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Some effects of cimetidine on the reproductive organs of rats

Pereira, O. C M
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 197-199
ENG
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36.06%
1. The development of genital organs of rats chronically treated with cimetidine showed that the drug may present anti-androgenic activity. 2. This treatment did not alter the sensitivity of vas deferens to noradrenaline, but increased their sensitivity to BaCl2. 3. In the male reproductive system, cimetidine must have peripheral actions apart from the central ones observed after chronic treatment.

EFEITO DE SURFACTANTES NA ESTABILIDADE DE COMPOSTOS DE USO TERAPEUTICO

De Oliveira, A. G.
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 183-197
POR
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36.16%
A critical revision of literature as regards to the drug stability in the presence of surfactants were realized. The functional groups envolved in the drug decomposition were used to the development of the discussion. The analysis indicated that the detergent effect can be used to control the rates and mechanisms of drug decomposition and to obtain specific information about the drug reactivity in the environment of pharmacological action.

Free radical production by azomethine H: Effects on pancreatic and hepatic tissues

Novelli, E. L B; Silva, A. M M; Monteiro, J. P.; Sacomani, L. B.; Novellif, J. L V B
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 319-324
ENG
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The antimalarial properties of azomethine H represent the basis for its use as a chemotherapeutic agent. This work was carried out in order to verify the biological side effects of azomethine H and to clarify the contribution of reactive oxygen species (ROS) in this process. It was shown that azomethine H increased serum activities of amylase, alanine transaminase (ALT) and the TEARS concentrations, in rats. No changes were observed in glutathione peroxidase and catalase activities. The drug-induced tissue damage might be due to superoxide radicals (O-2(.-)), since Cu-Zn superoxide dismutase activities were increased by azomethine I-I treatment. This study allows tentative conclusions to be drawn regarding which reactive oxygen metabolites play a role in azomethine H activity. We concluded that (O-2(.-)) maybe produced as a mediator of azomethine H action.

Thermoanalytical study of praziquantel-loaded PLGA nanoparticles

Mainardes, Rubiana Mara; Gremião, Maria Palmira Daflon; Evangelista, Raul Cesar
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 523-530
ENG
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Polymeric nanoparticles have received great attention as potential controlled drug delivery systems. Biodegradable polymers has been extensively used in the development of these drug carriers, and the polyesters such as polylactic acid, polyglycolic acid and their copolymers as poly-lactide-co- glycolide are the most used, considering its biocompatibility and biodegradability. Thermal analysis techniques have been used for pharmaceutical substances for more than 30 years and are routine methods for screening drug-excipient interactions. The aim of this work is to use thermal analysis to characterize PLGA nanoparticles containing a hydrophobic drug, praziquantel. The results show that the drug is in an amorphous state or in disordered crystalline phase of molecular dispersion in the PLGA polymeric matrix and that the microencapsulation process did not interfere with the chemical structure of the polymer, mantaining the structural drug integrity.

Qualidade dos medicamentos contendo dipirona encontrados nas residências de Araraquara e sua relação com a atenção farmacêutica

Serafim, Eliana Ometto Pavan; Del Vecchio, Adriana; Gomes, Juliana; Miranda, Aline; Moreno, Andréia de Haro; Loffredo, Leonor Monteiro de Castro; Salgado, Hérida Regina Nunes; Chung, Chin Man
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 127-135
POR
Relevância na Pesquisa
36.14%
Many studies had described the morbi-mortality related to medicines. As for the strategies to reduce the possible risks for medicine therapy is very important to readvise the pharmaceutical activity, once the pharmacist has potential for constitute an essential part for the solution of problems related to the utilization of medicines. The purpose of this work was to demonstrate that the therapeutic subdosage and the microbiological contamination may be directly involved with the inappropriate manipulation of medicines stored in residences. Liquid dosage forms containing dipyrone market in Brazil and stored at homes in Araraquara (SP) were analyzed regarding quantitative and microbiological analysis. Only in 57% from 128 samples analyzed the drug quantity was in accordance. Moreover, 26.2% from 128 samples analyzed presented S. aureus, E. coli and Salmonella sp. These results demonstrated clear reduction in their quality, as well as the presence of molds and/or bacteria in some medicines that still agreed with the expirations dates, showing the importance of the pharmacist in advising the correct use and store of medicines.

