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[PMID]:29366735
[Au] Autor:Mariz Gomes da Silva LM; de Oliveira JF; Silva WL; da Silva AL; de Almeida Junior ASA; Barbosa Dos Santos VH; Alves LC; Brayner Dos Santos FA; Costa VMA; Aires AL; de Lima MDCA; Albuquerque MCPA
[Ad] Endereço:Keizo Asami Immunopathology Laboratory (LIKA), Federal University of Pernambuco, 50740-465, Recife, PE, Brazil.
[Ti] Título:New 1,3-benzodioxole derivatives: Synthesis, evaluation of in vitro schistosomicidal activity and ultrastructural analysis.
[So] Source:Chem Biol Interact;283:20-29, 2018 Mar 01.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Schistosomiasis is considered a serious public health problem in 78 countries and territories located in Africa, Asia and America and it is estimated in more than 249 million people infected by any of the species of Schistosoma. The exclusive use of praziquantel (PZQ), effective drug against all species of Schistosoma, has been the basis of the development of a possible resistance against the strains of this parasite. In addition, PZQ is not effective against young forms of worms. Thus, there is a need for the development of new drugs with schistosomicidal activity. The objective of this work was to synthesize and to evaluate the therapeutic potential of new benzodioxole derivatives (3-14) candidates for schistosomicidal drugs. All compounds synthesized showed in vitro schistosomicidal activity. The derivative 12 was considered the best compound, since it took 100% of worms to mortality in the first 72 h of exposure at the concentration of 100 µM and 83.3% at the concentration of 50 µM. Furthermore, male and female adult worms, incubated for 24 h with the compound 12 showed tegument damages characterized by extensive desquamation and edema, tuber destruction, bubble formation and exposure of the muscle layer. This compound has a restricted structure, where the thiazolidinone is attached to the 4-position of the 1,3-benzodioxol ring. The structural conformation of derivative 12 was probably responsible for the promising schistosomicidal activity, where the presence of an electron/conformational restriction of the thiazolidine ring, as well as the action of bromine as a bulk substitute, favored an increase in biological activity. In addition, tegumentary changes caused by derivative 12 may also have been responsible for the death of adult worms of Schistosoma mansoni. Therefore, we verified that the results obtained in this study make benzodioxole derivatives possible candidates for prototypes of new schistosomicidal drugs.
[Mh] Termos MeSH primário: Dioxóis/química
Dioxóis/farmacologia
Schistosoma mansoni/efeitos dos fármacos
Esquistossomicidas/síntese química
Esquistossomicidas/farmacologia
[Mh] Termos MeSH secundário: Animais
Sobrevivência Celular/efeitos dos fármacos
Dioxóis/uso terapêutico
Células HeLa
Seres Humanos
Microscopia Eletrônica de Varredura
Praziquantel/farmacologia
Praziquantel/uso terapêutico
Schistosoma mansoni/ultraestrutura
Esquistossomose/tratamento farmacológico
Esquistossomose/patologia
Esquistossomicidas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dioxoles); 0 (Schistosomicides); 6490C9U457 (Praziquantel); F0XLL582B8 (1,3-benzodioxole)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180126
[St] Status:MEDLINE


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[PMID]:29077723
[Au] Autor:Burnim M; Ivy JA; King CH
[Ad] Endereço:Center for Global Health and Diseases and WHO Collaborating Centre for Research and Training for Schistosomiasis Elimination, Case Western Reserve University School of Medicine, Cleveland, Ohio, United States of America.
[Ti] Título:Systematic review of community-based, school-based, and combined delivery modes for reaching school-aged children in mass drug administration programs for schistosomiasis.
[So] Source:PLoS Negl Trop Dis;11(10):e0006043, 2017 Oct.
