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1.
Rev. CEFAC ; 21(2): e1319, 2019.
Article in English | LILACS-Express | LILACS | ID: biblio-1020353

ABSTRACT

ABSTRACT Purpose: to investigate, from a historical perspective, the path that led to the creation of the Speech-Language Pathology and Audiology Undergraduate Program of the Federal University of Bahia. Methods: this qualitative, cross-sectional study adopts an oral history methodology, using document analysis and interviews. Results: a narrative was developed, bringing to light the history of this program and pointing to specificities that involve the training in Speech-Language Pathology and Audiology offered by UFBA. It also highlights the collaboration given by the student activist movement to these accomplishments. Conclusion: the results of this research comprise a memory that can contribute to an in-depth reflection of the training in Speech-Language Pathology and Audiology in Brazil, making evident, in the process, the inseparability between educational and health demands.


RESUMO Objetivo: investigar, desde uma perspectiva histórica, o percurso que levou à constituição do Curso de Fonoaudiologia da Universidade Federal da Bahia (UFBA). Métodos: trata-se de estudo qualitativo e transversal. Adota metodologia da história oral, utilizando análise documental e entrevistas. Resultados: foi elaborada uma narrativa que revela a história do referido curso e aponta para especificidades que envolvem a formação em Fonoaudiologia oferecida pela UFBA. Destaca-se, ainda, a colaborativa presença do movimento estudantil nos avanços conquistados. Conclusão:os resultados dessa pesquisa compõem uma memória que pode contribuir para uma reflexão aprofundada a respeito da formação em Fonoaudiologia no Brasil, colocando em evidência a indissociabilidade entre demandas educacionais e de saúde nesse processo.

2.
Science ; 351(6271): 388-91, 2016 Jan 22.
Article in English | MEDLINE | ID: mdl-26798016

ABSTRACT

Ecological intensification, or the improvement of crop yield through enhancement of biodiversity, may be a sustainable pathway toward greater food supplies. Such sustainable increases may be especially important for the 2 billion people reliant on small farms, many of which are undernourished, yet we know little about the efficacy of this approach. Using a coordinated protocol across regions and crops, we quantify to what degree enhancing pollinator density and richness can improve yields on 344 fields from 33 pollinator-dependent crop systems in small and large farms from Africa, Asia, and Latin America. For fields less than 2 hectares, we found that yield gaps could be closed by a median of 24% through higher flower-visitor density. For larger fields, such benefits only occurred at high flower-visitor richness. Worldwide, our study demonstrates that ecological intensification can create synchronous biodiversity and yield outcomes.


Subject(s)
Bees , Biodiversity , Crop Production , Crops, Agricultural/growth & development , Pollination , Africa , Animals , Asia , Flowers/growth & development
3.
Nat Prod Commun ; 9(7): 941-2, 2014 Jul.
Article in English | MEDLINE | ID: mdl-25230498

ABSTRACT

As a continuation of our research on the Baccharis genus, the evaluation of the antioxidant effect by TRAP and TBARS assays of three isolated compounds from n-butanol fractions of B. articulata and B. usterii is reported. The structures of these compounds were established as 4-O-beta-D-glucopyranosyl-3,5-dimethoxybenzyl-methanol (1), 5-O-[E]-dicaffeoylquinic acid (2), and 7-hydroxy-5,4'-dimethoxyflavone (3). In the TRAP assay it was possible to observe an antioxidant effect of both n-butanol fractions at 1.25 microg/mL. Among the isolated compounds, compound 2 displayed a remarkable contribution to the total antioxidant capacity of the n-butanol fraction of B. usterii. Moreover, the n-butanol fractions of both species, compounds 1 and 2 at 40.0 microg/mL were efficient in protection of lipid peroxidation in the TBARS experiment. They are promising lead compounds for use in medicinal chemistry studies.


