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[PMID]:28867456
[Au] Autor:He W; Yang C; Zhao X; Wang Y
[Ad] Endereço:Key Laboratory of Biotechnology of Antibiotics, The National Health and Family Planning Commission (NHFPC), Institute of Medicinal Biotechnology, No. 1 Tian Tan Xi Li, Beijing 100050, PR China.
[Ti] Título:Antimicrobial activity of bitespiramycin, a new genetically engineered macrolide.
[So] Source:Bioorg Med Chem Lett;27(19):4576-4577, 2017 10 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The antimicrobial activity of bitespiramycin (BT) against Chlamydia trachomatis (Ct), Chlamydia pneumoniae (Cp), Ureaplasma urealyticum (Uu), and Mycoplasma pneumoniae (Mp), was compared with those of azithromycin (AZM) and acetylspiramycin (AT-SP) in vitro. Furthermore, the anti-Mp activities of BT and AZM were evaluated in a hamster model. The activities of BT in vitro were similar to those of AZM but were more effective than those of AT-SP. BT effectively inhibited Mp infection at a dose of 200mg/kg in a hamster model.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Chlamydia trachomatis/efeitos dos fármacos
Chlamydophila pneumoniae/efeitos dos fármacos
Mycoplasma pneumoniae/efeitos dos fármacos
Espiramicina/análogos & derivados
Ureaplasma urealyticum/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Relação Dose-Resposta a Droga
Testes de Sensibilidade Microbiana
Espiramicina/síntese química
Espiramicina/química
Espiramicina/farmacologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (bitespiramycin); 8025-81-8 (Spiramycin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170905
[St] Status:MEDLINE


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Mineo, José Roberto
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[PMID]:28803905
[Au] Autor:Ribeiro M; Franco PS; Lopes-Maria JB; Angeloni MB; Barbosa BF; Gomes AO; Castro AS; Silva RJD; Oliveira FC; Milian ICB; Martins-Filho OA; Ietta F; Mineo JR; Ferro EAV
[Ad] Endereço:Laboratory of Immunophysiology of Reproduction, Department of Histology and Embryology, Federal University of Uberlândia, Av. Pará, 1720, Uberlândia, CEP 38400 902, Brazil.
[Ti] Título:Azithromycin treatment is able to control the infection by two genotypes of Toxoplasma gondii in human trophoblast BeWo cells.
[So] Source:Exp Parasitol;181:111-118, 2017 Oct.
[Is] ISSN:1090-2449
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Trophoblast infection by Toxoplasma gondii plays a pivotal role in the vertical transmission of toxoplasmosis. Here, we investigate whether the antibiotic therapy with azithromycin, spiramycin and sulfadiazine/pyrimethamine are effective to control trophoblast infection by two Brazilian T. gondii genotypes, TgChBrUD1 or TgChBrUD2. Two antibiotic protocols were evaluated, as follow: i) pre-treatment of T. gondii-tachyzoites with selected antibiotics prior trophoblast infection and ii) post-treatment of infected trophoblasts. The infection index/replication and the impact of the antibiotic therapy on the cytokine milieu were characterized. It was observed that TgChBrUD2 infection induced lower infection index/replication as compared to TgChBrUD1. Regardless the therapeutic protocol, azithromycin was more effective to control the trophoblast infection with both genotypes when compared to conventional antibiotics. Azithromycin induced higher IL-12 production in TgChBrUD1-infected cells that may synergize the anti-parasitic effect. In contrast, the effectiveness of azithromycin to control the TgChBrUD2-infection was not associated with the IL-12 production. BeWo-trophoblasts display distinct susceptibility to T. gondii genotypes and the azithromycin treatment showed to be more effective than conventional antibiotics to control the T. gondii infection/replication regardless the parasite genotype.
[Mh] Termos MeSH primário: Antiprotozoários/farmacologia
Azitromicina/farmacologia
Toxoplasma/efeitos dos fármacos
Trofoblastos/parasitologia
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Citocinas/metabolismo
Combinação de Medicamentos
Genótipo
Seres Humanos
Interleucina-12/metabolismo
Pirimetamina/farmacologia
Espiramicina/farmacologia
Sulfadiazina/farmacologia
Toxoplasma/classificação
Toxoplasma/genética
Toxoplasma/imunologia
Trofoblastos/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiprotozoal Agents); 0 (Cytokines); 0 (Drug Combinations); 0N7609K889 (Sulfadiazine); 187348-17-0 (Interleukin-12); 8025-81-8 (Spiramycin); 83905-01-5 (Azithromycin); Z3614QOX8W (Pyrimethamine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170815
[St] Status:MEDLINE


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[PMID]:28391938
[Au] Autor:Sacco O; Vaiano V; Sannino D; Ciambelli P
[Ad] Endereço:University of Salerno, Department of Industrial Engineering, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
[Ti] Título:Visible light driven mineralization of spiramycin over photostructured N-doped TiO on up conversion phosphors.