[Is] ISSN:1935-2735
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The mainstay of current schistosomiasis control programs is mass preventive chemotherapy of school-aged children with praziquantel. This treatment is delivered through school-based, community-based, or combined school- and community-based systems. Attaining very high coverage rates for children is essential in mass schistosomiasis treatment programs, as is ensuring that there are no persistently untreated subpopulations, a potential challenge for school-based programs in areas with low school enrollment. This review sought to compare the different treatment delivery methods based both on their coverage of school-aged children overall and on their coverage specifically of non-enrolled children. In addition, qualitative community or programmatic factors associated with high or low coverage rates were identified, with suggestions for overall coverage improvement. METHODOLOGY/PRINCIPAL FINDINGS: This review was registered prospectively with PROSPERO (CRD 42015017656). Five hundred forty-nine publication of potential relevance were identified through database searches, reference lists, and personal communications. Eligible studies included those published before October 2015, written in English or French, containing quantitative or qualitative data about coverage rates for MDA of school-aged children with praziquantel. Among the 22 selected studies, combined community- and school-based programs achieved the highest median coverage rates (89%), followed by community-based programs (72%). School-based programs had both the lowest median coverage of children overall (49%) and the lowest coverage of the non-enrolled subpopulation of children. Qualitatively, major factors affecting program success included fear of side effects, inadequate education about schistosomiasis, lack of incentives for drug distributors, and inequitable distribution to minority groups. CONCLUSIONS/SIGNIFICANCE: This review provides an evidence-based framework for the development of future schistosomiasis control programs. Based on our results, a combined community and school-based delivery system should maximize coverage for both in- and out-of-school children, especially when combined with interventions such as snacks for treated children, educational campaigns, incentives for drug distributors, and active inclusion of marginalized groups. TRIAL REGISTRATION: ClinicalTrials.gov CRD42015017656.
[Mh] Termos MeSH primário: Quimioprevenção/métodos
Serviços de Saúde Comunitária
Esquistossomose/prevenção & controle
Esquistossomicidas/uso terapêutico
Instituições Acadêmicas
[Mh] Termos MeSH secundário: Quimioprevenção/estatística & dados numéricos
Criança
Ensaios Clínicos como Assunto
Assistência à Saúde
Transmissão de Doença Infecciosa/prevenção & controle
Esquema de Medicação
Seres Humanos
Praziquantel/uso terapêutico
Esquistossomose/parasitologia
Esquistossomose/transmissão
Esquistossomicidas/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Schistosomicides); 6490C9U457 (Praziquantel)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171119
[Lr] Data última revisão:
171119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171028
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pntd.0006043


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[PMID]:29059190
[Au] Autor:Karanja DMS; Awino EK; Wiegand RE; Okoth E; Abudho BO; Mwinzi PNM; Montgomery SP; Secor WE
[Ad] Endereço:Neglected Tropical Diseases Branch, Centre for Global Health Research, Kenya Medical Research Institute, Kisumu, Kenya.
[Ti] Título:Cluster randomized trial comparing school-based mass drug administration schedules in areas of western Kenya with moderate initial prevalence of Schistosoma mansoni infections.
[So] Source:PLoS Negl Trop Dis;11(10):e0006033, 2017 Oct.
[Is] ISSN:1935-2735
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Mass drug administration (MDA) using praziquantel is the WHO-recommended approach for control of schistosomiasis. However, few studies have compared the impact of different schedules of MDA on the resultant infection levels. We wished to evaluate whether annual MDA was more effective than less frequent treatments for reducing community-level prevalence and intensity of Schistosoma mansoni infections. METHODS: We performed a cluster randomized trial (ISRCTN 14849830) of 3 different MDA frequencies over a 5 year period in 75 villages with moderate (10%-24%) initial prevalence of S. mansoni in school children in western Kenya. Praziquantel was distributed by school teachers to students either annually, the first 2 years, or every other year over a 4 year period. Prevalence and intensity of infection were measured by stool examination in 9-12 year old students using the Kato-Katz method at baseline, each treatment year, and for the final evaluation at year 5. S. mansoni prevalence and intensity were also measured in first year students at baseline and year 5. RESULTS: Twenty-five schools were randomly assigned to each arm. S. mansoni prevalence and infection intensity in 9-12 year old students significantly decreased within each arm from baseline to year 5 but there were no differences between arms. There were no differences in infection levels in first year students either within or between arms. CONCLUSIONS: Strategies employing 2 or 4 rounds of MDA had a similar impact in schools with moderate initial prevalence, suggesting that schistosomiasis control can be sustained by school-based MDA, even if provided only every other year.