Molecular modeling databases: A new way in the search of protein targets for drug development

da Silveira, Nelson José Freitas; Bonalumi, Carlos Eduardo; Arcuri, Helen Andrade; de Azevedo Jr., Walter Filgueira
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 1-10
ENG
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DBMODELING is a relational database of annotated comparative protein structure models and their metabolic, pathway characterization. It is focused on enzymes identified in the genomes of Mycobacterium tuberculosis and Xylella fastidiosa. The main goal of the present database is to provide structural models to be used in docking simulations and drug design. However, since the accuracy of structural models is highly dependent on sequence identity between template and target, it is necessary to make clear to the user that only models which show high structural quality should be used in such efforts. Molecular modeling of these genomes generated a database, in which all structural models were built using alignments presenting more than 30% of sequence identity, generating models with medium and high accuracy. All models in the database are publicly accessible at http://www.biocristalografia.df.ibilce.unesp.br/tools. DBMODELING user interface provides users friendly menus, so that all information can be printed in one stop from any web browser. Furthermore, DBMODELING also provides a docking interface, which allows the user to carry out geometric docking simulation, against the molecular models available in the database. There are three other important homology model databases: MODBASE...

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
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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.

The inhibition of 5-enolpyruvylshikimate-3-phosphate synthase as a model for development of novel antimicrobials

Marques, Maurício Ribeiro; Pereira, José Henrique; Oliveira, Jaim S.; Basso, Luiz Augusto; de Azevedo Jr., Walter Filgueira; Santos, Diógenes Santiago; Palma, Mario Sergio
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Revisão Formato: 445-457
ENG
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36.16%
EPSP synthase (EPSPS) is an essential enzyme in the shikimate pathway, transferring the enolpyruvyl group of phosphoenolpyruvate to shikimate-3-phosphate to form 5-enolpyruvyl-3-shikimate phosphate and inorganic phosphate. This enzyme is composed of two domains, which are formed by three copies of βαβαββ-folding units; in between there are two crossover chain segments hinging the nearly topologically symmetrical domains together and allowing conformational changes necessary for substrate conversion. The reaction is ordered with shikimate-3-phosphate binding first, followed by phosphoenolpyruvate, and then by the subsequent release of phosphate and EPSP. N-[phosphomethyl]glycine (glyphosate) is the commercial inhibitor of this enzyme. Apparently, the binding of shikimate-3-phosphate is necessary for glyphosate binding, since it induces the closure of the two domains to form the active site in the interdomain cleft. However, it is somehow controversial whether binding of shikimate-3-phosphate alone is enough to induce the complete conversion to the closed state. The phosphoenolpyruvate binding site seems to be located mainly on the C-terminal domain, while the binding site of shikimate-3-phosphate is located primarily in the N-terminal domain residues. However...

Pharmacognostical evaluation of fruits of Solanum lycocarpum A. St.-Hill. (Solanaceae)

Araújo, M. G F; Galeane, M. C.; Castro, A. D.; Salgado, H. R N; Almeida, A. E.; Cunha, W. R.; Veneziani, R. C S; Moreira, R. R D
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 248-253
ENG
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This study describes the chemical and physical-chemical profile of plant drug and ethanolic extract obtained from fruits of Solanum lycocarpum A. St.-Hill. (Solanaceae). The physical and chemical analysis involved the granulometry determination, non-compacted apparent density, loss on drying in oven and in infrared scale, pH, ash values and extractive values. The results determined the physical-chemical characteristics of the drug plant. It was also carried out the microbiological control of the plant drug. The preliminary phytochemical screening featured the presence of tannins, flavonoids and saponins in the plant drug and alkaloids and steroids in the ethanolic exctract. The solamargine and solasonine glycoalkaloids were identified through TLC and GC/ MS. The levels of total phenols and tannins were quantified in the extract (8.90% and 6,85% respectively). Such studies contribute to the chemical identification and quality control of S. lycocarpum fruits. © 2010 Phcog.net.

