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[PMID]:28792526
[Au] Autor:Haserick JR; Klein JA; Costello CE; Samuelson J
[Ad] Endereço:Department of Molecular and Cell Biology, Boston University Goldman School of Dental Medicine, Boston, Massachusetts, United States of America.
[Ti] Título:Cryptosporidium parvum vaccine candidates are incompletely modified with O-linked-N-acetylgalactosamine or contain N-terminal N-myristate and S-palmitate.
[So] Source:PLoS One;12(8):e0182395, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Cryptosporidium parvum (studied here) and Cryptosporidium hominis are important causes of diarrhea in infants and immunosuppressed persons. C. parvum vaccine candidates, which are on the surface of sporozoites, include glycoproteins with Ser- and Thr-rich domains (Gp15, Gp40, and Gp900) and a low complexity, acidic protein (Cp23). Here we used mass spectrometry to determine that O-linked GalNAc is present in dense arrays on a glycopeptide with consecutive Ser derived from Gp40 and on glycopeptides with consecutive Thr derived from Gp20, a novel C. parvum glycoprotein with a formula weight of ~20 kDa. In contrast, the occupied Ser or Thr residues in glycopeptides from Gp15 and Gp900 are isolated from one another. Gly at the N-terminus of Cp23 is N-myristoylated, while Cys, the second amino acid, is S-palmitoylated. In summary, C. parvum O-GalNAc transferases, which are homologs of host enzymes, densely modify arrays of Ser or Thr, as well as isolated Ser and Thr residues on C. parvum vaccine candidates. The N-terminus of an immunodominant antigen has lipid modifications similar to those of host cells and other apicomplexan parasites. Mass spectrometric demonstration here of glycopeptides with O-glycans complements previous identification C. parvum O-GalNAc transferases, lectin binding to vaccine candidates, and human and mouse antibodies binding to glycopeptides. The significance of these post-translational modifications is discussed with regards to the function of these proteins and the design of serological tests and vaccines.
[Mh] Termos MeSH primário: Cryptosporidium parvum/imunologia
Vacinas Protozoárias/química
[Mh] Termos MeSH secundário: Acetilgalactosamina/química
Biologia Computacional
Criptosporidiose/imunologia
Criptosporidiose/prevenção & controle
Cryptosporidium parvum/enzimologia
Glicoproteínas/química
Espectrometria de Massas
Monossacarídeos/química
Miristatos/química
Palmitatos/química
Polissacarídeos/química
Proteínas de Protozoários/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glycoproteins); 0 (Monosaccharides); 0 (Myristates); 0 (Palmitates); 0 (Polysaccharides); 0 (Protozoan Proteins); 0 (Protozoan Vaccines); KM15WK8O5T (Acetylgalactosamine)
[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:170810
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0182395


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[PMID]:28188720
[Au] Autor:Oliveira JS; Lange S; Dobner B; Brezesinski G
[Ad] Endereço:Max Planck Institute of Colloids and Interfaces, Am Mühlenberg 1, 14476 Potsdam, Germany.
[Ti] Título:The effect of non-deuterated and deuterated isopropyl myristate on the thermodynamical and structural behavior of a 2D Stratum Corneum model with Ceramide [AP].
[So] Source:Chem Phys Lipids;204:1-9, 2017 Apr.
[Is] ISSN:1873-2941
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Isopropyl myristate (IPM) is a widely used penetration enhancer in pharmaceutical formulations, however, its mechanism of action on a molecular scale is still not completely understood. Previous work using a quaternary Stratum Corneum (SC) lipid model in bulk suggested the incorporation of isopropyl myristate into the SC lipid matrix, phase separation, and perturbation of the multilamellar lipid assembly. Here, we used 2D Langmuir monolayers of a ternary SC lipid model, containing ceramide AP C18:18, stearic acid and cholesterol in a molar ratio of [1:1:0.7], respectively, to shed light on the mechanism of action of this important lipophilic penetration enhancer. To do so, the synthesis of chain deuterated isopropyl myristate was successfully performed in order to study the different coupling possibilities between the hydrogenated and deuterated IPM and the alkyl chains of the SC molecules. Our results indicate that only a small portion of IPM is able to mix with our SC model leading to a limited fluidizing effect (small increase of the wavenumber of CH stretching vibration, increase of the SC layer flexibility), but will be squeezed out at higher lateral pressures. Furthermore, the deuteration of IPM enhances the miscibility with this SC model, probably due to a different coupling between the alkyl chains or the alkyl and deuterated chains. Additionally, using the pure D-form of CER[AP] in the SC model amplifies the obtained results.