Subject(s)
Antioxidants/pharmacology , Baccharis/chemistry , Phenols/chemistry , Phenols/pharmacology , Antioxidants/chemistry , Baccharis/classification , Thiobarbituric Acid Reactive Substances/chemistry
4.
Lasers Med Sci ; 29(1): 85-90, 2014 Jan.
Article in English | MEDLINE | ID: mdl-23404386

ABSTRACT

The present study investigated the effects of low-level light-emitting diode (LED) therapy (880 ± 10 nm) on interleukin (IL)-10 and type I and III collagen in an experimental model of Achilles tendinitis. Thirty male Wistar rats were separated into six groups (n = 5), three groups in the experimental period of 7 days, control group, tendinitis-induced group, and LED therapy group, and three groups in the experimental period of 14 days, tendinitis group, LED therapy group, and LED group with the therapy starting at the 7th day after tendinitis induction (LEDT delay). Tendinitis was induced in the right Achilles tendon using an intratendinous injection of 100 µL of collagenase. The LED parameters were: optical power of 22 mW, spot area size of 0.5 cm(2), and irradiation time of 170 s, corresponding to 7.5 J/cm(2) of energy density. The therapy was initiated 12 h after the tendinitis induction, with a 48-h interval between irradiations. The IL-10 and type I and III collagen mRNA expression were evaluated by real-time polymerase chain reaction at the 7th and 14th days after tendinitis induction. The results showed that LED irradiation increased IL-10 (p < 0.001) in treated group on 7-day experimental period and increased type I and III collagen mRNA expression in both treated groups of 7- and 14-day experimental periods (p < 0.05), except by type I collagen mRNA expression in LEDT delay group. LED (880 nm) was effective in increasing mRNA expression of IL-10 and type I and III collagen. Therefore, LED therapy may have potentially therapeutic effects on Achilles tendon injuries.


Subject(s)
Achilles Tendon/metabolism , Achilles Tendon/radiation effects , Collagen Type III/genetics , Collagen Type I/genetics , Interleukin-10/genetics , Phototherapy/methods , Tendinopathy/genetics , Tendinopathy/therapy , Animals , Disease Models, Animal , Male , RNA, Messenger/genetics , RNA, Messenger/metabolism , Rats , Rats, Wistar , Real-Time Polymerase Chain Reaction , Up-Regulation/radiation effects
6.
Int J Pharm ; 454(2): 621-4, 2013 Oct 01.
Article in English | MEDLINE | ID: mdl-23680728

ABSTRACT

Nanoliposomes are widely used for drug delivery in the human body. Cell-penetrating peptides are amphiphilic peptides inserting in the lipid bilayer of these lipid vesicles to induce the fusion with target cells. Separation by size exclusion chromatography coupled with the analysis by light scattering detectors provides both the hydrodynamic radius and the radius of gyration of all the liposomes in a sample. In this paper, the influence of the insertion of a cationic peptide, K2LA12, on the size and shape of anionic liposomes has been studied by this approach. The results obtained highlighted an increase in size and a slight deformation of the lipid vesicles depending on the concentration of peptides incorporated into the lipid bilayers.


Subject(s)
Cell-Penetrating Peptides/chemistry , Dimyristoylphosphatidylcholine/chemistry , Liposomes/chemistry , Nanostructures/chemistry , Phosphatidylglycerols/chemistry , Particle Size
7.
Psico (Porto Alegre) ; 43(3): 368-379, jul.-set. 2012.
Article in Portuguese | Index Psychology - journals | ID: psi-57361

ABSTRACT

O estágio é entendido legalmente como ato educativo escolar supervisionado, desenvolvido no ambiente de trabalho e destinado a preparar alunos em formação escolar para o trabalho produtivo. Esta pesquisa objetivou compreender o processo de subjetivação profissional de graduandas de Psicologia de uma universidade pública de Minas Gerais à luz de uma perspectiva crítica em psicologia escolar. Participaram três estudantes e suas respectivas supervisoras. Como recurso para a construção dos dados foi utilizado a história oral, por meio de entrevistas não estruturadas. Constatamos que o processo de formação do futuro psicólogo é constituído por determinações múltiplas que vão além do âmbito acadêmico e indicam o rompimento da dicotomia entre a dimensão profissional e a dimensão pessoal.(AU)


The stage is understood by law act as a supervised school education, developed in the workplace and to prepare students in school education for productive work. This research aimed to understand the undergraduates at a public university of Minas Gerais in the light of a critical perspective in school psychology. Participated in three students and their supervisors. As a resource to build on the data, oral history, through unstructured interviews. We found that the process of educating future psychologists consists of multiple determinations that go beyond the academic and indicate the breakup of the dichotomy between the professional dimension and personal dimension.(AU)


