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  1 / 127988 MEDLINE  
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[PMID]:29431945
[Au] Autor:Sinitskaya TA; Malinovskaya NN
[Ti] Título:[Toxicological-hygienic justification of the acceptable daily intake of acetamiprid].
[So] Source:Gig Sanit;95(11):1055-8, 2016.
[Is] ISSN:0016-9900
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Neonicotinoids are currently meaningful component of rotation schemes of insecticides of selective action in the system of integrated pest control, which have agricultural importance in many countries. The research results of the biological impact of acetamiprid (neonicotinoids) on the body of laboratory animals are given in the article. The study showed that the explored active substance is related to the moderately hazardous compounds (hazard category 3) in case of one-time per oral penetration. Acetamiprid has polytropic action in the case of chronic (12 months) oral entering the body of laboratory animals, it gives rise changes in functionality of the central nervous system, blood system, liver functioning. On the base of alterations of the studied indices there were established both the no-effect dose level (NOEL) and acceptable daily intake of acetamiprid for humans.
[Mh] Termos MeSH primário: Células Sanguíneas/efeitos dos fármacos
Sistema Nervoso Central/efeitos dos fármacos
Neonicotinoides
Envenenamento
[Mh] Termos MeSH secundário: Administração Oral
Animais
Comportamento Animal/efeitos dos fármacos
Modelos Animais de Doenças
Testes Hematológicos/métodos
Inseticidas/farmacologia
Inseticidas/toxicidade
Testes de Função Hepática/métodos
Concentração Máxima Permitida
Neonicotinoides/farmacologia
Neonicotinoides/toxicidade
Nível de Efeito Adverso não Observado
Órgãos em Risco
Envenenamento/sangue
Envenenamento/diagnóstico
Envenenamento/etiologia
Ratos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Insecticides); 0 (Neonicotinoids); 5HL5N372P0 (acetamiprid)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180213
[St] Status:MEDLINE


  2 / 127988 MEDLINE  
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[PMID]:29431329
[Au] Autor:Belyaeva NN; Sycheva LP
[Ti] Título:[Morphological comparative assessment of in vivo 2-week oral exposure of silver nanoparticles and silver sulfate on the mice liver].
[So] Source:Gig Sanit;95(9):899-902, 2016.
[Is] ISSN:0016-9900
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Currently the problem of the impact of nanoparticles and nanomaterials on human health remains to be poorly understood. As in our studies of the impact of silver nanoparticles on rats liver as well in works of other researchers there were investigated morphofunctional indices under peroral exposure. Although all researchers took different sizes, doses and concentrations of silver nanoparticles, various exposure time and different stabilizers, the same effects had been obtained, which, however, were occurred under both different doses and time of exposure. However, it was interesting to compare the impact of silver nanoparticles with reference substance - silver sulfate on the mice liver with the previously evaluated effect produced on the rats ' liver. By ourselves there was executed the morphological comparative evaluation of in vivo oral 2-weeks exposure of 4 concentrations (0.1; 5; 50 and 500 mg/l) of silver nanoparticles with size of 14 nm, stable arabian gum 1:7 by weight, and of 4 similar concentrations of silver sulfate on the liver of male mice СВАхС57В1/6 weighing 25-35g. 2 groups were considered as control: intact mice and mice received gum in water. Results of the exposure were assessed according to 10 morphological and functional indices. The impact of nanosilver was shown to initiate from its concentration of 50 mg/l and to express in the gain of the index of alteration of the cytoplasm of hepatocytes with the increasing in both severity of steatosis and the number of micronecroses, persisting at the same level at concentrations of 500 mg/l and with the elevation of the index of alteration of nuclei of hepatocytes, while the similar effect develops under the influence of silver sulfate at a concentration of 500 mg/l only. The remaining investigated morphofunctional indices did not differ significantly in all groups of mice. Unlike previously executed studies on rats, mice appeared to be sensitive to the effects of nano-silver more than to silver sulfate.