[Mh] Termos MeSH primário: Esquema de Medicação
Praziquantel/administração & dosagem
Schistosoma mansoni/efeitos dos fármacos
Esquistossomose mansoni/prevenção & controle
Esquistossomicidas/administração & dosagem
[Mh] Termos MeSH secundário: Animais
Criança
Fezes/parasitologia
Feminino
Seres Humanos
Quênia/epidemiologia
Masculino
Praziquantel/uso terapêutico
Prevalência
Schistosoma mansoni/isolamento & purificação
Esquistossomose mansoni/tratamento farmacológico
Esquistossomose mansoni/epidemiologia
Instituições Acadêmicas
Estudantes
Fatores de Tempo
Organização Mundial da Saúde
[Pt] Tipo de publicação:CLINICAL TRIAL; COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Schistosomicides); 6490C9U457 (Praziquantel)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171119
[Lr] Data última revisão:
171119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171024
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pntd.0006033


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[PMID]:28985236
[Au] Autor:Guidi A; Lalli C; Gimmelli R; Nizi E; Andreini M; Gennari N; Saccoccia F; Harper S; Bresciani A; Ruberti G
[Ad] Endereço:National Research Council, Institute of Cell Biology and Neurobiology, Campus A. Buzzati-Traverso, Monterotondo (Roma), Italy.
[Ti] Título:Discovery by organism based high-throughput screening of new multi-stage compounds affecting Schistosoma mansoni viability, egg formation and production.
[So] Source:PLoS Negl Trop Dis;11(10):e0005994, 2017 Oct.
[Is] ISSN:1935-2735
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Schistosomiasis, one of the most prevalent neglected parasitic diseases affecting humans and animals, is caused by the Platyhelminthes of the genus Schistosoma. Schistosomes are the only trematodes to have evolved sexual dimorphism and the constant pairing with a male is essential for the sexual maturation of the female. Pairing is required for the full development of the two major female organs, ovary and vitellarium that are involved in the production of different cell types such as oocytes and vitellocytes, which represent the core elements of the whole egg machinery. Sexually mature females can produce a large number of eggs each day. Due to the importance of egg production for both life cycle and pathogenesis, there is significant interest in the search for new strategies and compounds not only affecting parasite viability but also egg production. Here we use a recently developed high-throughput organism-based approach, based on ATP quantitation in the schistosomula larval stage of Schistosoma mansoni for the screening of a large compound library, and describe a pharmacophore-based drug selection approach and phenotypic analyses to identify novel multi-stage schistosomicidal compounds. Interestingly, worm pairs treated with seven of the eight compounds identified show a phenotype characterized by defects in eggshell assemblage within the ootype and egg formation with degenerated oocytes and vitelline cells engulfment in the uterus and/or oviduct. We describe promising new molecules that not only impair the schistosomula larval stage but also impact juvenile and adult worm viability and egg formation and production in vitro.
[Mh] Termos MeSH primário: Descoberta de Drogas/métodos
Schistosoma mansoni/efeitos dos fármacos
Schistosoma mansoni/fisiologia
Esquistossomicidas/farmacologia
[Mh] Termos MeSH secundário: Trifosfato de Adenosina/metabolismo
Animais
Feminino
Ensaios de Triagem em Larga Escala/métodos
Seres Humanos
Larva/efeitos dos fármacos
Estágios do Ciclo de Vida/efeitos dos fármacos
Masculino
Oócitos/efeitos dos fármacos
Oócitos/fisiologia
Óvulo/efeitos dos fármacos
Schistosoma mansoni/crescimento & desenvolvimento
Schistosoma mansoni/isolamento & purificação
Esquistossomose mansoni/parasitologia
Bibliotecas de Moléculas Pequenas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Schistosomicides); 0 (Small Molecule Libraries); 8L70Q75FXE (Adenosine Triphosphate)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171007
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pntd.0005994


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[PMID]:28735972
[Au] Autor:El Kouni MH
[Ad] Endereço:Department of Pharmacology and Toxicology, Center for AIDS Research, Comprehensive Cancer Center, General Clinical Research Center, University of Alabama at Birmingham, Birmingham, AL 35294, USA. Electronic address: melkouni@uab.edu.
[Ti] Título:Pyrimidine metabolism in schistosomes: A comparison with other parasites and the search for potential chemotherapeutic targets.
[So] Source:Comp Biochem Physiol B Biochem Mol Biol;213:55-80, 2017 Nov.