La etapa se entiende como un acto jurídicamente supervisado la educación escolar, desarrollada en el lugar de trabajo y preparar a los estudiantes en la educación escolar para el trabajo productivo. Esta investigación tuvo como objetivo comprender el proceso de subjetivación de los cursos de graduación de profesionales de la Psicología en una universidad pública de Minas Gerais, a la luz de una perspectiva crítica en psicología escolar. Participó en tres estudiantes y sus supervisores. Como una característica para la construcción de la historia de datos se utiliza por vía oral, por medio de entrevistas no estructuradas. Se encontró que el proceso de educar a los futuros psicólogos se compone de múltiples determinaciones que van más allá de lo académico y lo indica la ruptura de la dicotomía entre la dimensión profesional y la dimensión personal.(AU)


Subject(s)
Humans , Male , Female , Young Adult , Adult , Training Support , Students , Psychology
8.
Psico (Porto Alegre) ; 43(3): 368-379, jul.-set. 2012.
Article in Portuguese | LILACS | ID: lil-743603

ABSTRACT

O estágio é entendido legalmente como ato educativo escolar supervisionado, desenvolvido no ambiente de trabalho e destinado a preparar alunos em formação escolar para o trabalho produtivo. Esta pesquisa objetivou compreender o processo de subjetivação profissional de graduandas de Psicologia de uma universidade pública de Minas Gerais à luz de uma perspectiva crítica em psicologia escolar. Participaram três estudantes e suas respectivas supervisoras. Como recurso para a construção dos dados foi utilizado a história oral, por meio de entrevistas não estruturadas. Constatamos que o processo de formação do futuro psicólogo é constituído por determinações múltiplas que vão além do âmbito acadêmico e indicam o rompimento da dicotomia entre a dimensão profissional e a dimensão pessoal.


The stage is understood by law act as a supervised school education, developed in the workplace and to prepare students in school education for productive work. This research aimed to understand the undergraduates at a public university of Minas Gerais in the light of a critical perspective in school psychology. Participated in three students and their supervisors. As a resource to build on the data, oral history, through unstructured interviews. We found that the process of educating future psychologists consists of multiple determinations that go beyond the academic and indicate the breakup of the dichotomy between the professional dimension and personal dimension.


La etapa se entiende como un acto jurídicamente supervisado la educación escolar, desarrollada en el lugar de trabajo y preparar a los estudiantes en la educación escolar para el trabajo productivo. Esta investigación tuvo como objetivo comprender el proceso de subjetivación de los cursos de graduación de profesionales de la Psicología en una universidad pública de Minas Gerais, a la luz de una perspectiva crítica en psicología escolar. Participó en tres estudiantes y sus supervisores. Como una característica para la construcción de la historia de datos se utiliza por vía oral, por medio de entrevistas no estructuradas. Se encontró que el proceso de educar a los futuros psicólogos se compone de múltiples determinaciones que van más allá de lo académico y lo indica la ruptura de la dicotomía entre la dimensión profesional y la dimensión personal.


Subject(s)
Humans , Male , Female , Young Adult , Psychology , Students
9.
J Enzyme Inhib Med Chem ; 26(2): 204-15, 2011 Apr.
Article in English | MEDLINE | ID: mdl-20545489

ABSTRACT

Cell cycle progression is dependent on the intracellular iron level and chelators can lead to iron depletion and decrease cell proliferation. This antiproliferative effect can be inhibited by exogenous iron. In this work, we present the synthesis of some new synthetic calix[4]arene podands bearing diamino-tetraesters, diamino-tetraalcohols, diamino-tetraacid and tetraaryloxypentoxy groups at the lower rim, designed as potential iron chelators. We report their effect on cell proliferation, in comparison with the new oral chelator ICL670A (4-[3,5-bis-(2-hydroxyphenyl)-1,2,4-triazol-1-yl]-benzoic acid). The antiproliferative effect of these new compounds was studied in the human hepatocarcinoma HepaRG cell cultures using cell nuclei counting after staining with the DNA intercalating fluorescence dye, Hoechst 33342. Their cytotoxicity was evaluated by the extracellular LDH activity. Preliminary results indicated that their antiproliferative effect was mainly due to their cytotoxicity. The efficiency of these compounds, being comparable to that of ICL670, was independent of iron depletion. This effect remains to be further explored. Moreover, it also shows that the new substituted calix[4]arenes could open the way to valuable new approaches for medicinal chemistry scaffolding.