[Mh] Termos MeSH primário: Doença Hepática Induzida por Substâncias e Drogas
Fígado Gorduroso
Fígado
Nanoestruturas
Compostos de Prata
[Mh] Termos MeSH secundário: Administração Oral
Animais
Doença Hepática Induzida por Substâncias e Drogas/diagnóstico
Doença Hepática Induzida por Substâncias e Drogas/etiologia
Modelos Animais de Doenças
Fígado Gorduroso/induzido quimicamente
Fígado Gorduroso/patologia
Células Hep G2
Seres Humanos
Fígado/efeitos dos fármacos
Fígado/patologia
Camundongos
Nanoestruturas/química
Nanoestruturas/toxicidade
Necrose
Compostos de Prata/química
Compostos de Prata/toxicidade
Testes de Toxicidade/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Silver Compounds)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180213
[St] Status:MEDLINE


  3 / 127988 MEDLINE  
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[PMID]:29367486
[Au] Autor:Miyazawa N; Yoshimoto H; Kurihara S; Hamaya T; Eguchi F
[Ad] Endereço:Faculty of Regional Environment Science, Tokyo University of Agriculture.
[Ti] Título:Improvement of Diet-induced Obesity by Ingestion of Mushroom Chitosan Prepared from Flammulina velutipes.
[So] Source:J Oleo Sci;67(2):245-254, 2018 Feb 01.
[Is] ISSN:1347-3352
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The anti-obesity effects of mushroom chitosan prepared from Flammulina velutipes were investigated using an animal model with diet-induced obesity. In this study, 5-week-old imprinting control region (ICR) mice were divided into six groups of 10 mice each and fed different diets based on the MF powdered diet (standard diet) for 6 weeks: standard diet control group, high-fat diet control group (induced dietary obesity) consisting of the standard diet and 20% lard, and mushroom chitosan groups consisting of the high-fat diet with mushroom chitosan added at 100, 500, 1,000, and 2,000 mg/kg body weight. On the final day of the experiment, mean body weight was 39.1 g in the high-fat control group and 36.3 g in the 2,000 mg/kg mushroom chitosan group, compared to 35.8 g in the standard diet control group. In the mushroom chitosan groups, a dose-dependent suppression of weight gain and marked improvements in serum triglycerides, total cholesterol, LDL-cholesterol, and HDL-cholesterol were found. The mushroom chitosan groups showed fewer and smaller fat deposits in liver cells than the high-fat diet control group, and liver weight was significantly reduced. Glutamic oxaloacetic transaminase (GOT) and glutamate pyruvic transaminase (GPT), which are indices of the hepatic function, all showed dose-dependent improvement with mushroom chitosan administration. These results suggested that mushroom chitosan acts to suppress enlargement of the liver from fat deposition resulting from a high-fat diet and to restore hepatic function. The lipid content of feces showed a marked increase correlated with the mushroom chitosan dose. These findings suggest the potential use of mushroom chitosan as a functional food ingredient that contributes to the prevention or improvement of dietary obesity by inhibiting digestion and absorption of fats in the digestive tract and simultaneously promotes lipolysis in adipocytes.
[Mh] Termos MeSH primário: Quitosana/administração & dosagem
Quitosana/isolamento & purificação
Dieta Hiperlipídica/efeitos adversos
Flammulina/química
Obesidade/prevenção & controle
Fitoterapia
[Mh] Termos MeSH secundário: Adipócitos/metabolismo
Administração Oral
Animais
Fármacos Antiobesidade
Quitosana/farmacologia
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Lipólise/efeitos dos fármacos
Masculino
Camundongos Endogâmicos ICR
Hepatopatia Gordurosa não Alcoólica/prevenção & controle
Obesidade/etiologia
Obesidade/metabolismo
Ganho de Peso/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Obesity Agents); 9012-76-4 (Chitosan)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180126
[St] Status:MEDLINE
[do] DOI:10.5650/jos.ess17159


  4 / 127988 MEDLINE  
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[PMID]:29320574
[Au] Autor:Inoue A; Furukawa A; Yamamoto H; Ohta S; Linh NDH; Syerikjan T; Kaida S; Yamaguchi T; Murata S; Obata T; Tani M; Murata K
[Ad] Endereço:Department of Radiology, Shiga University of Medical Science, Otsu, Shiga, Japan.