[So] Source:J Environ Sci (China);54:268-276, 2017 Apr.
[Is] ISSN:1001-0742
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A novel visible light-active photocatalyst formulation (NdT/OP) was obtained by supporting N-doped TiO (NdT) particles on up-conversion luminescent organic phosphors (OP). The photocatalytic activity of such catalysts was evaluated for the mineralization process of spiramycin in aqueous solution. The effect of NdT loading in the range 15-60wt.% on bulk and surface characteristics of NdT/OP catalysts was investigated by several chemico-physical characterization techniques. The photocatalytic performance of NdT/OP catalysts in the removal of spyramicin from aqueous solution was assessed through photocatalytic tests under visible light irradiation. Total organic carbon (TOC) of aqueous solution, and CO and CO gas concentrations evolved during the photodegradation were analyzed. A dramatic enhancement of photocatalytic activity of the photostructured visible active NdT/OP catalysts, compared to NdT catalyst, was observed. Only CO was detected in gas-phase during visible light irradiation, proving that the photocatalytic process is effective in the mineralization of spiramycin, reaching very high values of TOC removal. The photocatalyst NdT/OP at 30wt.% of NdT loading showed the highest photocatalytic activity (58% of TOC removed after 180min irradiation against only 31% removal after 300min of irradiation of NdT). We attribute this enhanced activity to the high effectiveness in the utilization of visible light through improved light harvesting and exploiting. OP particles act as "photoactive support", able to be excited by the external visible light irradiation, and reissue luminescence of wavelength suitable to promote NdT photomineralization activity.
[Mh] Termos MeSH primário: Antibacterianos/química
Nitrogênio/química
Espiramicina/química
Titânio/química
Poluentes Químicos da Água/química
[Mh] Termos MeSH secundário: Cinética
Luz
Modelos Químicos
Fotólise
Raios Ultravioleta
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Water Pollutants, Chemical); 15FIX9V2JP (titanium dioxide); 8025-81-8 (Spiramycin); D1JT611TNE (Titanium); N762921K75 (Nitrogen)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170421
[Lr] Data última revisão:
170421
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170411
[St] Status:MEDLINE


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[PMID]:28278108
[Au] Autor:Li Z; Hu F; Ye R; Lv H; Zeng J
[Ad] Endereço:a The State Key Laboratory of Bioreactor Engineering , East China University of Science and Technology , Shanghai , China.
[Ti] Título:Influence of Al on the titer of spiramycin and effective components in fermentor.
[So] Source:Prep Biochem Biotechnol;47(5):481-488, 2017 May 28.
[Is] ISSN:1532-2297
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Spiramycin is a multicomponent antibiotic, and different components have different antibacterial activities. In Streptomyces spiramyceticus 16-10-2, spiramycin II and spiramycin III (SPMII and SPMIII) are the main components, while spiramycin I (SPMI) needs to be controlled below 12%. Based on this, the influences of Al on total spiramycin titer and components were investigated in this work. Those experiments were mainly performed in 15 L fermentor and Al made a great improvement in spiramycin titer. The optimal adding concentration and adding time of Al were 0.32 g/L at 12 hr. Under this condition, spiramycin titer was increased by 19.51% compared with the control. Moreover, the percentage of SPMII and SPMIII was increased by 7.14%. At the same time, the time of mycelia autolysis was lengthened. In addition, the specific activities of acetyl-CoA synthetase, acetate kinase, acetylphosphotransferase, and acylating enzyme were much higher than those of control. The content of acetic acid and succinic acid was beyond 3 and 4.5 times than that of control, respectively.