[Mh] Termos MeSH primário: Ceramidas/química
Miristatos/química
Pele/química
Termodinâmica
[Mh] Termos MeSH secundário: Seres Humanos
Lipídeos/química
Modelos Moleculares
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ceramides); 0 (Lipids); 0 (Myristates); 0RE8K4LNJS (isopropyl myristate)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170509
[Lr] Data última revisão:
170509
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170212
[St] Status:MEDLINE


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[PMID]:28132900
[Au] Autor:Eichner A; Stahlberg S; Sonnenberger S; Lange S; Dobner B; Ostermann A; Schrader TE; Hauß T; Schroeter A; Huster D; Neubert RH
[Ad] Endereço:Institute of Pharmacy, Martin Luther University Halle-Wittenberg, 06120 Halle/Saale, Germany.
[Ti] Título:Influence of the penetration enhancer isopropyl myristate on stratum corneum lipid model membranes revealed by neutron diffraction and H NMR experiments.
[So] Source:Biochim Biophys Acta;1859(5):745-755, 2017 05.
[Is] ISSN:0006-3002
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The stratum corneum (SC) provides the main barrier properties in native skin. The barrier function is attributed to the intercellular lipids, forming continuous multilamellar membranes. In this study, SC lipid membranes in model ratios were enriched with deuterated lipids in order to investigate structural and dynamical properties by neutron diffraction and H solid-state NMR spectroscopy. Further, the effect of the penetration enhancer isopropyl myristate (IPM) on the structure of a well-known SC lipid model membrane containing synthetically derived methyl-branched ceramide [EOS], ceramide [AP], behenic acid and cholesterol (23/10/33/33wt%) was investigated. IPM supported the formation of a single short-periodicity phase (SPP), in which we determined the molecular organization of CER[AP] and CER[EOS]-br for the first time. Furthermore, the thermotropic phase behavior of the lipid system was analyzed by additional neutron diffraction studies as well as by H solid-state NMR spectroscopy, covering temperatures of 32°C (physiological skin temperature), 50°C, and 70°C with a subsequent cooldown back to skin temperature. Both techniques revealed a phase transition and a hysteresis effect. During the cooldown, Bragg peaks corresponding to a long-periodicity phase (LPP) appeared. Additionally, H NMR revealed that the IPM molecules are isotopic mobile at all temperatures.
[Mh] Termos MeSH primário: Epiderme/química
Bicamadas Lipídicas/química
Espectroscopia de Ressonância Magnética/métodos
Miristatos/farmacologia
Difração de Nêutrons/métodos
[Mh] Termos MeSH secundário: Ceramidas/química
Transição de Fase
Temperatura Cutânea
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Ceramides); 0 (Lipid Bilayers); 0 (Myristates); 0RE8K4LNJS (isopropyl myristate)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170831
[Lr] Data última revisão:
170831
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170131
[St] Status:MEDLINE


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[PMID]:27696467
[Au] Autor:Oppolzer D; Barroso M; Passarinha L; Gallardo E
[Ad] Endereço:Centro de Investigação em Ciências da Saúde (CICS-UBI), Universidade da Beira Interior, Covilhã, Portugal.
[Ti] Título:Determination of ethyl glucuronide and fatty acid ethyl esters in hair samples.
[So] Source:Biomed Chromatogr;31(4), 2017 Apr.
[Is] ISSN:1099-0801
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Hair testing for alcohol biomarkers is an important tool for monitoring alcohol consumption. We propose two methods for assessing alcohol exposure through combined analysis of ethyl glucuronide (EtG) and fatty acid ethyl esters (FAEEs) species (ethyl myristate, palmitate, stearate and oleate) in hair (30 mg). EtG was analysed by liquid chromatography-tandem mass spectrometry, while FAEEs were analysed by gas chromatography-tandem mass spectrometry using electron impact ionization. Both methods were validated according to internationally accepted guidelines. Linearity was proven between 3 and 500 pg/mg for EtG and 30-5000 pg/mg for FAEEs, and the limits of quantification were 3 pg/mg for EtG and 30 pg/mg for each of the four FAEEs. Precision and accuracy were considered adequate, processed EtG samples were found to be stable for up to 96 h left in the injector and processed FAEEs samples for up to 24 h. Matrix effects were not significant. Both methods were applied to the analysis of 15 authentic samples, using the cut-off values proposed by the Society of Hair Testing for interpretation. The results agreed well with the self-reported alcohol consumption in most cases, and demonstrated the suitability of the methods to be applied in routine analysis of alcohol biomarkers, allowing monitoring consumption using low sample amounts.
