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  1 / 907 MEDLINE  
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[PMID]:29274217
[Au] Autor:Szymczak J; Kozlowska J; Doligalska M
[Ad] Endereço:Department of Parasitology, Faculty of Biology, University of Warsaw, ul. Miecznikowa 1, 02-096 Warsaw, Poland
[Ti] Título:Evaluation of inhibitory effect of redox-active antimalarial drug against Babesia microti in mice
[So] Source:Ann Parasitol;63(3):223­227, 2017.
[Is] ISSN:2299-0631
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:Babesiosis is an emerging, tick-transmitted disease caused by the intraerythrocytic parasite Babesia microti. In immunocompetent individuals, B. microti infection quickly resolves after antibabesial treatment. Immunocompromised patients and those of advanced age experience chronic and relapsing babesiosis, accompanied by severe complications and often, a fatal outcome. In these individuals, B. microti infection may persist despite multiple courses of treatment with antiprotozoal drugs. The increasing incidence of human babesiosis caused by B. microti, coupled with a growing number of immunosuppressed people who do not respond to standard antibabesial therapy, emphasises the need for new therapeutics for this protozoan infection with more effective mechanisms of action. Plasmodione, namely 3-[4-(trifluoromethyl)benzyl]-menadione, acts as a redox cycler and disrupts the redox homeostasis of Plasmodium-infected erythrocytes. The present study was designed to evaluate the potential inhibitory effect of this novel antimalarial compound against intraerythrocytic stages of B. microti in mice. Our results demonstrate that plasmodione did not reduce the level of parasitemia in B. microti-infected mice, indicating that interfering with the parasite redox balance is not an effective strategy to restrict the division of this protozoan. The mechanism of parasite resistance to plasmodione may be based on the differences in the oxidative metabolisms of Babesia and Plasmodium parasites inside infected erythrocytes. The significance of our results is discussed in relation to the development of novel antibabesial drugs based on redox-active benzylmenadiones.
[Mh] Termos MeSH primário: Antimaláricos/uso terapêutico
Babesia microti
Babesiose/tratamento farmacológico
Vitamina K 3/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Antimaláricos/farmacologia
Babesiose/parasitologia
Camundongos
Oxirredução
Vitamina K 3/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-(4-(trifluoromethyl)benzyl)menadione); 0 (Antimalarials); 723JX6CXY5 (Vitamin K 3)
[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:171224
[St] Status:MEDLINE
[do] DOI:10.17420/ap6303.109


  2 / 907 MEDLINE  
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[PMID]:27776223
[Au] Autor:Zhang Q; Wang Z; Hou F; Harding R; Huang X; Dong A; Walker JR; Tong Y
[Ad] Endereço:Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
[Ti] Título:The substrate binding domains of human SIAH E3 ubiquitin ligases are now crystal clear.
[So] Source:Biochim Biophys Acta;1861(1 Pt A):3095-3105, 2017 01.
[Is] ISSN:0006-3002
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Seven in absentia homologs (SIAHs) comprise a family of highly conserved E3 ubiquitin ligases that play an important role in regulating signalling pathways in tumorigenesis, including the DNA damage repair and hypoxia response pathways. SIAH1 and SIAH2 have been found to function as a tumour repressor and a proto-oncogene, respectively, despite the high sequence identity of their substrate binding domains (SBDs). Ubiquitin-specific protease USP19 is a deubiquitinase that forms a complex with SIAHs and counteracts the ligase function. Much effort has been made to find selective inhibitors of the SIAHs E3 ligases. Menadione was reported to inhibit SIAH2 specifically. METHODS: We used X-ray crystallography, peptide array, bioinformatic analysis, and biophysical techniques to characterize the structure and interaction of SIAHs with deubiquitinases and literature reported compounds. RESULTS: We solved the crystal structures of SIAH1 in complex with a USP19 peptide and of the apo form SIAH2. Phylogenetic analysis revealed the SIAH/USP19 complex is conserved in evolution. We demonstrated that menadione destabilizes both SIAH1 and SIAH2 non-specifically through covalent modification. CONCLUSIONS: The SBDs of SIAH E3 ligases are structurally similar with a subtle stability difference. USP19 is the only deubiquitinase that directly binds to SIAHs through the substrate binding pocket. Menadione is not a specific inhibitor for SIAH2. GENERAL SIGNIFICANCE: The crystallographic models provide structural insights into the substrate binding of the SIAH family E3 ubiquitin ligases that are critically involved in regulating cancer-related pathways. Our results suggest caution should be taken when using menadione as a specific SIAH2 inhibitor.