Subject(s)
Antineoplastic Agents/pharmacology , Calixarenes/pharmacology , Hepatocytes/drug effects , Phenols/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Calixarenes/chemical synthesis , Calixarenes/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Cells, Cultured , Female , Humans , Liver/cytology , Molecular Structure , Phenols/chemical synthesis , Phenols/chemistry , Solubility
10.
J Enzyme Inhib Med Chem ; 25(2): 216-27, 2010 Apr.
Article in English | MEDLINE | ID: mdl-19883235

ABSTRACT

Cell cycle progression is dependent on the intracellular iron level, and chelators lead to iron depletion and decrease cell proliferation. This antiproliferative effect can be inhibited by exogenous iron. In this work, we present the synthesis of new synthetic calix[4]arene podands bearing alkyl acid and alkyl ester groups at the lower rim, designed as potential iron chelators. We report their effect on cell proliferation, in comparison with the new oral chelator ICL670 (4-[3,5-bis-(2-hydroxyphenyl)-1,2,4-triazol-1-yl]-benzoic acid). The antiproliferative effect of these new compounds was studied in human hepatocarcinoma HepaRG cell cultures using the MTT assay. Their cytotoxicity was evaluated by extracellular LDH activity. Preliminary results indicate that their antiproliferative effect is due to their cytotoxicity. The efficiency of these compounds, comparable to that of ICL670, was independent of iron depletion. This effect remains to be further explored. Moreover, it also shows that novel substituted calix[4]arenes could open the way to new valuable medicinal chemistry scaffolding.


Subject(s)
Calixarenes , Cell Proliferation/drug effects , Iron Chelating Agents , Iron/pharmacology , Phenols , Benzoates/pharmacology , Calixarenes/chemistry , Calixarenes/pharmacology , Cell Line, Tumor , Deferasirox , Drug Design , Humans , Iron/metabolism , Iron Chelating Agents/chemical synthesis , Iron Chelating Agents/chemistry , Iron Chelating Agents/pharmacology , Phenols/chemistry , Phenols/pharmacology , Triazoles/pharmacology
11.
Rev. Ter. Man ; 7(31): 168-172, maio-jun. 2009. ilus, tab
Article in Portuguese | LILACS | ID: lil-537999

ABSTRACT

A articulação talocrural é essencial para o desenvolvimento da marcha, adaptando-se aos diversos tipos de superfícies, estando diretamente relacionada com o equilíbrio e estabilidade. Técnicas de manipulação osteopática têm sido usadas para tratar distúrbios e restaurar a mecânica articular, e podem influenciar diretamente o sistema de controle postural. O objetivo do estudo foi analisar as alterações na estabilidade unipodal de tornozelo geradas por meio da aplicação de uma técnica de thrust. Participaram deste estudo 20 homens com idade 22±2 anos, divididos em dois grupos: G1 (n=10) grupo que recebeu a técnica manipulativa e G2 (n=10) controle. A técnica utilizada foi a manipulação talocrural no membro inferior dominante. Os valores estabilométricos foram obtidos pela plataforma Cibex Reactor antes e cinco minutos após a aplicação da técnica em G1. Os voluntários de G2 foram submetidos ao mesmo protocolo de avaliação, porém sem receber a técnica thrust. Foram obtidos os seguintes resultados: Em G1, observou-se diferenças estatisticamente signifi cantes após a manipulação talocrural (p<0,05), antes os voluntários apresentaram valores estabilométricos de 8.169 pontos. Após a intervenção experimental houve uma queda de 14,35% (6.996 pontos), indicando que houve uma alteração na estabilidade quando comparado ao grupo controle, o qual não obteve diferenças nos resultados. Assim, sugere-se que a manipulação pode ser eficaz na melhora do equilíbrio e estabilidade unipodal de tornozelo.


The talocrural joint is essential for the gait development. It adapts itself to the various areas and types of terrain where you walk and is directly related to balance and stability. Manipulative techniques were used to treat disorders and restore the joint movements, and may influence the postural control system. The study’s goal was to evaluate the immediate changes in stability generated by the application of thrust technique. Twenty men, 22±2 years old, were separated into two groups: G1 (n=10) manipulated group, and G2 (n=10) control group. The technique used was the talocrural thrust in the dominant leg. The data was collected by the stabilometric platform Cibex Reactor before and five minutes after the application of the technique in G1. The group G2 performed only the stabilometric test at the same time, without receiving the thrust. The values obtained were statistically signifi cant for G1 after the manipulation (P<0,05), the stabilometric values before the technique was 8.169 points, and after was a decline of 14.35% (6,996 points), indicating that there was a change in the stability when compared to the control group, which there were no differences between the results. The results of this study suggest that the manipulation can be effective in improving balance and stability.