[Ti] Título:Acceleration of small bowel motility after oral administration of dai-kenchu-to (TJ-100) assessed by cine magnetic resonance imaging.
[So] Source:PLoS One;13(1):e0191044, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Dai-kenchu-to (TJ-100) is an herbal medicine used to shorten the duration of intestinal transit by accelerating intestinal movement. However, intestinal movement in itself has not been evaluated in healthy volunteers using radiography, fluoroscopy, and radioisotopes because of exposure to ionizing radiation. The purpose of this study was to evaluate the effect of TJ-100 on intestinal motility using cinematic magnetic resonance imaging (cine MRI) with a steady-state free precession sequence. Ten healthy male volunteers received 5 g of either TJ-100 or lactose without disclosure of the identity of the substance. Each volunteer underwent two MRI examinations after taking the substances (TJ-100 and lactose) on separate days. They drank 1200 mL of tap water and underwent cine MRI after 10 min. A steady-state free precession sequence was used for imaging, which was performed thrice at 0, 10, 20, 30, 40, and 50 min. The bowel contraction frequency and distention score were assessed. Wilcoxon signed-rank test was used, and differences were considered significant at a P-value <0.05. The bowel contraction frequency tended to be greater in the TJ-100 group and was significantly different in the ileum at 20 (TJ-100, 8.95 ± 2.88; lactose, 4.80 ± 2.92; P < 0.05) and 50 min (TJ-100, 9.45 ± 4.49; lactose, 4.45 ± 2.65; P < 0.05) between the groups. No significant differences were observed in the bowel distention scores. Cine MRI demonstrated that TJ-100 activated intestinal motility without dependence on ileum distention.
[Mh] Termos MeSH primário: Motilidade Gastrointestinal
Intestino Delgado/fisiologia
Imagem Cinética por Ressonância Magnética/métodos
Extratos Vegetais/administração & dosagem
[Mh] Termos MeSH secundário: Administração Oral
Adulto
Método Duplo-Cego
Seres Humanos
Intestino Delgado/diagnóstico por imagem
Meia-Idade
Estudos Prospectivos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Plant Extracts); 0 (dai-kenchu-to)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0191044


  5 / 127988 MEDLINE  
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[PMID]:28465178
[Au] Autor:Das S; Ghosh S; De AK; Bera T
[Ad] Endereço:Laboratory of Nanomedicine, Division of Pharmaceutical Biotechnology, Department of Pharmaceutical Technology, Jadavpur University, 188 Raja S.C. Mallick Road, Kolkata, 700 032, W.B., India.
[Ti] Título:Oral delivery of ursolic acid-loaded nanostructured lipid carrier coated with chitosan oligosaccharides: Development, characterization, in vitro and in vivo assessment for the therapy of leishmaniasis.
[So] Source:Int J Biol Macromol;102:996-1008, 2017 Sep.
[Is] ISSN:1879-0003
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Visceral leishmaniasis (VL) is a life-threatening disease caused by Leishmania donovani due to uncontrolled parasitisation of liver, spleen, and bone marrow. Ursolic acid (UA), a promising anti-inflammatory, anti-bacterial and anti-diabetic drug used successfully for treatment of ailments. Development of new delivery system is extremely urgent for UA with better efficacy and fewer side effects. The aim of present research work was to formulate and evaluate the potential anti-leishmanial activity of UA loaded N-octyl-chitosan surface decorated nanostructured lipid carrier system (UA-NLC) for delivery to the macrophages for VL. UA-NLC were prepared and characterized for shape, size, fourier transforms scanning electron microscopy (FESEM), transmittance electron microscopy (TEM), entrapment efficiency and in vitro drug release. The results indicate that the formulated UA-NLC had nano size range (103.7±2.8nm to 143.0±3.8nm) with high drug loading capacity (12.05±0.54%) and entrapment efficiency (88.63±2.7%). Ex vivo drug uptake by macrophage was also evaluated. The UA-NLC was more effective against AG83 wild type (12 fold), SSG-R (4 fold), PMM-R (4 fold) and GE1 field isolated (3 fold) cellular amastigotes than its free form. In vivo study showed orally effective UA-NLC could suppress the parasite burden to 98.75%.