[Mh] Termos MeSH primário: Proteínas Nucleares/química
Ubiquitina-Proteína Ligases/química
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Carcinogênese/metabolismo
Carcinogênese/patologia
Cristalografia por Raios X
Endopeptidases/metabolismo
Evolução Molecular
Seres Humanos
Modelos Moleculares
Proteínas Nucleares/antagonistas & inibidores
Filogenia
Ligação Proteica
Domínios Proteicos
Estabilidade Proteica/efeitos dos fármacos
Estrutura Secundária de Proteína
Especificidade por Substrato/efeitos dos fármacos
Ubiquitina-Proteína Ligases/antagonistas & inibidores
Vitamina K 3/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Nuclear Proteins); 723JX6CXY5 (Vitamin K 3); EC 2.3.2.27 (Ubiquitin-Protein Ligases); EC 2.3.2.27 (seven in absentia proteins); EC 3.4.- (Endopeptidases); EC 3.4.- (USP19 protein, human)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171224
[Lr] Data última revisão:
171224
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161107
[St] Status:MEDLINE


  3 / 907 MEDLINE  
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[PMID]:28858751
[Au] Autor:Yuan TF; Wang ST; Li Y
[Ad] Endereço:Department of Clinical Laboratory, Renmin Hospital of Wuhan University, Wuhan 430060, China.
[Ti] Título:Quantification of menadione from plasma and urine by a novel cysteamine-derivatization based UPLC-MS/MS method.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1063:107-111, 2017 Sep 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Menadione, as the crucial component of vitamin Ks, possessed significant nutritional and clinical values. However, there was still lack of favourable quantification strategies for it to date. For improvement, a novel cysteamine derivatization based UPLC-MS/MS method was presented in this work. The derivatizating reaction was proved non-toxic, easy-handling and high-efficient, which realized the MS detection of menadione under positive mode. Benefitting from the excellent sensitivity of the derivatizating product as well as the introduction of the stable isotope dilution technique, the quantification could be achieved in the range of 0.05-50.0ng/mL for plasma and urine matrixes with satisfied accuracy and precision. After analysis of the samples from healthy volunteers after oral administration of menadione sodium bisulfite tablets, the urinary free menadione was quantified for the very first time. We believe the progress in this work could largely promote the exploration of the metabolic mechanism of vitamin K in vivo.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Cisteamina/química
Espectrometria de Massas em Tandem/métodos
Vitamina K 3/sangue
Vitamina K 3/urina
[Mh] Termos MeSH secundário: Seres Humanos
Modelos Lineares
Reprodutibilidade dos Testes
Sensibilidade e Especificidade
Vitamina K 3/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
5UX2SD1KE2 (Cysteamine); 723JX6CXY5 (Vitamin K 3)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170901
[St] Status:MEDLINE


  4 / 907 MEDLINE  
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[PMID]:28751209
[Au] Autor:Gozal E; Metz CJ; Dematteis M; Sachleben LR; Schurr A; Rane MJ
[Ad] Endereço:Department of Pediatrics PRI, University of Louisville, School of Medicine, Louisville, KY, USA; Department of Physiology, University of Louisville, School of Medicine, Louisville, KY, USA; Department of Pharmacology & Toxicology, University of Louisville, School of Medicine, Louisville, KY, USA
[Ti] Título:PKA activity exacerbates hypoxia-induced ROS formation and hypoxic injury in PC-12 cells.