[Mh] Termos MeSH primário: Alumínio/metabolismo
Antibacterianos/metabolismo
Espiramicina/metabolismo
Streptomyces/metabolismo
[Mh] Termos MeSH secundário: Acilação
Aminoglicosídeos/metabolismo
Reatores Biológicos
Cátions/metabolismo
Fermentação
Microbiologia Industrial
Espiramicina/análogos & derivados
Streptomyces/enzimologia
Streptomyces/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aminoglycosides); 0 (Anti-Bacterial Agents); 0 (Cations); 033ECH6IFG (demycarosylturimycin H); 05298J5WMU (acetylspiramycin); 0NHE9TRJ93 (spiramycin III); 8025-81-8 (Spiramycin); CPD4NFA903 (Aluminum)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171006
[Lr] Data última revisão:
171006
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170310
[St] Status:MEDLINE
[do] DOI:10.1080/10826068.2017.1292290


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[PMID]:28236765
[Au] Autor:Chen S; Liu Y; Zhang J; Gao B
[Ad] Endereço:Shandong Provincial Key Laboratory of Water Pollution Control and Resource Reuse, School of Environmental Science and Engineering, Shandong University, Jinan, 250100, PR China.
[Ti] Título:iTRAQ-based quantitative proteomic analysis of Microcystis aeruginosa exposed to spiramycin at different nutrient levels.
[So] Source:Aquat Toxicol;185:193-200, 2017 Apr.
[Is] ISSN:1879-1514
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Research on the combined effects of antibiotic contaminants and environmental factors in cyanobacteria is still limited. This study focused on the action and its mechanism of spiramycin combined with changes in nitrogen and phosphorus level in Microcystis aeruginosa at environmentally relevant concentrations. Though photosynthetic activity was stimulated by spiramycin at a high nutrient level, no significant correlation (p>0.05) was found between photosynthesis-related proteins and growth-related proteins, and the growth rate was inhibited by 200ngL of spiramycin. At low nitrogen and low phosphorus levels, up-regulated photosynthesis-related proteins were closely correlated with (p<0.05) stress response-related, transcription-related and cell division-related proteins, which consequently led to stimulated growth of M. aeruginosa under spiramycin exposure. Spiramycin exposure also regulated the production of microcystins (MCs) and the expression of two microcystin synthetases (mcyB and mcyC). The spiramycin-induced protein secretion process and the up-regulation of ATP binding cassette transporters might contribute to the increased MC release. Enolase, superoxide dismutase, protein GrpE, DNA-directed RNA polymerase subunit alpha and serine protease were candidate target proteins of spiramycin in M. aeruginosa under different nutrient conditions. Coexisting spiramycin mitigated the threat of cyanobacteria to aquatic environments at a high nutrient level but aggravated cyanobacterial bloom at a low nitrogen level.
[Mh] Termos MeSH primário: Marcação por Isótopo/métodos
Microcystis/metabolismo
Proteômica/métodos
Espiramicina/toxicidade
[Mh] Termos MeSH secundário: Análise por Conglomerados
Microcistinas/biossíntese
Microcystis/citologia
Microcystis/efeitos dos fármacos
Microcystis/crescimento & desenvolvimento
Mapas de Interação de Proteínas
Espiramicina/análise
Poluentes Químicos da Água/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Microcystins); 0 (Water Pollutants, Chemical); 77238-39-2 (microcystin); 8025-81-8 (Spiramycin)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170515
[Lr] Data última revisão:
170515
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170226
[St] Status:MEDLINE


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[PMID]:27979264
[Au] Autor:García Mayor MA; Paniagua González G; Garcinuño Martínez RM; Fernández Hernando P; Durand Alegría JS
[Ad] Endereço:Department of Analytical Sciences, Faculty of Sciences, National University of Distance, 28040 Madrid, Spain.
[Ti] Título:Synthesis and characterization of a molecularly imprinted polymer for the determination of spiramycin in sheep milk.
[So] Source:Food Chem;221:721-728, 2017 Apr 15.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of molecularly imprinted polymers (MIPs) comprising reactionary sites which are complementary to macrolide antibiotic spiramycin (SPI) were synthetized by noncovalent bulk polymerization technique. MIPs were synthesized under different polymerization process and their recognition efficiency was evaluated in binding studies in comparison with non-imprinted polymers. The best MIP was morphologically characterized and equilibrium assays were carried out. The MIP was evaluated as a sorbent for extraction and preconcentration of SPI from aqueous and sheep milk samples, and an off-line MISPE method followed by high-performance liquid chromatography with UV diode-array detection was established. Good linearity were obtained for SPI in a range of 24-965µgkg and the average recoveries at three spiked levels in milk samples were higher than 90% (RSD<5%). Limit of quantification was 24.1µgkg . Cross-reactivity studies from other macrolides with similar structure were tested. The optimum imprinted polymer showed a good selectivity and affinity for SPI, demonstrating the potential of the proposed MISPE for rapid, sensitive and effective sample pretreatment for selective determination of SPI in sheep milk samples.