[Is] ISSN:1879-1107
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Schistosomes are responsible for the parasitic disease schistosomiasis, an acute and chronic parasitic ailment that affects >240 million people in 70 countries worldwide. It is the second most devastating parasitic disease after malaria. At least 200,000 deaths per year are associated with the disease. In the absence of the availability of vaccines, chemotherapy is the main stay for combating schistosomiasis. The antischistosomal arsenal is currently limited to a single drug, Praziquantel, which is quite effective with a single-day treatment and virtually no host-toxicity. Recently, however, the question of reduced activity of Praziquantel has been raised. Therefore, the search for alternative antischistosomal drugs merits the study of new approaches of chemotherapy. The rational design of a drug is usually based on biochemical and physiological differences between pathogens and host. Pyrimidine metabolism is an excellent target for such studies. Schistosomes, unlike most of the host tissues, require a very active pyrimidine metabolism for the synthesis of DNA and RNA. This is essential for the production of the enormous numbers of eggs deposited daily by the parasite to which the granulomas response precipitates the pathogenesis of schistosomiasis. Furthermore, there are sufficient differences between corresponding enzymes of pyrimidine metabolism from the host and the parasite that can be exploited to design specific inhibitors or "subversive substrates" for the parasitic enzymes. Specificities of pyrimidine transport also diverge significantly between parasites and their mammalian host. This review deals with studies on pyrimidine metabolism in schistosomes and highlights the unique characteristic of this metabolism that could constitute excellent potential targets for the design of safe and effective antischistosomal drugs. In addition, pyrimidine metabolism in schistosomes is compared with that in other parasites where studies on pyrimidine metabolism have been more elaborate, in the hope of providing leads on how to identify likely chemotherapeutic targets which have not been looked at in schistosomes.
[Mh] Termos MeSH primário: Pirimidinas/biossíntese
Schistosoma/metabolismo
Esquistossomose/metabolismo
[Mh] Termos MeSH secundário: Animais
Praziquantel/uso terapêutico
Esquistossomose/tratamento farmacológico
Esquistossomicidas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Pyrimidines); 0 (Schistosomicides); 6490C9U457 (Praziquantel); K8CXK5Q32L (pyrimidine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170915
[Lr] Data última revisão:
170915
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170725
[St] Status:MEDLINE


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[PMID]:28504841
[Au] Autor:Soares MH; Dias HJ; Vieira TM; de Souza MGM; Cruz AFF; Badoco FR; Nicolella HD; Cunha WR; Groppo M; Martins CHG; Tavares DC; Magalhães LG; Crotti AEM
[Ad] Endereço:Núcleo de Pesquisas em Ciências Exatas e Tecnológicas, Universidade de Franca, CEP 14040-600, Franca, SP, Brazil.
[Ti] Título:Chemical Composition, Antibacterial, Schistosomicidal, and Cytotoxic Activities of the Essential Oil of Dysphania ambrosioides (L.) Mosyakin & Clemants (Chenopodiaceae).
[So] Source:Chem Biodivers;14(8), 2017 Aug.
[Is] ISSN:1612-1880
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:We have investigated the chemical composition and the antibacterial activity of the essential oil of Dysphania ambrosioides (L.) Mosyakin & Clemants (Chenopodiaceae) (DA-EO) against a representative panel of cariogenic bacteria. We have also assessed the in vitro schistosomicidal effects of DA-EO on Schistosoma mansoni and its cytotoxicity to GM07492-A cells in vitro. Gas chromatography (GC) and gas chromatography-mass spectrometry (GC/MS) revealed that the monoterpenes cis-piperitone oxide (35.2%), p-cymene (14.5%), isoascaridole (14.1%), and α-terpinene (11.6%) were identified by as the major constituents of DA-EO. DA-EO displayed weak activity against Streptococcus sobrinus and Enterococcus faecalis (minimum inhibitory concentration (MIC) = 1000 µg/ml). On the other hand, DA-EO at 25 and 12.5 µg/ml presented remarkable schistosomicidal action in vitro and killed 100% of adult worm pairs within 24 and 72 h, respectively. The LC values of DA-EO were 6.50 ± 0.38, 3.66 ± 1.06, and 3.65 ± 0.76 µg/ml at 24, 48, and 72 h, respectively. However, DA-EO at concentrations higher than 312.5 µg/ml significantly reduced the viability of GM07492-A cells (IC  = 207.1 ± 4.4 µg/ml). The selectivity index showed that DA-EO was 31.8 times more toxic to the adult S. mansoni worms than GM07492-A cells. Taken together, these results demonstrate the promising schistosomicidal potential of the essential oil of Dysphania ambrosioides.