[So] Source:Toxicol Lett;279:107-114, 2017 Sep 05.
[Is] ISSN:1879-3169
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Hypoxia is a primary factor in many pathological conditions. Hypoxic cell death is commonly attributed to metabolic failure and oxidative injury. cAMP-dependent protein kinase A (PKA) is activated in hypoxia and regulates multiple enzymes of the mitochondrial electron transport chain, thus may be implicated in cellular energy depletion and hypoxia-induced cell death. Wild type (WT) PC-12 cells and PKA activity-deficient 123.7 PC-12 cells were exposed to 3, 6, 12 and 24h hypoxia (0.1% or 5% O ). Hypoxia, at 24h 0.1% O , induced cell death and increased reactive oxygen species (ROS) in WT PC-12 cells. Despite lower ATP levels in normoxic 123.7 cells than in WT cells, hypoxia only decreased ATP levels in WT cells. However, menadione-induced oxidative stress similarly affected both cell types. While mitochondrial COX IV expression remained consistently higher in 123.7 cells, hypoxia decreased COX IV expression in both cell types. N-acetyl cysteine antioxidant treatment blocked hypoxia-induced WT cell death without preventing ATP depletion. Transient PKA catα expression in 123.7 cells partially restored hypoxia-induced ROS but did not alter ATP levels or COX IV expression. We conclude that PKA signaling contributes to hypoxic injury, by regulating oxidative stress rather than by depleting ATP levels. Therapeutic strategies targeting PKA signaling may improve cellular adaptation and recovery in hypoxic pathologies.
[Mh] Termos MeSH primário: Neoplasias das Glândulas Suprarrenais/enzimologia
Subunidades Catalíticas da Proteína Quinase Dependente de AMP Cíclico/metabolismo
Neurônios/enzimologia
Estresse Oxidativo
Feocromocitoma/enzimologia
Espécies Reativas de Oxigênio/metabolismo
Hipóxia Tumoral
[Mh] Termos MeSH secundário: Trifosfato de Adenosina/metabolismo
Neoplasias das Glândulas Suprarrenais/genética
Neoplasias das Glândulas Suprarrenais/patologia
Animais
Subunidades Catalíticas da Proteína Quinase Dependente de AMP Cíclico/genética
Complexo IV da Cadeia de Transporte de Elétrons/metabolismo
Metabolismo Energético
Neurônios/efeitos dos fármacos
Neurônios/patologia
Estresse Oxidativo/efeitos dos fármacos
Células PC12
Feocromocitoma/genética
Feocromocitoma/patologia
Ratos
Transdução de Sinais
Fatores de Tempo
Transfecção
Vitamina K 3/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Reactive Oxygen Species); 723JX6CXY5 (Vitamin K 3); 8L70Q75FXE (Adenosine Triphosphate); EC 1.9.3.1 (Electron Transport Complex IV); EC 2.7.11.11 (Cyclic AMP-Dependent Protein Kinase Catalytic Subunits)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170729
[St] Status:MEDLINE


  5 / 907 MEDLINE  
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[PMID]:28590909
[Au] Autor:Kurdi SE; Muaileq DA; Alhazmi HA; Bratty MA; Deeb SE
[Ad] Endereço:.
[Ti] Título:Comparing monolithic and fused core HPLC columns for fast chromatographic analysis of fat-soluble vitamins.
[So] Source:Acta Pharm;67(2):203-213, 2017 Jun 27.