[Mh] Termos MeSH primário: Quitosana/química
Portadores de Fármacos/química
Leishmaniose/tratamento farmacológico
Lipídeos/química
Nanoestruturas/química
Triterpenos/química
Triterpenos/farmacologia
[Mh] Termos MeSH secundário: Administração Oral
Animais
Desenho de Drogas
Liberação Controlada de Fármacos
Feminino
Macrófagos/efeitos dos fármacos
Masculino
Camundongos
Camundongos Endogâmicos BALB C
Oligossacarídeos/química
Triterpenos/administração & dosagem
Triterpenos/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Lipids); 0 (Oligosaccharides); 0 (Triterpenes); 9012-76-4 (Chitosan); P3M2575F3F (ursolic acid)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE


  6 / 127988 MEDLINE  
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[PMID]:29458539
[Au] Autor:Ma ST; Ding GJ; Huang XW; Wang ZW; Wang L; Yu ML; Shi W; Jiang YP; Tang LJ; Xu YG; Li YJ
[Ad] Endereço:College of Veterinary Medicine, Northeast Agricultural University, Mu Cai Street No. 59, Xiang Fang District, Harbin, PR China.
[Ti] Título:Immunogenicity in chickens with orally administered recombinant chicken-borne Lactobacillus saerimneri expressing FimA and OmpC antigen of O78 avian pathogenic Escherichia coli.
[So] Source:J Med Microbiol;67(3):441-451, 2018 Mar.
[Is] ISSN:1473-5644
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Avian colibacillosis is responsible for economic losses to poultry producers worldwide. To combat this, we aimed to develop an effective oral vaccine for chicken against O78 avian pathogenic Escherichia coli (APEC) infection through a Lactobacillus delivery system. METHODOLOGY: Eight Lactobacillus strains isolated from the intestines of broiler chickens were evaluated based on their in vitro adherence ability to assess their potential as a delivery vector. Fimbrial subunit A (FimA) and outer-membrane protein C (OmpC) of APEC with and without fusion to dendritic cell-targeting peptide (DCpep) and microfold cell-targeting peptide (Co1) were displayed on the surface of Lactobacillus saerimneri M-11 and yielded vaccine groups (pPG-ompC-fimA/M-11 and pPG-ompC-fimA-Co1-DCpep/M-11, respectively). The colonization of the recombinant strains in vivo was assessed and the immunogenicity and protective efficacy of orally administered recombinant strains in chickens were evaluated. RESULTS: The colonization of the recombinant strains in vivo revealed no significant differences between the recombinant and wild-type strains. Chickens orally administered with vaccine groups showed significantly higher levels of OmpC/FimA-specific IgG in serum and mucosal IgA in cecum lavage, nasal lavage and stool compared to the pPG/M-11 group. After challenge with APEC CVCC1553, better protective efficacy was observed in chickens orally immunized with pPG-ompC-fimA/M-11 and pPG-ompC-fimA-Co1-DCpep/M-11, but no significant differences were observed between the two groups. CONCLUSIONS: Recombinant chicken-borne L. saerimneri M-11 showed good immunogenicity in chickens, suggesting that it may be a promising vaccine candidate against APEC infections. However, the activity of mammalian DCpep and Co1 was not significant in chickens.