[Mh] Termos MeSH primário: Chenopodiaceae/química
Óleos Voláteis/química
Óleos Voláteis/farmacologia
Schistosoma mansoni/efeitos dos fármacos
Esquistossomicidas/química
Esquistossomicidas/farmacologia
[Mh] Termos MeSH secundário: Animais
Antibacterianos/química
Antibacterianos/isolamento & purificação
Antibacterianos/farmacologia
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Chenopodiaceae/metabolismo
Enterococcus faecalis/efeitos dos fármacos
Cromatografia Gasosa-Espectrometria de Massas
Seres Humanos
Lactobacillus casei/efeitos dos fármacos
Testes de Sensibilidade Microbiana
Óleos Voláteis/isolamento & purificação
Óleos Voláteis/toxicidade
Esquistossomicidas/isolamento & purificação
Streptococcus/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Oils, Volatile); 0 (Schistosomicides)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170927
[Lr] Data última revisão:
170927
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170516
[St] Status:MEDLINE
[do] DOI:10.1002/cbdv.201700149


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Alves, Luiz Carlos
Texto completo SciELO Brasil
[PMID]:28380119
[Au] Autor:Matos-Rocha TJ; Lima MD; Silva AL; Oliveira JF; Gouveia AL; Silva VB; Almeida AS; Brayner FA; Cardoso PR; Pitta-Galdino MD; Pitta ID; Rêgo MJ; Alves LC; Pitta MG
[Ad] Endereço:Fundação Oswaldo Cruz (Fiocruz/PE), Centro de Pesquisas Aggeu Magalhães, Laboratório de Biologia Celular e Molecular, Recife, Pernambuco, Brazil.
[Ti] Título:Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents.
[So] Source:Rev Inst Med Trop Sao Paulo;59:e8, 2017 Apr 03.
[Is] ISSN:1678-9946
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:Introduction:: Schistosomiasis is an infectious parasitic disease caused by trematodes of the genus Schistosoma, which threatens at least 258 million people worldwide and its control is dependent on a single drug, praziquantel. The aim of this study was to evaluate the anti-Schistosoma mansoni activity in vitro of novel imidazolidine derivatives. Material and methods: : We synthesized two novel imidazolidine derivatives: (LPSF/PTS10) (Z)-1-(2-chloro-6-fluorobenzyl)-4-(4-dimethylaminobenzylidene)-5-thioxoimidazolidin-2-one and (LPSF/PTS23) (Z)-1-(2-chloro-6-fluoro-benzyl)-5-thioxo-4-(2,4,6-trimethoxy-benzylidene)-imidazolidin-2-one. The structures of two compounds were determined by spectroscopic methods. During the biological assays, parameters such as motility, oviposition, mortality and analysis by Scanning Electron Microscopy were performed. Results: : LPSF/PTS10 and LPSF/PTS23 were considered to be active in the separation of coupled pairs, mortality and to decrease the motor activity. In addition, LPSF/PTS23 induced ultrastructural alterations in worms, after 24 h of contact, causing extensive erosion over the entire body of the worms. Conclusion: : The imidazolidine derivatives containing the trimetoxy and benzylidene halogens showed promising in vitro schistosomicidal activity.
[Mh] Termos MeSH primário: Imidazolidinas/farmacologia
Células-Tronco de Sangue Periférico/efeitos dos fármacos
Schistosoma mansoni/efeitos dos fármacos
Esquistossomicidas/farmacologia
[Mh] Termos MeSH secundário: Animais
Seres Humanos
Imidazolidinas/síntese química
Imidazolidinas/toxicidade
Camundongos
Microscopia Eletrônica de Varredura
Testes de Sensibilidade Parasitária
Schistosoma mansoni/ultraestrutura
Esquistossomicidas/síntese química
Esquistossomicidas/toxicidade
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Imidazolidines); 0 (Schistosomicides)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170601
[Lr] Data última revisão:
170601
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170406
[St] Status:MEDLINE


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[PMID]:28373144
[Au] Autor:Aly I; Taher EE; El-Sayed H; Mohammed FA; ELnain G; Hamad RS; Bayoumy EM
[Ad] Endereço:Parasitology Laboratory, Theodor Bilharz Research Institute, Giza, Egypt.