[Is] ISSN:1846-9558
[Cp] País de publicação:Croatia
[La] Idioma:eng
[Ab] Resumo:HPLC stationary phases of monolithic and fused core type can be used to achieve fast chromatographic separation as an alternative to UPLC. In this study, monolithic and fused core stationary phases are compared for fast separation of four fat-soluble vitamins. Three new methods on the first and second generation monolithic silica RP-18e columns and a fused core pentafluoro-phenyl propyl column were developed. Application of three fused core columns offered comparable separations of retinyl palmitate, DL-α-tocopheryl acetate, cholecalciferol and menadione in terms of elution speed and separation efficiency. Separation was achieved in approx. 5 min with good resolution (Rs > 5) and precision (RSD ≤ 0.6 %). Monolithic columns showed, however, a higher number of theoretical plates, better precision and lower column backpressure than the fused core column. The three developed methods were successfully applied to separate and quantitate fat-soluble vitamins in commercial products.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/instrumentação
Vitaminas/análise
[Mh] Termos MeSH secundário: Colecalciferol/análise
Dióxido de Silício
Vitamina A/análogos & derivados
Vitamina A/análise
Vitamina K 3/análise
alfa-Tocoferol/análise
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Vitamins); 11103-57-4 (Vitamin A); 1C6V77QF41 (Cholecalciferol); 1D1K0N0VVC (retinol palmitate); 723JX6CXY5 (Vitamin K 3); 7631-86-9 (Silicon Dioxide); H4N855PNZ1 (alpha-Tocopherol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170608
[St] Status:MEDLINE


  6 / 907 MEDLINE  
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[PMID]:28365246
[Au] Autor:Vinnai JR; Cumming RC; Thompson GJ; Timoshenko AV
[Ad] Endereço:Department of Biology, The University of Western Ontario, London, ON, Canada, N6A 5B7.
[Ti] Título:The association between oxidative stress-induced galectins and differentiation of human promyelocytic HL-60 cells.
[So] Source:Exp Cell Res;355(2):113-123, 2017 Jun 15.
[Is] ISSN:1090-2422
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Galectins are multifunctional ß-galactoside-binding proteins that are involved in the regulation of cellular stress responses and differentiation. The relationship between these processes is unclear and we report here that galectins display oxidative-stress specific expression patterns in neutrophil-like differentiated HL-60 cells. Three galectins (-1, -3, and -10) are upregulated in response to either menadione or DMSO exposure whereas galectins -9 and -12 exhibited a stimulus-dependent downregulation. Changes in galectin expression are oxidant dependent based on the observations that 1) oxidative stress biomarkers HMOX1 (heme oxygenase-1) and NCF1 (neutrophil cytosolic factor 1, which is also a biomarker of neutrophil differentiation) are elevated in both cases, and 2) the antioxidant N-acetyl-L-cysteine restores basal expression of galectin-3 following oxidant exposure. In addition, our results suggest that the regulation of oxidative stress-sensitive galectins involves DNA hypomethylation mechanisms. Expression of galectin-3 and galectin-12 exhibits an opposite relationship to the expression of HMOX1/NCF1, suggesting a stimulatory and inhibitory role of these galectins in neutrophil-like differentiation of HL-60 cells. We also show that the inhibition of galectins reduces the growth rate of HL-60 cells, and facilitates their neutrophil-like differentiation. Collectively, our findings indicate that the process of cellular differentiation implicates, in part, oxidative stress-sensitive galectins, which further highlights a biological significance of galectin network remodeling in cells.