Subject(s)
Humans , Male , Adult , Tarsal Joints , Osteopathic Medicine , Ankle
12.
Eur J Med Chem ; 44(6): 2643-50, 2009 Jun.
Article in English | MEDLINE | ID: mdl-19056149

ABSTRACT

We report the synthesis of collagen related peptides containing the peptide sequence Lys-Hyp-Gly-Glu-Hyp-Gly-Pro-Lys. The anti-thrombotic activity effects of different glycine mutations in this sequence were studied in regard with their different adopted conformations. The biological results could be correlated to the glycine propensity to adopt a more stable polyproline II helix conformation. The incorporation of these sequences in "collagen-like" alpha-triple-helix peptides shows a pro-thrombotic activity compared to a scrambled negative control peptide which possesses no significant activity.


Subject(s)
Collagen Type III/pharmacology , Oligopeptides/pharmacology , Platelet Aggregation Inhibitors/pharmacology , Platelet Aggregation/drug effects , Blood Platelets/drug effects , Circular Dichroism/methods , Collagen Type III/chemical synthesis , Collagen Type III/chemistry , Drug Evaluation, Preclinical , Humans , Molecular Mimicry , Oligopeptides/chemical synthesis , Oligopeptides/chemistry , Platelet Aggregation Inhibitors/chemical synthesis , Platelet Aggregation Inhibitors/chemistry , Protein Conformation , Protein Structure, Secondary , Structure-Activity Relationship , Thermodynamics , Time Factors
13.
Eur J Med Chem ; 42(5): 694-701, 2007 May.
Article in English | MEDLINE | ID: mdl-17316914

ABSTRACT

We report the synthesis of collagen related peptides containing the peptide sequence Lys-Hyp-Gly-Glu-Hyp-Gly-Pro-Lys. The alpha-triple helix peptides behave as type III collagen analogues supporting platelet aggregation, while the homotrimer which does not exhibit a triple-helical conformation inhibits type III collagen-induced human platelet aggregation. The incorporation of the octapeptide sequence in type III collagen mimetic peptides may lead to the loss of the anti-thrombotic activity for a pro-thrombotic one.


Subject(s)
Collagen Type III/pharmacology , Platelet Aggregation/drug effects , Amino Acid Sequence , Circular Dichroism , Collagen Type III/chemistry , Humans , Molecular Mimicry , Molecular Sequence Data , Nuclear Magnetic Resonance, Biomolecular , Spectrometry, Mass, Electrospray Ionization
14.
Rev. SPAGESP ; 7(2): 30-39, ago.-dez. 2006.
Article in Portuguese | Index Psychology - journals | ID: psi-36295

ABSTRACT

Esse artigo consiste de um relato de experiência cujo objetivo é descrever a estrutura e o funcionamento do atendimento em psicoterapia de grupo, orientado por uma perspectiva construcionista social, tal como realizado em um estágio curricular do curso de Psicologia da Universidade Federal de Uberlândia. A perspectiva teórica utilizada enfatiza a análise do processo social de construção dos sentidos; uma postura de co-construção entre terapeuta e cliente; o olhar sobre os relacionamentos nos quais o cliente está envolvido; a multiplicidade de formas de descrever um problema; e um discurso de potencialidades positivas e de construção de realidades futuras. Os grupos, realizados sob supervisão de um docente, são coordenados por quatro estagiárias divididas em duplas de campo e equipe reflexiva. Os grupos fechados têm 12 sessões semanais de 1h30 de duração e têm como clientela a população adulta. Os principais desafios enfrentados pelas estagiárias se referem à aprendizagem da postura de não-saber e à utilização de perguntas conversacionais. Por meio deste estágio, tem sido possível reconhecer a produtividade, bem como os desafios, da construção desta nova perspectiva em terapia de grupo (AU)