[Mh] Termos MeSH primário: Infecções por Escherichia coli/veterinária
Vacinas contra Escherichia coli/imunologia
Proteínas de Fímbrias/imunologia
Imunogenicidade da Vacina
Lactobacillus/genética
Porinas/imunologia
Doenças das Aves Domésticas/imunologia
[Mh] Termos MeSH secundário: Administração Oral
Animais
Anticorpos Antibacterianos/sangue
Antígenos de Bactérias/genética
Antígenos de Bactérias/imunologia
Ceco/imunologia
Galinhas
Escherichia coli/imunologia
Escherichia coli/patogenicidade
Infecções por Escherichia coli/imunologia
Infecções por Escherichia coli/prevenção & controle
Proteínas de Fímbrias/genética
Imunoglobulina A/sangue
Imunoglobulina G/sangue
Intestinos/microbiologia
Lactobacillus/crescimento & desenvolvimento
Lactobacillus/imunologia
Lactobacillus/isolamento & purificação
Porinas/genética
Doenças das Aves Domésticas/prevenção & controle
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antibodies, Bacterial); 0 (Antigens, Bacterial); 0 (Escherichia coli Vaccines); 0 (Immunoglobulin A); 0 (Immunoglobulin G); 0 (OmpC protein); 0 (Porins); 0 (fimbrillin); 147680-16-8 (Fimbriae Proteins)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180221
[St] Status:MEDLINE
[do] DOI:10.1099/jmm.0.000679


  7 / 127988 MEDLINE  
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Texto completo
[PMID]:29270996
[Au] Autor:Maldonado MR; Bracht L; de Sá-Nakanishi AB; Corrêa RCG; Comar JF; Peralta RM; Bracht A
[Ad] Endereço:Department of Biochemistry, University of Maringá, Maringá, Brazil.
[Ti] Título:Actions of p-synephrine on hepatic enzyme activities linked to carbohydrate metabolism and ATP levels in vivo and in the perfused rat liver.
[So] Source:Cell Biochem Funct;36(1):4-12, 2018 Jan.
[Is] ISSN:1099-0844
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:p-Synephrine is one of the main active components of the fruit of Citrus aurantium (bitter orange). Extracts of the bitter orange and other preparations containing p-synephrine have been used worldwide to promote weight loss and for sports performance. The purpose of the study was to measure the action of p-synephrine on hepatic enzyme activities linked to carbohydrate and energy metabolism and the levels of adenine mononucleotides. Enzymes and adenine mononucleotides were measured in the isolated perfused rat liver and in vivo after oral administration of the drug (50 and 300 mg/kg) by using standard techniques. p-Synephrine increased the activity of glycogen phosphorylase in vivo and in the perfused liver. It decreased, however, the activities of pyruvate kinase and pyruvate dehydrogenase also in vivo and in the perfused liver. p-Synephrine increased the hepatic pools of adenosine diphosphate and adenosine triphosphate. Stimulation of glycogen phosphorylase is consistent with the reported increased glycogenolysis in the perfused liver and increased glycemia in rats. The decrease in the pyruvate dehydrogenase activity indicates that p-synephrine is potentially capable of inhibiting the transformation of carbohydrates into lipids. The capability of increasing the adenosine triphosphate-adenosine diphosphate pool indicates a beneficial effect of p-synephrine on the cellular energetics.