[Mh] Termos MeSH primário: Diferenciação Celular
Galectinas/biossíntese
Galectinas/metabolismo
Estresse Oxidativo
[Mh] Termos MeSH secundário: Calixarenos/farmacologia
Diferenciação Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Dissacarídeos/farmacologia
Relação Dose-Resposta a Droga
Galectinas/genética
Células HL-60
Seres Humanos
Lactose/farmacologia
Estresse Oxidativo/efeitos dos fármacos
Relação Estrutura-Atividade
Tiogalactosídeos/farmacologia
Vitamina K 3/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Disaccharides); 0 (Galectins); 0 (Thiogalactosides); 0 (compound 0118); 130036-26-9 (Calixarenes); 65R938S4DV (lactobionic acid); 723JX6CXY5 (Vitamin K 3); 80441-61-8 (thiodigalactoside); J2B2A4N98G (Lactose)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170403
[St] Status:MEDLINE


  7 / 907 MEDLINE  
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[PMID]:28197850
[Au] Autor:Eriksen JG; Kaalund I; Clemmensen O; Overgaard J; Pfeiffer P
[Ad] Endereço:Department of Oncology, Odense University Hospital, 5000, Odense C, Denmark. jesper@oncology.dk.
[Ti] Título:Placebo-controlled phase II study of vitamin K3 cream for the treatment of cetuximab-induced rash.
[So] Source:Support Care Cancer;25(7):2179-2185, 2017 Jul.
[Is] ISSN:1433-7339
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Cetuximab inhibits the epidermal growth factor receptor (EGFR), and papulopustular eruptions is a frequent side effect. Vitamin K3 (menadione) has preclinically shown to be a potential activator of the EGFR by phosphorylating the receptor (pEGFR). The present randomised study investigated the effect of a vitamin K3 cream on cetuximab-induced rash. MATERIALS AND METHODS: Thirty patients were included in this double-blinded placebo-controlled trial. Patients receiving cetuximab 500 mg/m every second week plus chemotherapy for metastatic cancer were included. In each patient, vitamin K3 cream and placebo were applied twice daily on two separate areas of the skin of minimum 10 × 10 cm for up to 2 months. Papulopustular eruptions were evaluated clinically and monitored by clinical photos. Skin biopsies, from ten patients taken before and after 1 month of treatment from each treatment area, were stained for EGFR and pEGFR. RESULTS: Application of vitamin K3 cream twice daily during treatment with cetuximab did not reduce the number of papulopustular eruptions, and this was independent of the use of systemic tetracycline. No significant changes in the staining of EGFR or pEGFR were observed in the skin of the vitamin K3-treated area compared to the placebo area. CONCLUSION: The present data do not support any clinical or immunohistochemical benefit of using vitamin K3 cream for cetuximab-induced rash.
[Mh] Termos MeSH primário: Cetuximab/efeitos adversos
Exantema/induzido quimicamente
Vitamina K 3/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Idoso
Feminino
Seres Humanos
Masculino
Meia-Idade
Vitamina K 3/administração & dosagem
Vitamina K 3/farmacologia
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE II; JOURNAL ARTICLE
[Nm] Nome de substância:
723JX6CXY5 (Vitamin K 3); PQX0D8J21J (Cetuximab)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171108
[Lr] Data última revisão:
171108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170216
[St] Status:MEDLINE
[do] DOI:10.1007/s00520-017-3623-x


  8 / 907 MEDLINE  
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[PMID]:28166978
[Au] Autor:Abbasi T; Shakeri M; Zaghari M; Kohram H
[Ad] Endereço:Department of Animal Science, Faculty of Agricultural Science & Engineering, College of Agriculture and Natural Resources, University of Tehran, Karaj, Iran.
[Ti] Título:Growth performance parameters, bone calcification and immune response of in ovo injection of 25-hydroxycholecalciferol and vitamin K in male ross 308 broilers.
[So] Source:Theriogenology;90:260-265, 2017 Mar 01.