Estudo clínico randomizado e aberto para avaliação de eficácia e superioridade dos medicamentos EF028 aerossol, EF028 creme e Andolba® frente ao tratamento controle e comparativo de não inferioridade entre os medicamentos EF028 aerossol, EF028 creme e Andolba® para avaliação de eficácia na redução da sintomatologia dolorosa

Da Costa, Marcelo Cariola Corrêa; Carramão, Sílvia Silva; Pinto, Patrícia Camarano; Milan, Ana Lúcia Koff; Pannuti, Estela Maia Bellini
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 195-200
POR
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Aim: This study aimed to evaluate the efficacy of a new topical drug (EF028) in two separate presentations (aerosol and cream) in a comparative way with the already registered medication, Andolba® (benzocaine, benzoxiquina chloride benzeconio, menthol) and the negative control (hygiene), in the analgesic efficacy after episiotomy wound, reducing the requirement for systemic medication. Methods: 60 patients were voluntary post normal vaginal childbirth with episiotomy, were divided into four groups to comparatively assess the action of the product EF028 (cream and aerosol), Andolba® and soap, the efficacy of decreasing painful symptoms from daily use for 2 times a day for seven days. Clinical assessments and subjective pain occurred daily until the third postoperative day and on the 7th postoperative day. Results: The results showed that the drugs promoted a reduction of painful symptoms and there was no statistically significant difference (p <0.05) between presentations of drug EF028 (cream and aerosol) and Andolba® and the three products were significantly higher (p <0.05) to the control. Conclusions: The evaluated drugs EF028 aerosol, EF028 cream and Andolba® had similar efficacy in relieving the painful symptoms of the perineal region in postoperative episiotomy can be considered as indication for postoperative episiotomies. © Copyright Moreira Jr. Editora.

Adverse drug reaction as cause of hospital admission of elderly people: a pilot study

Varallo, Fabiana R.; Lima, Marcos F.R.; Galduróz, José C.F.; Mastroianni, Patricia C.
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 347
ENG
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46.12%
The objective of this study was to estimate the prevalence of adverse drug reactions (ADR) related to hospital admission of elderly people, identifying the use of potentially inappropriate medication (PIM), the ADR and the risk factors associated with the hospitalization. A cross-sectional study was conducted in a private hospital of São Paulo State, Brazil. All patients aged ≥ 60 years, admitted in the general practice ward in May 2006 were interviewed about the drugs used and the symptoms/complaints that resulted in hospitalization. More than a half (54.5 %) of elderly hospitalizations were related with ADR. The therapeutic classes involved with ADR were: cardiovascular (37.7 %), central nervous (34.6 %) and respiratory (5.7 %). The ADR observed were disorders in circulatory (28.4 %), digestive (20.0 %) and respiratory (18.9 %) tracts. 27 elderly had made PIM and in 20 of them this was the cause of hospitalization. Polypharmacy was an ADR risk factor (p = 0.021).These data allows the healthcare professionals upgrade, qualifying them in pharmcovigilance.

β-conglycinin combined with fenofibrate or rosuvastatin have exerted distinct hypocholesterolemic effects in rats

Ferreira, Ederlan S.; Silva, Maraiza A.; Demonte, Aureluce; Neves, Valdir A.
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica
ENG
Relevância na Pesquisa
36.18%
Background: There is increasing interest in non-pharmacological control of cholesterol and triglyceride levels in the plasma and diet-drug association represent an important area of studies. The objective of this study was to observe the hypocholesterolemic effect of soybean β-conglycinin (7S protein) alone and combined with fenofibrate and rosuvastatin, two hypolipidemic drugs. Methods. The protein and drugs were administered orally once a day to rats and the effects were evaluated after 28 days. Wistar rats were divided into six groups (n = 9): hypercholesterolemic diet (HC), HC+7S protein (300 mg.kg-1 day-1) (HC-7S), HC+fenofibrate (30 mg.kg-1 day-1)(HC-FF), HC+rosuvastatin (10 mg.kg-1 day-1)(HC-RO), HC+7S+fenofibrate (HC-7S-FF) and HC+7S+rosuvastatin (HC-7S-RO). Results: Animals in HC-7S, HC-FF and HC-RO exhibited reductions of 22.9, 35.8 and 18.8% in total plasma cholesterol, respectively. In HC-7S-FF, animals did not show significant alteration of the level in HC+FF while the group HC-7S-RO showed a negative effect in comparison with groups taking only protein (HC-7S) or drug (HC-RO). The administration of the protein, fenofibrate and rosuvastatin alone caused increases in the plasma HDL-C of the animals, while the protein-drug combinations led to an increase compared to HC-FF and HC-RO. The plasma concentration of triacylgycerides was significantly reduced in the groups without association...