[Mh] Termos MeSH primário: Antibacterianos/análise
Leite/química
Impressão Molecular/métodos
Polímeros/química
Espiramicina/análise
[Mh] Termos MeSH secundário: Animais
Polímeros/síntese química
Ovinos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Polymers); 8025-81-8 (Spiramycin)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:171003
[Lr] Data última revisão:
171003
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161217
[St] Status:MEDLINE


  7 / 495 MEDLINE  
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PubMed Central Texto completo
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[PMID]:27542116
[Au] Autor:Borkowski PK; Brydak-Godowska J; Basiak W; Switaj K; Zarnowska-Prymek H; Olszynska-Krowicka M; Kajfasz P; Rabczenko D
[Ad] Endereço:Former Department of Zoonoses and Tropical Diseases, Medical University of Warsaw, Poland, present Department of Infectious, Tropical Diseases and Hepatology, Medical University of Warsaw, Poland.
[Ti] Título:The Impact of Short-Term, Intensive Antifolate Treatment (with Pyrimethamine and Sulfadoxine) and Antibiotics Followed by Long-Term, Secondary Antifolate Prophylaxis on the Rate of Toxoplasmic Retinochoroiditis Recurrence.
[So] Source:PLoS Negl Trop Dis;10(8):e0004892, 2016 Aug.
[Is] ISSN:1935-2735
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To assess the impact of intensive antifolate treatment, followed by secondary antifolate prophylaxis (A-SP) on the recurrence rate of toxoplasmic retinochoroiditis (TRC). To investigate whether there are any other factors potentially predisposing for recurrence. MATERIAL AND METHODS: A total of 637 medical records of TRC patients, who had been treated in the years 1994-2013 were reviewed. All patients were treated with pyrimethamine /sulfadoxine one 25mg/500mg tablet daily (P/S 25/500mg) for 21 days with a double loading dose for the first two days. From Day 2 the patients also received prednisone at a starting dose of 40mg and spiramycine 3 million IU three times daily, given for 10 days followed by azithromycin 500mg once daily for another 6 days. The analysis of the recurrence rate involved 352 patients who had completed 6-month secondary prophylaxis (P/S one 25 mg/500mg tablet twice a week). RESULTS: When secondary antifolate prophylaxis (A-SP) was instituted immediately after the treatment for TRC, the probability of 3-year recurrence-free survival after the first course of A-SP was 90.9%. A recurrence was most likely approximately 3.5 years after the first treatment. A univariate Cox regression model demonstrated that a risk for recurrence was 2.82 times higher (p = 0.02) in patients with retinal scars. In the multivariate analysis, the risk for recurrence was 2.41 higher (p = 0.06). In patients with haemorrhagic lesions the risk for recurrence was lower, aRR = 0.17 (approaching borderline statistical significance p = 0.08). CONCLUSIONS: With the institution of A-SP of immediately after the intensive treatment for TRC, i.e. when a reactivation was most likely, there was no recurrence during A-SP. Following A-SP the recurrence rates were low and recurrence-free periods tended to be longer. The treatment regimen employed had a beneficial effect on the recurrence interval as it reduced and delayed the highest probability of recurrence.