[Ti] Título:Efficacy of soluble glycoprotein fraction from Allium sativum purified by size exclusion chromatography on murine Schistosomiasis mansoni.
[So] Source:Microb Pathog;107:243-248, 2017 Jun.
[Is] ISSN:1096-1208
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In this work, the efficiency of crude MeOH extracts and soluble glycoprotein fraction of Allium sativum purified by size-exclusion chromatography (SEC) on parasitological, histopathological and some biochemical parameters in Schistosoma mansoni infected mice were investigated. Animals were infected by tail immersion with 100 cercariae/each mouse and divided into five groups in addition to the normal control. The results revealed a significant decrease in mean worm burden in all treated mice especially in the group treated with soluble glycoprotein fraction of A. sativum as compared to infected non-treated control with the disappearance of female worms. Administration of the studied extracts revealed remarkable amelioration in the levels of all the measured parameters in S. mansoni infected mice. In addition, treatment of mice with crude A. sativum MeOH extract and soluble glycoprotein fraction of A. sativum decreased significantly the activities of studied enzymes as compared to the infected untreated group. The highest degrees of enhancement in pathological changes was observed in the treated one with soluble glycoprotein fraction of A. sativum compared to the infected group represented by small sized, late fibro-cellular granuloma, the decrease in cellular constituents and degenerative changes in eggs. In conclusion, A. sativum treatment had effective schistosomicidal activities, through reduction of worm burden and tissue eggs, especially when it was given in purified glycoprotein fraction. Moreover, the soluble glycoprotein fraction of A. sativum largely modulates both the size and the number of granulomas.
[Mh] Termos MeSH primário: Cromatografia em Gel/métodos
Alho/química
Glicoproteínas/química
Glicoproteínas/farmacologia
Extratos Vegetais/farmacologia
Schistosoma mansoni/efeitos dos fármacos
Esquistossomose mansoni/tratamento farmacológico
[Mh] Termos MeSH secundário: Fosfatase Alcalina/sangue
Animais
Modelos Animais de Doenças
Feminino
Granuloma/parasitologia
Granuloma/patologia
Fígado/parasitologia
Fígado/patologia
Masculino
Camundongos
Contagem de Ovos de Parasitas
Schistosoma mansoni/patogenicidade
Esquistossomose mansoni/sangue
Esquistossomose mansoni/parasitologia
Esquistossomose mansoni/patologia
Esquistossomicidas/farmacologia
Soro/química
Transaminases/sangue
gama-Glutamiltransferase/sangue
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glycoproteins); 0 (Plant Extracts); 0 (Schistosomicides); EC 2.3.2.2 (gamma-Glutamyltransferase); EC 2.6.1.- (Transaminases); EC 3.1.3.1 (Alkaline Phosphatase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171027
[Lr] Data última revisão:
171027
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170405
[St] Status:MEDLINE


  9 / 1311 MEDLINE  
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Rodrigues, Vanderlei
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[PMID]:27936310
[Au] Autor:Martins MH; Fracarolli L; Vieira TM; Dias HJ; Cruz MG; Deus CC; Nicolella HD; Stefani R; Rodrigues V; Tavares DC; Magalhães LG; Crotti AE
[Ad] Endereço:Núcleo de Pesquisas em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 - Parque Universitário, CEP 14404600, Franca, SP, Brazil.
[Ti] Título:Schistosomicidal Effects of the Essential Oils of Citrus limonia and Citrus reticulata Against Schistosoma mansoni.
[So] Source:Chem Biodivers;14(1), 2017 Jan.