Comparison of impurity profiles of lipiblock® vs. orlistat using HPLC and LC-MS/MS

Schneider, Alex; Wessjohann, Ludger A.; Severi, Juliana A.; Wagner, Vilegas
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 91-96
ENG
Relevância na Pesquisa
36.15%
Comparative HPLC-UV and LC-MS/MS studies of impurity profiles of a reference sample (Xenical®, F. Hoffmann-La Roche Ltd., Switzerland) vs. generic (Lipiblock®, EMS-Sigma Pharma, a generic drug) were carried out with ethanol extracts of commercial samples. The generic formulation contained higher levels of common impurities as well as a considerable number of impurities not found in the reference product. The detected impurity profile of Lipiblock® revealed that it most likely is based on fermentation. Since the effect of the impurities is unknown, at this point fully synthetic Xenical® appears to offer a better safety margin than Lipiblock® which, however, compares quite well to other generic formulations.

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
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46.21%
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.

In vitro targeting of Polo-like kinase 1 in bladder carcinoma: Comparative effects of four potent inhibitors

Brassesco, María Sol; Pezuk, Julia Alejandra; Morales, Andressa Gois; De Oliveira, Jaqueline Carvalho; Roberto, Gabriela Molinari; Da Silva, Glenda Nicioli; De Oliveira, Harley Francisco; Scrideli, Carlos Alberto; Tone, Luiz Gonzaga
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 648-657
ENG
Relevância na Pesquisa
36.14%
Despite the improvements in neoadjuvant chemotherapy, the outcome of patients with advanced bladder cancer has changed very little over the past 30 years. In the present study we tested and compared the in vitro antitumor activities of four different inhibitors of Polo-like kinase 1 (PLK1) (BI 2536, BI 6727, GW843682X, and GSK461364), against 3 bladder carcinoma cell lines RT4, 5637 and T24. The impact on radiosensitivity and drug interactions in simultaneous treatments with cisplatin, methotrexate, and doxorubicin were also investigated. Our results showed that PLK1 inhibition prevented cell proliferation and clonogenicity, causing significant inhibition of invasion of tumor cells, though modest differences were observed between drugs. Moreover, all PLK1 inhibitors induced G2/M arrest, with the subsequent induction of death in all 3 cell lines. Drug interactions studies showed auspicious results for all PLK1 inhibitors when combined with the commonly used cisplatin and methotrexate, though combinations with doxorubicin showed mostly antagonistic effects. Comparably, the four PLK1 inhibitors efficiently sensitized cells to ionizing radiation. Our findings demonstrate that irrespective of the inhibitor used, the pharmacological inhibition of PLK1 constrains bladder cancer growth and dissemination...

A polymorphic drug pump in the malaria parasite

Saliba, Kevin; Lehane, Adele; Kirk, Kiaran
Fonte: Blackwell Publishing Ltd Publicador: Blackwell Publishing Ltd
Tipo: Artigo de Revista Científica
Relevância na Pesquisa
36.09%
The human malaria parasite, Plasmodium falciparum, has long been known to have a homologue of the human 'multidrug resistance' P-glycoprotein. P-glycoprotein is an ABC transporter that pumps drugs from multidrug-resistant cancer cells. The malaria parasit

A chemoenzymatic synthesis of the anti-influenza agent Tamiflu

Matveenko, Maria; Willis, Anthony; Banwell, Martin
Fonte: Elsevier Publicador: Elsevier
Tipo: Artigo de Revista Científica
Relevância na Pesquisa
36.09%
The anti-influenza drug Tamiflu® is synthesized from enzymatically derived, enantiomerically pure, and readily available cis-1,2-dihydrocatechol.