[Mh] Termos MeSH primário: Antagonistas do Ácido Fólico/uso terapêutico
Pirimetamina/uso terapêutico
Sulfadoxina/uso terapêutico
Toxoplasmose Ocular/tratamento farmacológico
Toxoplasmose Ocular/prevenção & controle
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Idoso de 80 Anos ou mais
Anti-Inflamatórios/uso terapêutico
Coccidiostáticos/administração & dosagem
Coccidiostáticos/uso terapêutico
Esquema de Medicação
Quimioterapia Combinada
Feminino
Antagonistas do Ácido Fólico/administração & dosagem
Seres Humanos
Masculino
Registros Médicos
Meia-Idade
Prednisona/administração & dosagem
Prednisona/uso terapêutico
Pirimetamina/administração & dosagem
Recidiva
Prevenção Secundária/métodos
Espiramicina/administração & dosagem
Espiramicina/uso terapêutico
Sulfadoxina/administração & dosagem
Toxoplasmose Ocular/etiologia
Toxoplasmose Ocular/parasitologia
Resultado do Tratamento
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Coccidiostats); 0 (Folic Acid Antagonists); 8025-81-8 (Spiramycin); 88463U4SM5 (Sulfadoxine); VB0R961HZT (Prednisone); Z3614QOX8W (Pyrimethamine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170720
[Lr] Data última revisão:
170720
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160820
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pntd.0004892


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[PMID]:27501415
[Au] Autor:Klich K; Pyta K; Kubicka MM; Ruszkowski P; Celewicz L; Gajecka M; Przybylski P
[Ad] Endereço:Faculty of Chemistry, Adam Mickiewicz University , Umultowska 89b, 61-614 Poznan, Poland.
[Ti] Título:Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
[So] Source:J Med Chem;59(17):7963-73, 2016 Sep 08.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Huisgen cycloaddition allowed obtaining of novel triazole-bridged antibiotics (6-16) with the reconstructed C(5) arm of spiramycin. (1)H-(1)H NOESY couplings indicated the structure of novel derivatives in solution and demonstrated that the rebuilt C(5) arm is slightly differently oriented relative to the aglycone part if compared to that of spiramycin (1). Combined analysis of biological data together with experimentally determined lipophilicity (clogP) and solubility show the importance of the chemical nature of the newly introduced triazole C(5) arm in the presence of attractive antibacterial and anticancer potency. The most cytotoxic active triazole conjugates having a hydrophobic and bulky C(5) arm showed higher selectivity toward cancer cell lines (HeLa, KB, MCF-7, Hep-G2, and U87) relative to HDF normal cells than that of the parent spiramycin. Our studies have demonstrated that the aldehyde group is not crucial for the presence of interesting antibacterial [MIC(S. pneumoniae) ∼ 1.2 µM] and anticancer [IC50(HepG2) ∼ 6 µM] properties of 16-membered lactone macrolides based on spiramycin's aglycone.
[Mh] Termos MeSH primário: Antibacterianos/química
Antineoplásicos/química
Espiramicina/análogos & derivados
Espiramicina/química
Triazóis/química
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/farmacologia
Antineoplásicos/síntese química
Antineoplásicos/farmacologia
Linhagem Celular Tumoral
Reação de Cicloadição
Ensaios de Seleção de Medicamentos Antitumorais
Bactérias Gram-Positivas/efeitos dos fármacos
Seres Humanos
Testes de Sensibilidade Microbiana
Modelos Moleculares
Solubilidade
Espiramicina/síntese química
Espiramicina/farmacologia
Relação Estrutura-Atividade
Termodinâmica
Triazóis/síntese química
Triazóis/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antineoplastic Agents); 0 (Triazoles); 8025-81-8 (Spiramycin)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170713
[Lr] Data última revisão:
170713
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160809
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.6b00764


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[PMID]:27398599
[Au] Autor:Kim MO; Ryu HW; Choi JH; Son TH; Oh SR; Lee HS; Yuk HJ; Cho S; Kang JS; Lee CW; Lee J; Lee CK; Hong ST; Lee SU
[Ad] Endereço:Natural Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology, 30 Yeongudanji-ro, Ochang, Cheongju, Chungbuk, 28116, Korea.
[Ti] Título:Anti-Obesity Effects of Spiramycin In Vitro and In Vivo.
[So] Source:PLoS One;11(7):e0158632, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The effects of spiramycin on adipogenesis and high fat diet (HFD)-induced obesity were investigated. Potential mechanisms contributing to these effects were elucidated. The inhibitory effect of spiramycin on adipocyte differentiation was assessed using 3T3-L1 preadipocyte cells, in which several parameters involved in AMPK signal pathways and lipid metabolism were examined. To further investigate the pharmacological effects of spiramycin in vivo, we examined several obesity-related parameters in HFD-induced obese mice. Spiramycin significantly inhibited preadipocyte differentiation by attenuating intracellular lipid accumulation. Spiramycin also reduced the expression of adipogenic master regulators (PPARγ, C/EBPα, and SREBP1c) and their downstream target genes (FAS, aP2, and GLUT4) in 3T3-L1 cells. In addition, AMPK phosphorylation was increased by spiramycin treatment in 3T3-L1 cells during early differentiation. Notably, HFD-induced obese mice administered spiramycin showed substantial decreases in body weight gain, serum leptin levels, adipose tissue mass, and hepatic lipid accumulation. Moreover, the decreased levels of GPT and GOT in the serum indicated that spiramycin attenuated hepatic injury caused by HFD. Taken together, these results demonstrate for the first time that spiramycin effectively attenuates HFD-induced obesity and hepatic steatosis by inhibiting adipogenesis.