Subject(s)
Humans , Psychotherapy, Group , Professional Training , Professional Practice
15.
Rev. SPAGESP ; 7(2): 30-39, dez. 2006.
Article in Portuguese | LILACS, Index Psychology - journals | ID: lil-693417

ABSTRACT

Esse artigo consiste de um relato de experiência cujo objetivo é descrever a estrutura e o funcionamento do atendimento em psicoterapia de grupo, orientado por uma perspectiva construcionista social, tal como realizado em um estágio curricular do curso de Psicologia da Universidade Federal de Uberlândia. A perspectiva teórica utilizada enfatiza a análise do processo social de construção dos sentidos; uma postura de co-construção entre terapeuta e cliente; o olhar sobre os relacionamentos nos quais o cliente está envolvido; a multiplicidade de formas de descrever um problema; e um discurso de potencialidades positivas e de construção de realidades futuras. Os grupos, realizados sob supervisão de um docente, são coordenados por quatro estagiárias divididas em duplas de campo e equipe reflexiva. Os grupos fechados têm 12 sessões semanais de 1h30 de duração e têm como clientela a população adulta. Os principais desafios enfrentados pelas estagiárias se referem à aprendizagem da postura de não-saber e à utilização de perguntas conversacionais. Por meio deste estágio, tem sido possível reconhecer a produtividade, bem como os desafios, da construção desta nova perspectiva em terapia de grupo.


This article describes the structure and the functioning of a social constructionist group therapy program, as carried out in the Psychology internship at the Universidade Federal de Uberlândia. This theoretical perspective emphasizes the analysis of the social process of making sense; a stance of co-construction between therapist and client; a focus on the relationships in which the client is involved; the multiplicity of forms to describe a problem; and a discourse of positive potentials and the construction of future realities. The groups are coordinated by four trainees divided in pairs of field therapists and reflecting team members. The closed groups have 12 weekly sessions of 1h30 of duration and are attended by adult people. The main challenges faced by the trainees are related to the learning of the not-knowing position and the use of conversational questions. Through this experience, it has been possible to recognize the productivity, as well as the challenges, of the construction of this new perspective in group therapy.


Este artículo consiste de un relato de experiencia cuyo objetivo es describir la estructura y el funcionamiento del atendimiento en psicoterapia de grupo, orientado por una perspectiva construccionista social, tal como realizado en una práctica curricular del curso de Psicología de la Universidade Federal de Uberlândia. La perspectiva teórica utilizada enfatiza el análisis del proceso social de construcción de los sentidos; una postura de co-construcción entre terapeuta y cliente; la mirada sobre los relacionamientos en los cuales el cliente está envuelto; la multiplicidad de formas de describir un problema; y un discurso de potencialidades positivas y de construcción de realidades futuras. Los grupos, realizados con supervisión de un docente, son coordinados por cuatro practicantes dividas en duplas de campo y equipo reflexivo. Los grupos cerrados tienen 12 sesiones semanales de 1h30 de duración y tienen como clientela la población adulta. Los principales desafíos enfrentados por las practicantes se refieren al aprendizaje de la postura de no-saber y a la utilización de preguntas conversacionales. Por medio de esta práctica, ha sido posible reconocer la productividad, bien como los desafíos de la construcción de esta nueva perspectiva en terapia de grupo.


Subject(s)
Internship and Residency , Psychology , Psychotherapy, Group , Staff Development
16.
J Enzyme Inhib Med Chem ; 21(3): 261-70, 2006 Jun.
Article in English | MEDLINE | ID: mdl-16918073

ABSTRACT

Cell cycle progression is dependent on intracellular iron level and chelators lead to iron depletion and decrease cell proliferation. This antiproliferative effect can be inhibited by exogenous iron. In this work, we present the synthesis of new synthetic calix[4]arene podands bearing two aspartic/glutamic acid, ornithine groups or hydrazide function at the lower rim, designed as potential iron chelators. The synthesis only afforded calix[4]arenes in the cone conformation. We report their effect on cell proliferation, in comparison with the new oral chelator ICL670A (4-[3,5-bis-(2-hydroxyphenyl)-1,2,4-triazol-1-yl]-benzoic acid). The antiproliferative effect of these new compounds was studied in the rat hepatoma cell line Fao by measuring mitochondrial succinate dehydrogenase activity. Their cytotoxicity was evaluated by extracellular LDH activity. Preliminary results indicated that among all tested compounds, monohydrazidocalix[4]arene 2 which is not cytotoxic in Fao cells exhibits interesting antiproliferative activity. This effect, independent on iron depletion, remains to be further explored. Moreover, it also shows that new substituted calix[4]arenes could open the way to new valuable medicinal chemistry scaffolding.