Structural Investigation of the Hedamycin:d(ACCGGT) 2 Complex by NMR and Restrained Molecular Dynamics

Owen, Elisabeth; Burley, Glenn; Carver, John; Wickham, Geoffrey; Keniry, Max
Fonte: Academic Press Publicador: Academic Press
Tipo: Artigo de Revista Científica
Relevância na Pesquisa
36.14%
Hedamycin, a member of the pluramycin family of drugs, displays a range of biological responses including antitumor and antimicrobial activity. The mechanism of action is via direct interaction with DNA through intercalation between the bases of the oligonucleotide and alkylation of a guanine residue at 5′-PyG-3′ sites. There appears to be some minor structural differences between two earlier studies on the interaction of hedamycin with 5′-PyG-3′ sites. In this study, a high-resolution NMR analysis of the hedamycin:d(ACCGGT)2 complex was undertaken in order to investigate the effect of replacing the thymine with a guanine at the preferred 5′-CGT-3′ site. The resultant structure was compared with earlier work, with particular emphasis placed on the drug conformation. The structure of the hedamycin:d(ACCGGT)2 complex has many features in common with the two previous NMR structures of hedamycin:DNA complexes but differed in the conformation and orientation of the N,N-dimethylvancosamine saccharide of hedamycin in one of these structures. The preferential binding of hedamycin to 5′-CG-3′ over 5′-TG-3′ binding sites is explained in terms of the orientation and location of the N,N-dimethylvancosamine saccharide in the minor groove.

Identification of sulfated oligosaccharide-based inhibitors of tumour growth and metastasis using novel in vitro assays for angiogenesis and heparanase activity

Parish, Christopher; Freeman, Craig; Brown, Kylie; Francis, Doug; Cowden, William
Fonte: American Association for Cancer Research Publicador: American Association for Cancer Research
Tipo: Artigo de Revista Científica
Relevância na Pesquisa
36.09%
Inhibitors of tumor angiogenesis and metastasis are rapidly emerging as important new drug candidates for cancer therapy. To facilitate the identification of such drugs, we recently developed novel and rapid in vitro assays for human angiogenesis and for

The Malaria Parasites Chloroquine Resistance Transporter is a Member of the Drug/Metabolite Transporter Superfamily

Martin, Rowena; Kirk, Kiaran
Fonte: Society for Molecular Biology Evolution Publicador: Society for Molecular Biology Evolution
Tipo: Artigo de Revista Científica
Relevância na Pesquisa
46.14%
The malaria parasite's chloroquine resistance transporter (CRT) is an integral membrane protein localized to the parasite's acidic digestive vacuole. The function of CRT is not known and the protein was originally described as a transporter simply because it possesses 10 transmembrane domains. In wild-type (chloroquine-sensitive) parasites, chloroquine accumulates to high concentrations within the digestive vacuole and it is through interactions in this compartment that it exerts its antimalarial effect. Mutations in CRT can cause a decreased intravacuolar concentration of chloroquine and thereby confer chloroquine resistance. However, the mechanism by which they do so is not understood. In this paper we present the results of a detailed bioinformatic analysis that reveals that CRT is a member of a previously undefined family of proteins, falling within the drug/metabolite transporter superfamily. Comparisons between CRT and other members of the superfamily provide insight into the possible role of the protein and into the significance of the mutations associated with the chloroquine resistance phenotype. The protein is predicted to function as a dimer and to be oriented with its termini in the parasite cytosol. The key chloroquine-resistance-conferring mutation (K76T) is localized in a region of the protein implicated in substrate selectivity. The mutation is predicted to alter the selectivity of the protein such that it is able to transport the cationic (protonated) form of chloroquine down its steep concentration gradient...