra were arbitrary units of the peak height from the central zero base line to the signals obtained at 279.0, 257.5 and 256.3 nm for quantification of Amaryl® tablets 1 mg, Amaryl® tablets 2 mg and Amaryl® tablets 4 mg, respectively. The method was completely validated according to the International Conference on Harmonization (ICH) guidelines, showing accuracy, precision, selectivity, robustness and linearity. The validated method is suitable for quality control applications, since it does not use polluting reagents, it is simple and has low-cost.

Synthesis of 4-acryloylmorpholine-based hydrogels and investigation of their drug release behaviors

Efe,Hülya; Bicen,Merve; Kahraman,Memet Vezir; Kayaman-Apohan,Nilhan
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/05/2013 EN
Relevância na Pesquisa
35.94%
In this study, hydrogels based on an amphiphilic, water soluble, bisubstituted and biocompatible acrylamide derivative, namely 4-acryloylmorpholine (4-AcM), were prepared. 4-AcM based hydrogels with different compositions were synthesized by photopolymerization from the mixtures of poly(ethylene glycol) diacrylate (PEG-DA) and poly(2-hydroxy ethyl methacrylate) (HEMA), and characterized by Fourier transform infrared spectroscopy (FTIR). Gel percentage and equilibrium swelling ratios were determined. Images obtained by scanning electron microscopy (SEM) confirmed porous structure of the hydrogels. Ciprofloxacin.HCl was chosen as a model drug in order to understand the drug loading and release behaviors of the hydrogels. As 4-AcM content increased, higher drug release was observed. On the other hand, the increase in crosslinking density due to PEG-DA content resulted in the swelling decrease of the hydrogel and reduced the diffusion of the drug.

Eribulin drug review

Shetty, Nishitha; Gupta, Sudeep
Fonte: Medknow Publications & Media Pvt Ltd Publicador: Medknow Publications & Media Pvt Ltd
Tipo: Artigo de Revista Científica
Publicado em //2014 EN
Relevância na Pesquisa
35.94%
Eribulin is an anticancer drug approved for treatment of metastatic breast cancer. This drug is a synthetic derivative from Japanese marine sponge Halichondria okadai. It acts by interfering with the microtubular growth ultimately leading to apoptosis after prolonged mitotic blockage. In patients with metastatic breast cancer refractory to anthracyclines and taxanes, eribulin is one of the life-saving options. Neutropenia, neuropathy and QT prolongation are the most frequent adverse events associated with this drug. Phase I/II trials are also underway in refractory lung, ovarian, pancreatic, bladder, and soft tissue tumors. Larger prospective studies will define the role of this drug in a wide variety of tumors, and the future looks very promising.

Target-Fishing entzündungsrelevanter Arzneistoffe sowie biochemisch- molekularpharmakologische Charakterisierung der Arzneistoff-Target Interaktion; Target-fishing of drugs relevant to inflammation and biochemical molecular pharmacological characterisation of the drug-target interaction

Behnke, Felix
Fonte: Universidade de Tubinga Publicador: Universidade de Tubinga
Tipo: Dissertação
DE_DE
Relevância na Pesquisa
35.94%
Der Pull-down Assay ist ein nützliches Werkzeug für die Identifizierung und Evaluierung von Arzneistoff Zielstrukturen. In sogenannten “Target-Fishing” Experimenten wird ein Arzneistoff oder eine pharmakologisch aktive Substanz kovalent an eine unlösliche Matrix gebunden und mit einen Zelllysat als Proteinquelle inkubiert. Proteine, die hierbei an den Arzneistoff binden, können isoliert und identifiziert werden. Diese Arbeit beschreibt grundlegende Verbesserungen sowie die beispielhafte Anwendung zur Identifizierung von Zielstrukturen für bislang uncharakterisierte, anti-entzündliche Wirkungen ausgewählter Substanzen. Im methodischen Teil dieser Arbeit werden (i) grundlegende Verbesserungen experimenteller Bedingungen, (ii) innovative Strategien der Liganden Immobilisation, (iii) die Entwicklung eines biokompatiblen, UV Licht spaltbaren Linker-Systems, (iv) die Etablierung einer semi-quantitativen Fishing-Methode zur Unterscheidung zwischen selektiv und unselektiv gebundenen Targets sowie (v) die Etablierung der zweidimensionalen-differential Gelelektrophorese für die Analyse von Target-Fishing Eluaten, dargestellt. Für die Verbesserung grundlegender, experimenteller Bedingungen des Target-Fishings wurde der Einfluss verschiedener Puffer-Systeme...

RNAi-based discovery and validation of new drug targets in filarial nematodes

Behm, Carolyn; Bendig, Mary; McCarter, James; Sluder, Ann
Fonte: Elsevier Publicador: Elsevier
Tipo: Artigo de Revista Científica
Relevância na Pesquisa
35.94%
Human filarial nematodes cause river blindness and lymphatic filariasis, both of which are diseases that produce considerable morbidity. Control of these diseases relies on drug treatments that are ineffective against macrofilariae and are threatened by the development of resistance. New validated drug targets are required to allow development of new classes of antifilarial drugs. To identify and validate potential new drug targets, we propose a collaborative research strategy utilizing bioinformatic filters and assessment of gene function by RNA interference in Caenorhabditis elegans and Brugia malayi.

Determinação da glibenclamida por espectrofotometria derivada no ultravioleta para avaliação do teste ou perfil de dissolução de comprimidos; Glibenclamide determination by derivative ultraviolet spectrophotometry for test or dissolution profile assessment in tablets

Martins, Janaina Diniz; Nery, Christiane Gino Colu; Pianetti, Gerson Antônio; Viana-Júnior, Nilton de Souza; Vianna-Soares, Cristina Duarte
Fonte: Universidade de São Paulo. Faculdade de Ciências Farmacêuticas Publicador: Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
Tipo: info:eu-repo/semantics/article; info:eu-repo/semantics/publishedVersion; Artigo Avaliado pelos Pares Formato: application/pdf
Publicado em 01/03/2007 POR
Relevância na Pesquisa
36.13%
A glibenclamida (GLIB) ou gliburida, agente hipoglicemiante oral de segunda geração, da classe das sulfoniluréias, é usada sob a forma de comprimidos para controle do diabetes mellitus. Possui baixa solubilidade aquosa, podendo proporcionar baixa liberação no teste de dissolução de comprimidos e acarretar variabilidades no tratamento. A solução metanólica de GLIB apresenta máximos de absorção em lambda 210 nm, 227,5 nm e 300 nm na região ultravioleta (UV). Após liberaçao de comprimidos, a sua determinação espectrofotométrica na região UV é dificultada devido à baixa concentração proporcionada após o teste de dissolução (comprimidos GLIB 5 mg, volume de meio 900 mL, 0,56 mg%) e à baixa absortividade em comprimento de onda característico, lambda 300 nm. Por estas razões, até hoje, não existe um método de análise proposto para o teste de dissolução em farmacopéias nacional ou estrangeiras para monografia de glibenclamida comprimidos. A falta de uniformidade nestes procedimentos onera a execução de testes de dissolução para verificação da equivalência farmacêutica de especialidades candidatas a genéricos. Este trabalho propõe a determinação espectrofotométrica de GLIB por derivada de primeira e segunda ordens (máximos lambda 238 nm e 218 nm...