[Mh] Termos MeSH primário: Trifosfato de Adenosina/metabolismo
Metabolismo dos Carboidratos/efeitos dos fármacos
Fígado/efeitos dos fármacos
Fígado/enzimologia
Sinefrina/farmacologia
[Mh] Termos MeSH secundário: Administração Oral
Animais
Citrus/química
Glicogênio Fosforilase/metabolismo
Fígado/irrigação sanguínea
Fígado/cirurgia
Masculino
Complexo Piruvato Desidrogenase/antagonistas & inibidores
Complexo Piruvato Desidrogenase/metabolismo
Piruvato Quinase/antagonistas & inibidores
Piruvato Quinase/metabolismo
Ratos
Ratos Wistar
Sinefrina/administração & dosagem
Sinefrina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Pyruvate Dehydrogenase Complex); 8L70Q75FXE (Adenosine Triphosphate); EC 2.4.1.- (Glycogen Phosphorylase); EC 2.7.1.40 (Pyruvate Kinase); PEG5DP7434 (Synephrine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171223
[St] Status:MEDLINE
[do] DOI:10.1002/cbf.3311


  8 / 127988 MEDLINE  
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[PMID]:29191556
[Au] Autor:Thompson AM; Marshall AJ; Maes L; Yarlett N; Bacchi CJ; Gaukel E; Wring SA; Launay D; Braillard S; Chatelain E; Mowbray CE; Denny WA
[Ad] Endereço:Auckland Cancer Society Research Centre, School of Medical Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand. Electronic address: am.thompson@auckland.ac.nz.
[Ti] Título:Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
[So] Source:Bioorg Med Chem Lett;28(2):207-213, 2018 01 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A 900 compound nitroimidazole-based library derived from our pretomanid backup program with TB Alliance was screened for utility against human African trypanosomiasis (HAT) by the Drugs for Neglected Diseases initiative. Potent hits included 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides, which surprisingly displayed good metabolic stability and excellent cell permeability. Following comprehensive mouse pharmacokinetic assessments on four hits and determination of the most active chiral form, a thiazine oxide counterpart of pretomanid (24) was identified as the best lead. With once daily oral dosing, this compound delivered complete cures in an acute infection mouse model of HAT and increased survival times in a stage 2 model, implying the need for more prolonged CNS exposure. In preliminary SAR findings, antitrypanosomal activity was reduced by removal of the benzylic methylene but enhanced through a phenylpyridine-based side chain, providing important direction for future studies.
[Mh] Termos MeSH primário: Nitroimidazóis/farmacologia
Bibliotecas de Moléculas Pequenas/farmacologia
Tripanossomíase Africana/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Oral
Animais
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Seres Humanos
Camundongos
Estrutura Molecular
Nitroimidazóis/administração & dosagem
Nitroimidazóis/química
Bibliotecas de Moléculas Pequenas/administração & dosagem
Bibliotecas de Moléculas Pequenas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (2-nitro-6-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo(2,1-b)(1,3)oxazine); 0 (Nitroimidazoles); 0 (Small Molecule Libraries)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171202
[St] Status:MEDLINE


  9 / 127988 MEDLINE  
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[PMID]:28457894
[Au] Autor:Zupancic O; Bernkop-Schnürch A
[Ad] Endereço:Department of Pharmaceutical Technology, Institute of Pharmacy, Leopold-Franzens-University Innsbruck, Innrain 80/82, Center for Chemistry and Biomedicine, 6020 Innsbruck, Austria.
[Ti] Título:Lipophilic peptide character - What oral barriers fear the most.
[So] Source:J Control Release;255:242-257, 2017 Jun 10.
[Is] ISSN:1873-4995
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Peptide therapeutics is currently one of the fastest growing markets worldwide and consequently convenient ways of administration for these drugs are highly on demand. In particular, oral dosage forms would be preferred. A relative large molecular weight and high hydrophilicity, however, result in comparatively very low oral bioavailability being in most cases below 1%. Lipid based formulations (LBF), in particular self-emulsifying drug delivery systems (SEDDS) and solid lipid nanoparticles (SLN) as well as liposomes are among the most promising tools for oral peptide delivery. Key to success in orally delivering peptides via LBF seems to be a sufficiently high lipophilic character of those therapeutic agents. Hence, different non-covalent and covalent peptide lipidization methods from drug delivery point of view are presented. On the one hand, among non-covalent lipidization methods hydrophobic ion pairing seems to be a promising way to sufficiently increase peptide lipophilicity providing high drug payloads in the lipid phase, a protective effect against presystemic metabolism via thiol-disulphide exchange reactions and proteolysis as well as an improved intestinal membrane permeability. On the other hand, covalent methods like conjugating fatty acids via amidation, esterification, reversible aqueous lipidization (REAL) and cyclization also show potential. The present review therefore describes those lipidization methods in detail and critically evaluates their contribution in successfully overcoming the oral barriers.