[Is] ISSN:1879-3231
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:This experiment aimed to evaluate the effects of in ovo injection of 25-hydroxycholecalciferol (25-OH-D ) and Vitamin K on growth performance, bone calcification and immune system responses in male Ross 308 broilers. Twelve treatment groups with a total number of 768 experimental hatching eggs, four replications and 16 eggs in each replication were selected to form a completely randomized design of factorial arrangement. Treatments included: (1) distilled water, (2) 0.4 µg D , (3) 0.4 µg D + 2 µg K , (4) 0.4 µg D + 6 µg K , (5) 0.6 µg D , (6) 0.6 µg D + 2 µg K , (7) 0.6 µg D + 6 µg K , (8) 0.8 µg D , (9) 0.8 µg D + 2 µg K , (10) 0.8 µg D + 6 µg K , (11) 2 µg K and (12) 6 µg K . Eggs were transferred to corresponding hatching baskets on the 18th day of incubation and received 0.5 ml of experimental solutions specific to each treatment. The results of our experiments showed that Treatment No. 4 ranked the best out of those administered; holding the highest level of weight gain, feed intake during the breeding period (grower and finisher), bone calcium and phosphorus concentration, and tibia fractural force, (p < 0.05). Treatment No. 4 also showed a significant increase in antibody titer against the SRBC. Maximum stimulation to PHA injection also belonged to this treatment. In contrast, treatment No. 1 held the greatest alkaline phosphates amount (p < 0.05). No improvements were observed in calcium egg shells compared to the control group. Our data implies that appropriate levels of Vitamins D and K in ovo injection has beneficial effects on growth performance, immune system and bone development.
[Mh] Termos MeSH primário: 25-Hidroxivitamina D 2/farmacologia
Calcifediol/farmacologia
Calcificação Fisiológica/efeitos dos fármacos
Galinhas/crescimento & desenvolvimento
Vitamina K 3/farmacologia
[Mh] Termos MeSH secundário: Animais
Densidade Óssea/efeitos dos fármacos
Cálcio/metabolismo
Galinhas/imunologia
Galinhas/metabolismo
Relação Dose-Resposta a Droga
Injeções
Masculino
Óvulo
Fósforo/metabolismo
Tíbia/crescimento & desenvolvimento
Tíbia/lesões
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
21343-40-8 (25-Hydroxyvitamin D 2); 27YLU75U4W (Phosphorus); 723JX6CXY5 (Vitamin K 3); P6YZ13C99Q (Calcifediol); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171113
[Lr] Data última revisão:
171113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170208
[St] Status:MEDLINE


  9 / 907 MEDLINE  
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[PMID]:28106855
[Au] Autor:Urgin K; Jida M; Ehrhardt K; Müller T; Lanzer M; Maes L; Elhabiri M; Davioud-Charvet E
[Ad] Endereço:UMR 7509 CNRS-Université de Strasbourg, Bioorganic and Medicinal Chemistry Team, European School of Chemistry, Polymers and Materials (ECPM), 25, rue Becquerel, F-67087 Strasbourg, France. urginkarene@gmail.com.
[Ti] Título:Pharmacomodulation of the Antimalarial Plasmodione: Synthesis of Biaryl- and N-Arylalkylamine Analogues, Antimalarial Activities and Physicochemical Properties.
[So] Source:Molecules;22(1), 2017 Jan 19.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:With the aim of increasing the structural diversity on the early antimalarial drug plasmodione, an efficient and versatile procedure to prepare a series of biaryl- and -arylalkylamines as plasmodione analogues is described. Using the naturally occurring and commercially available menadione as starting material, a 2-step sequence using a Kochi-Anderson reaction and subsequent Pd-catalyzed Suzuki-Miyaura coupling was developed to prepare three representative biphenyl derivatives in good yields for antimalarial evaluation. In addition, synthetic methodologies to afford 3-benzylmenadione derivatives bearing a terminal - (Me)2 or - (Et)2 in different positions ( , and on the aryl ring of the benzylic chain of plasmodione were investigated through reductive amination was used as the optimal route to prepare these protonable -arylalkylamine privileged scaffolds. The antimalarial activities were evaluated and discussed in light of their physicochemical properties. Among the newly synthesized compounds, the -position of the substituent remains the most favourable position on the benzyl chain and the carbamate - HBoc was found active both in vitro (42 nM versus 29 nM for plasmodione) and in vivo in -infected mice. The measured acido-basic features of these new molecules support the cytosol-food vacuole shuttling properties of non-protonable plasmodione derivatives essential for redox-cycling. These findings may be useful in antimalarial drug optimization.