Subject(s)
Calixarenes/pharmacology , Carcinoma, Hepatocellular/drug therapy , Cell Proliferation/drug effects , Iron Chelating Agents/pharmacology , Phenols/pharmacology , Animals , Benzoates/pharmacology , Calixarenes/chemical synthesis , Calixarenes/chemistry , Carcinoma, Hepatocellular/enzymology , Carcinoma, Hepatocellular/pathology , Cell Line, Tumor , Deferasirox , Drug Screening Assays, Antitumor , Hydroxyl Radical/antagonists & inhibitors , Hydroxyl Radical/metabolism , Iron Chelating Agents/chemical synthesis , Iron Chelating Agents/chemistry , Molecular Structure , Phenols/chemical synthesis , Phenols/chemistry , Rats , Solubility , Structure-Activity Relationship , Triazoles/pharmacology , Tumor Cells, Cultured
17.
Histochem Cell Biol ; 125(4): 407-17, 2006 Apr.
Article in English | MEDLINE | ID: mdl-16205938

ABSTRACT

Platelet interactions with collagen are orchestrated by the presence or the migration of platelet receptor(s) for collagen into lipid rafts, which are specialized lipid microdomains from the platelet plasma membrane enriched in signalling proteins. Electron microscopy shows that in resting platelets, TIIICBP, a receptor specific for type III collagen, is present on the platelet membrane and associated with the open canalicular system, and redistributes to the platelet membrane upon platelet activation. After platelet lysis by 1% Triton X-100 and the separation of lipid rafts on a discontinuous sucrose gradient, TIIICBP is recovered in lipid raft-containing fractions and Triton X-100 insoluble fractions enriched in cytoskeleton proteins. Platelet aggregation, induced by type III collagen, was inhibited after disruption of the lipid rafts by cholesterol depletion, whereas platelet adhesion under static conditions did not require lipid raft integrity. These results indicate that TIIICBP, a platelet receptor involved in platelet interaction with type III collagen, is localized within platelet lipid rafts where it could interact with other platelet receptors for collagen (GP VI and alpha2beta1 integrin) for efficient platelet activation.


Subject(s)
Blood Platelets/metabolism , Collagen Type III/metabolism , Membrane Microdomains/metabolism , Receptors, Collagen/metabolism , Blood Platelets/ultrastructure , Cell Membrane/metabolism , Cell Membrane/ultrastructure , Cholesterol/metabolism , Cytoskeleton/metabolism , Cytoskeleton/ultrastructure , Humans , Integrin alpha2beta1/metabolism , Membrane Microdomains/ultrastructure , Peptide Fragments/metabolism , Platelet Membrane Glycoproteins/metabolism
18.
Vascul Pharmacol ; 44(1): 42-9, 2006 Jan.
Article in English | MEDLINE | ID: mdl-16269270

ABSTRACT

Platelet adhesion to subendothelial types I and III collagens exposed upon vascular injury plays a crucial role in hemostasis and thrombosis. We previously identified a KOGEOGPK sequence (O for hydroxyproline) within type III collagen interacting with platelets, and demonstrated a strong inhibitory effect of the KOGEOGPK peptide on human platelet interactions with type III collagen in vitro. In the present study, we tested the antithrombotic effect of KOGEOGPK in vivo. In a mouse model of pulmonary thromboembolism induced by intravenous injection of type III collagen and epinephrine, prior administration of 80 mg/kg KOGEOGPK reduced by 50% the size of thrombi embolized in lungs, compared to vehicle-treated mice (p<0.0001). In a mouse model of photochemically induced lesion of caecum venules and arterioles, intravenous injection of 80 mg/kg KOGEOGPK decreased by 76% the occurrence of arteriole occlusion 45 min after vascular injury (p<0.05). A moderate antithrombotic effect of KOGEOGPK was also observed in the injured venules. In addition, intracardiac injection of KOGEOGPK had no effect on the tail bleeding time. These findings demonstrate a substantial contribution of platelet interactions with the type III collagen-related KOGEOGPK sequence in thrombus formation in vivo with preferential involvement in arterial thrombosis.