[Mh] Termos MeSH primário: Fármacos Antiobesidade/farmacologia
Obesidade/tratamento farmacológico
Espiramicina/farmacologia
[Mh] Termos MeSH secundário: Células 3T3-L1
Proteínas Quinases Ativadas por AMP/metabolismo
Adipogenia/efeitos dos fármacos
Animais
Fármacos Antiobesidade/uso terapêutico
Proteína alfa Estimuladora de Ligação a CCAAT/genética
Dieta Hiperlipídica/efeitos adversos
Regulação da Expressão Gênica/efeitos dos fármacos
Metabolismo dos Lipídeos/efeitos dos fármacos
Camundongos
Camundongos Endogâmicos C57BL
Obesidade/etiologia
Obesidade/metabolismo
Obesidade/patologia
PPAR gama/genética
Espiramicina/uso terapêutico
Proteína de Ligação a Elemento Regulador de Esterol 1/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Obesity Agents); 0 (CCAAT-Enhancer-Binding Protein-alpha); 0 (PPAR gamma); 0 (Sterol Regulatory Element Binding Protein 1); 8025-81-8 (Spiramycin); EC 2.7.11.31 (AMP-Activated Protein Kinases)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160712
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0158632


  10 / 495 MEDLINE  
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Fotocópia
[PMID]:27363037
[Au] Autor:Ismail HI; Sheir HT
[Ti] Título:IMMUNOTHERAPEUTIC EFFECT OF SPIRAMYCIN IN EXPERIMENTAL GIARDIASIS.
[So] Source:J Egypt Soc Parasitol;46(1):19-25, 2016 Apr.
[Is] ISSN:1110-0583
[Cp] País de publicação:Egypt
[La] Idioma:eng
[Ab] Resumo:Giardiasis is a major global cause of water borne diarrheal disease, which contributes greatly to the burden of malnutrition and malabsorption especially in children. There is a great demand for a new effective therapeutic agent against giardiasis that can be used safely during pregnancy, lactation and in infants. In the present study, the therapeutic effect of spiramycin as well as its immunomodulatory mechanism of action in giardiasis had been investigated. 90 Swiss albino mice were used in this study and classified into 3 groups: GI: 40 mice infected with Giardia lamblia cysts, GII: 40 infected mice that received spiramycin treatment in a daily oral dose of 1000 IU/gm body weight for one week starting one week post infection and GIII: 10 control uninfected untreated mice. 20 mice from each infected group were sacrificed 2 weeks post infection (p.i.) and the remaining mice were sacrificed 4 weeks p.i. Mice of the control groups were sacrificed at one time. The antigiardial therapeutic efficacy of spiramycin was assessed 2 and 4 weeks p.i. by counting of Giardia cysts in stool of mice and studying the histopathological changes and disaccharidase activity in small intestine of mice of different groups. Significant reduction in cysts number shedded in stool of treated animals reached 95.73%. The histopathological changes were mild in all infected groups 2 weeks p.i., while 4 weeks p.i. There was also a significant increase in the number of IELs in treated groups denoting the stimulatory effect of spiramycin on lymphocytic proliferation. On studying the disaccharidase activity, there was significant increase in both sucrase and maltase activities in the treated groups as compared with the nontreated groups. The possible immunomodulatory mechanism of action of spiramycin was studied by measuring the local IgA deposition in small intestinal mucosa by PAP technique 4 weeks p.i. The levels of IgA in small intestine were higher in SP-treated group as compared with the non-treated group. The present results suggested that spiramycin has high efficacy as anti-giardial agent possibly by stimulation of local IgA production.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Giardíase/tratamento farmacológico
Espiramicina/farmacologia
[Mh] Termos MeSH secundário: Animais
Giardia lamblia
Giardíase/parasitologia
Camundongos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 8025-81-8 (Spiramycin)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:160701
[Lr] Data última revisão:
160701
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160702
[St] Status:MEDLINE



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