[Mh] Termos MeSH primário: Aminas/administração & dosagem
Aminas/síntese química
Antimaláricos/administração & dosagem
Antimaláricos/síntese química
Malária/tratamento farmacológico
[Mh] Termos MeSH secundário: Aminas/química
Aminas/farmacologia
Animais
Antimaláricos/química
Antimaláricos/farmacologia
Técnicas de Química Combinatória
Camundongos
Estrutura Molecular
Oxirredução
Plasmodium berghei/efeitos dos fármacos
Relação Estrutura-Atividade
Vitamina K 3/análogos & derivados
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Antimalarials); 723JX6CXY5 (Vitamin K 3)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170505
[Lr] Data última revisão:
170505
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170121
[St] Status:MEDLINE


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[PMID]:28017859
[Au] Autor:Kapadia GJ; Soares IA; Rao GS; Badoco FR; Furtado RA; Correa MB; Tavares DC; Cunha WR; Magalhães LG
[Ad] Endereço:Department of Pharmaceutical Sciences, College of Pharmacy, Howard University, Washington, DC 20059, USA.
[Ti] Título:Antiparasitic activity of menadione (vitamin K ) against Schistosoma mansoni in BABL/c mice.
[So] Source:Acta Trop;167:163-173, 2017 Mar.
[Is] ISSN:1873-6254
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Schistosomiasis is one of the neglected tropical diseases affecting nearly quarter of a billion people in economically challenged tropical and subtropical countries of the world. Praziquantel (PZQ) is the only drug currently available to treat this parasitic disease in spite being ineffective against juvenile worms and concerns about developing resistance to treat reinfections. Our earlier in vitro viability studies demonstrated significant antiparasitic activity of menadione (MEN) (vitamin K ) against Schistosoma mansoni adult worms. To gain insight into plausible mechanism of antischistosomal activity of MEN, its effect on superoxide anion levels in adult worms were studied in vitro which showed significant increases in both female and male worms. Further confirmation of the deleterious morphological changes in their teguments and organelles were obtained by ultrastructural analysis. Genotoxic and cytotoxic studies in male Swiss mice indicated that MEN was well tolerated at the oral dose of 500mg/kg using the criteria of MNPCE frequency and PCE/RBC ratio in the bone marrow of infected animals. The in vivo antiparasitic activity of MEN was conducted in female BALB/c mice infected with S. mansoni and significant reductions (P<0.001) in total worm burden were observed at single oral doses of 40 and 400mg/kg (48.57 and 61.90%, respectively). Additionally, MEN significantly reduced (P<0.001) the number of eggs in the liver of infected mice by 53.57 and 58.76%, respectively. Similarly, histological analysis of the livers showed a significant reduction (P<0.001) in the diameter of the granulomas. Since MEN is already in use globally as an over-the-counter drug for a variety of common ailments and a dietary supplement with a safety record in par with similar products when used in recommended doses, the above antiparasitic results which compare reasonably well with PZQ, make a compelling case for considering MEN to treat S. mansoni infection in humans.
[Mh] Termos MeSH primário: Antiparasitários/farmacologia
Schistosoma mansoni/efeitos dos fármacos
Vitamina K 3/farmacologia
[Mh] Termos MeSH secundário: Animais
Relação Dose-Resposta a Droga
Feminino
Granuloma/parasitologia
Fígado/parasitologia
Masculino
Camundongos
Camundongos Endogâmicos BALB C
Schistosoma mansoni/ultraestrutura
Esquistossomose/tratamento farmacológico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiparasitic Agents); 723JX6CXY5 (Vitamin K 3)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161227
[St] Status:MEDLINE



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