[Mh] Termos MeSH primário: Lipídeos/química
Peptídeos/química
[Mh] Termos MeSH secundário: Administração Oral
Animais
Sistemas de Liberação de Medicamentos
Seres Humanos
Absorção Intestinal
Peptídeos/administração & dosagem
Peptídeos/farmacocinética
Peptídeos/uso terapêutico
Proteólise
Vacinas
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Lipids); 0 (Peptides); 0 (Vaccines)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE


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[PMID]:27778440
[Au] Autor:De Gottardi A; Trebicka J; Klinger C; Plessier A; Seijo S; Terziroli B; Magenta L; Semela D; Buscarini E; Langlet P; Görtzen J; Puente A; Müllhaupt B; Navascuès C; Nery F; Deltenre P; Turon F; Engelmann C; Arya R; Caca K; Peck-Radosavljevic M; Leebeek FWG; Valla D; Garcia-Pagan JC; VALDIG Investigators
[Ad] Endereço:Hepatology, Department of Clinical Research and Clinic of Visceral Surgery and Medicine, Inselspital, University of Berne, Berne, Switzerland.
[Ti] Título:Antithrombotic treatment with direct-acting oral anticoagulants in patients with splanchnic vein thrombosis and cirrhosis.
[So] Source:Liver Int;37(5):694-699, 2017 May.
[Is] ISSN:1478-3231
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Direct-acting oral anticoagulants (DOACs) are used in patients with splanchnic vein thrombosis (SVT) and cirrhosis, but evidence for safety and efficacy in this setting is limited. Our aim was to identify indications and reasons for starting or switching to DOACs and to report adverse effects, complications and short-term outcome. METHODS: Data collection including demographic information, laboratory values, treatment and complications through the Vascular Liver Disease Interest Group Consortium. RESULTS: Forty-five centres (90%) of the consortium completed the initial eCRF. We report here a series of 94 patients from 17 centres. Thirty-six patients (38%) had cirrhosis. Child-Pugh score was 6 (range 5-8), and MELD score 10.2 (range 6-19). Indications for anticoagulation were splanchnic vein thrombosis (75%), deep vein thrombosis (5%), atrial fibrillation (14%) and others (6%). DOACs used were rivaroxaban (83%), dabigatran (11%) and apixaban (6%). Patients were followed up for a median duration of 15 months (cirrhotic) and 26.5 months (non-cirrhotic). Adverse events occurred in 17% of patients and included one case of recurrent portal vein thrombosis and five cases of bleeding. Treatment with DOACs was stopped in three cases. The major reasons for choosing DOACs were no need for monitoring or inadequacy of INR to guide anticoagulation in cirrhotic patients. Renal and liver function did not change during treatment. CONCLUSIONS: A consistent number of patients with SVT and/or cirrhosis are currently treated with DOACs, which seem to be effective and safe. These data provide a basis for performing randomized clinical trials of DOACs vs. low molecular weight heparin or vitamin K antagonists.
[Mh] Termos MeSH primário: Anticoagulantes/efeitos adversos
Anticoagulantes/uso terapêutico
Fibrilação Atrial/tratamento farmacológico
Cirrose Hepática/complicações
Trombose Venosa/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Oral
Adolescente
Adulto
Idoso
Idoso de 80 Anos ou mais
Europa (Continente)
Feminino
Hemorragia Gastrointestinal/induzido quimicamente
Seres Humanos
Masculino
Meia-Idade
Circulação Esplâncnica/fisiologia
Vitamina K/antagonistas & inibidores
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY
[Nm] Nome de substância:
0 (Anticoagulants); 12001-79-5 (Vitamin K)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180307
[Lr] Data última revisão:
180307
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161026
[St] Status:MEDLINE
[do] DOI:10.1111/liv.13285



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