[Is] ISSN:1612-1880
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:We report the in vitro schistosomicidal effects of the essential oil obtained from Citrus limonia leaves (CL-EO) and C. reticulata fruit peels (CR-EO), cultivated in Brazil, against Schistosoma mansoni worms. Limonene (29.9%), ß-pinene (12.0%), sabinene (9.0%), citronellal (9.0%), and citronellol (5.8%) are the major constituents of CL-EO; limonene (26.5%), γ-terpinene (17.2%), linalool (11.1%), octanal (8.0%), myrcene (6.2%), and capraldehyde (3.9%) predominate in CR-EO. CL-EO displayed moderate lethal concentration 50% (LC ) of 81.7 and 38.9 µg/ml against male and female worms at 24 and 72 h, respectively. At concentrations of 25 and 100 µg/ml, CL-EO separated between 50 and 75% of the coupled worm pairs during the evaluated period. CR-EO presented moderate LC of 81.7 µg/ml against male and female worms at 24 and 72 h. However, this oil separated coupled worm pairs more effectively than CL-EO and displayed lower cytotoxicity to GM07492-A cells (IC = 987.7 ± 88.9 µg/ml) as compared to CL-EO (IC = 187.8 ± 2.9 µg/ml). The enantiomers (+)-(R)-limonene and (-)-(S)-limonene did not affect S. mansoni adult worm pairs significantly. Taken together, these data indicate that CL-EO and CR-EO exhibit moderate in vitro schistosomicidal activity against adult S. mansoni worms.
[Mh] Termos MeSH primário: Citrus/química
Óleos Voláteis/farmacologia
Schistosoma mansoni/efeitos dos fármacos
Esquistossomicidas/farmacologia
[Mh] Termos MeSH secundário: Animais
Feminino
Frutas
Masculino
Óleos Voláteis/análise
Folhas de Planta/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Oils, Volatile); 0 (Schistosomicides)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170127
[Lr] Data última revisão:
170127
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161210
[St] Status:MEDLINE
[do] DOI:10.1002/cbdv.201600194


  10 / 1311 MEDLINE  
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[PMID]:27454107
[Au] Autor:Kang NX; Zhu YJ; Zhao JP; Zhu WF; Liu YL; Xu QM; Zhuge HX; Khan IA; Yang SL
[Ad] Endereço:a School of Biology & Basic Medical Science , Soochow University , Suzhou 215123 , China.
[Ti] Título:Antischistosomal activity of hederacochiside C against Schistosoma japonicum harbored in experimentally infected animals.
[So] Source:J Asian Nat Prod Res;19(4):402-415, 2017 Apr.
[Is] ISSN:1477-2213
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The present study was undertaken to investigate whether hederacochiside C (HSC) possesses antischistosomal effects and anti-inflammatory response activities in Schistosoma japonicum-infected mice. Different concentrations of HSC were administrated to the mice infected by schistosomula or adult worm by intravenous injection twice a day for five consecutive days. The total worm burden, female worm burden, and the egg burden in liver of mice treated with 400 mg/kg HSC were fewer than those in non-treated ones. Murine immune responses following HSC treatment were investigated using enzyme-linked immunosorbent assays (ELISA). Our results indicated that 200 mg/kg HSC could reduce the expression of IgG, tumor necrosis factor (TNF)-α, interleukin (IL)-4 and IL-17 in comparison to infected group, exhibiting best immunomodulatory effects. In addition, scanning electron microscopical examination revealed that male worms treated with HSC lost their normal surface architecture since its surface showed extensive swelling, erosion, and peeling in tegumental regions. Remarkable amelioration was noticed in histopathological investigations, and 200 mg/kg HSC treatment could reduce the size of granulomatous inflammatory infiltrations in the liver which was reflected in nearly normalization of liver architecture. These results suggested that HSC had potential antischistosomal activity and provided a basis for subsequent experimental.
[Mh] Termos MeSH primário: Anti-Inflamatórios/isolamento & purificação
Anti-Inflamatórios/farmacologia
Saponinas/isolamento & purificação
Saponinas/farmacologia
Schistosoma japonicum/efeitos dos fármacos
Esquistossomicidas/isolamento & purificação
Esquistossomicidas/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/química
Feminino
Seres Humanos
Imunoglobulina G/efeitos dos fármacos
Interleucina-17/metabolismo
Interleucina-4/metabolismo
Fígado/patologia
Masculino
Camundongos
Estrutura Molecular
Saponinas/química
Esquistossomicidas/química
Fator de Necrose Tumoral alfa/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Immunoglobulin G); 0 (Interleukin-17); 0 (Saponins); 0 (Schistosomicides); 0 (Tumor Necrosis Factor-alpha); 0 (hederacochiside C); 207137-56-2 (Interleukin-4)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170412
[Lr] Data última revisão:
170412
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160726
[St] Status:MEDLINE
[do] DOI:10.1080/10286020.2016.1208181



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