Subject(s)
Fibrinolytic Agents/pharmacology , Peptides/pharmacology , Platelet Aggregation Inhibitors/pharmacology , Pulmonary Embolism/prevention & control , Thrombosis/prevention & control , Animals , Arterioles/drug effects , Arterioles/pathology , Cecum/blood supply , Collagen Type III/chemistry , Epinephrine , Lung/drug effects , Lung/pathology , Mice , Mice, Inbred C57BL , Peptides/chemical synthesis , Platelet Aggregation/drug effects , Pulmonary Embolism/chemically induced , Pulmonary Embolism/pathology , Rose Bengal , Thrombosis/chemically induced , Thrombosis/pathology , Venules/drug effects , Venules/pathology
19.
J Nat Prod ; 67(10): 1697-700, 2004 Oct.
Article in English | MEDLINE | ID: mdl-15497942

ABSTRACT

From the leaves of Ilex affinis and Ilex buxifolia, two adulterant species of "erva mate" (Ilex paraguariensis), three new triterpenoid glycosides were isolated. Affinoside 1 (3beta-O-[beta-D-glucopyranosyl-(1-->3)-[2-O-acetyl-(1-->2]]-alpha-L-arabinopyranosyl pomolic acid 28-O-beta-D-glucopyranosyl ester, 1) was isolated from I. affinis, while buxifolioside I (28-O-beta-D-glucopyranosyl ester of (20S)-3alpha,19alpha-dihydroxyurs-12-ene-23,28-dioic acid, 7) and buxifolioside II (28-O-beta-D-glucopyranosyl ester of (20S)-3beta,19alpha-dihydroxyurs-12-en-24,28-dioic acid, 8) were isolated from I. buxifolia. Along with these new compounds, ilexoside II (2), ursolic acid (3), 28-nor-ursolic acid (4), 3beta-O-acetylursolic acid (5), and uvaol (6) were also isolated. The observed results confirm the structural specificity of the I. paraguariensis triterpenoids and reinforce a previous proposal to detect mate adulteration by triterpenoid analysis. In addition, the in vitro antitrypanosomal activity of some Ilex triterpenoids is also reported.


Subject(s)
Ilex/chemistry , Plants, Medicinal/chemistry , Triterpenes/isolation & purification , Trypanocidal Agents/isolation & purification , Brazil , Molecular Structure , Plant Leaves/chemistry , Stereoisomerism , Triterpenes/chemistry , Triterpenes/pharmacology , Trypanocidal Agents/chemistry , Trypanocidal Agents/pharmacology , Ursolic Acid
20.
Ciênc. cult. (Säo Paulo) ; 49(5/6): 359-63, Sept.-Dec. 1997. graf
Article in English | LILACS | ID: lil-214097

ABSTRACT

Ilex paraguariensis is widely used in South Brazil, Argentinna, Paraguay and Uruguay as a beverage (maté) and also as a traditional medicinal plant. During the past ten years, we have systematically studied the saponins of the leaves of genuine maté (Ilex paraguariensis) and the other Ilex species reported as adulterants, searching for chemical differences. Here we give a brief account of the elucidated saponin structures. Ilex paraguariensis and Ilex dumosa can be considered as saponin rich species, containing between 5-10 per cent of crude saponins in the leaves, in opposition to other species that showed a lower saponin content. All the saponins from Ilex paraguariensis leaves identified up to now are glycosides of ursolic or oleanolic acid. From Ilex dumosa, the most frequently quoted maté adulterant, we have isolated and elucidated the structures of ten saponins, almost all of them being glycosides of oleanolic acid and one of 29-hydroxyoleanolic acid. In comparison, the saponin pattern for the other South American Ilex species investigated up to now is different. The saponins from I. pseudobuxus, I. argentina, I. taubertiana and I. theezans all have the aglycones derived from the 19alpha-hydroxyursolic acid. Saponins containing this type of aglycone were not found in the leaves of Ilex paraguariensis and Ilex dumosa. These are important features, that may have taxonomical significance. Furthermore, this knowledge is necessary to develop methodologies for quality control of maté products and to identify the compounds involved in the tast, flavor and pharmacological properties.


Subject(s)
Beverages , Plant Leaves/chemistry , Saponins/analysis , Brazil
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