[Mh] Termos MeSH primário: Ésteres/análise
Ácidos Graxos/análise
Glucuronatos/análise
Cabelo/química
[Mh] Termos MeSH secundário: Adulto
Consumo de Bebidas Alcoólicas/metabolismo
Biomarcadores/análise
Pré-Escolar
Ácidos Graxos/química
Cromatografia Gasosa-Espectrometria de Massas/métodos
Seres Humanos
Limite de Detecção
Miristatos/análise
Ácidos Oleicos/análise
Ácidos Palmíticos/análise
Reprodutibilidade dos Testes
Extração em Fase Sólida
Estearatos/análise
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers); 0 (Esters); 0 (Fatty Acids); 0 (Glucuronates); 0 (Myristates); 0 (Oleic Acids); 0 (Palmitic Acids); 0 (Stearates); 17685-04-0 (ethyl glucuronide); 6995S49749 (ethyl myristate); C64RTC734W (ethyl stearate); IRD3M534ZM (ethyl palmitate); Z2Z439864Y (ethyl oleate)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170317
[Lr] Data última revisão:
170317
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161004
[St] Status:MEDLINE
[do] DOI:10.1002/bmc.3858


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[PMID]:27491272
[Au] Autor:Ilbasmis-Tamer S; Tugcu-Demiroz F; Degim IT
[Ad] Endereço:a Faculty of Pharmacy, Department of Pharmaceutical Technology , Gazi University , Etiler , Ankara , Turkey.
[Ti] Título:Carbon nanotube membranes to predict skin permeability of compounds.
[So] Source:Pharm Dev Technol;22(4):606-616, 2017 Jun.
[Is] ISSN:1097-9867
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In the present study, carbon nanotube (CNT) membranes were prepared to predict skin penetration properties of compounds. A series of penetration experiments using Franz diffusion cells were performed with 16 different membrane compositions for model chemicals. Similar experiments were also carried out with same model molecules using five different commercially available synthetic membranes and human skins for the comparison. Model chemicals were selected as diclofenac, dexketoprofen and salicylic acid. Their permeability coefficients and flux values were calculated. Correlations between permeability values of model compounds for human skins and developed model membranes were investigated. Good correlations were obtained for CNT membrane, isopropyl myristate-treated CNT membrane (IM-CNT membrane) and bovine serum albumin-cholesterol, dipalmitoyl phosphatidyl choline-treated membrane (BSA-Cholesterol-DPPC-IM-CNT membrane). An artificial neural network (ANN) model was developed using some molecular properties and penetration coefficients from pristine CNT membranes to predict skin permeability values and quite good predictions were made.
[Mh] Termos MeSH primário: Anti-Infecciosos/farmacocinética
Anti-Inflamatórios não Esteroides/farmacocinética
Diclofenaco/farmacocinética
Cetoprofeno/análogos & derivados
Membranas Artificiais
Ácido Salicílico/farmacocinética
Absorção Cutânea
Trometamina/farmacocinética
[Mh] Termos MeSH secundário: Animais
Bovinos
Colesterol/química
Simulação por Computador
Seres Humanos
Cetoprofeno/farmacocinética
Modelos Biológicos
Miristatos/química
Nanotubos de Carbono/química
Nanotubos de Carbono/ultraestrutura
Redes Neurais (Computação)
Permeabilidade
Soroalbumina Bovina/química
Pele/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Membranes, Artificial); 0 (Myristates); 0 (Nanotubes, Carbon); 023C2WHX2V (Tromethamine); 0RE8K4LNJS (isopropyl myristate); 144O8QL0L1 (Diclofenac); 27432CM55Q (Serum Albumin, Bovine); 90Y4QC304K (Ketoprofen); 97C5T2UQ7J (Cholesterol); N674F7L21E (dexketoprofen trometamol); O414PZ4LPZ (Salicylic Acid)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160806
[St] Status:MEDLINE
[do] DOI:10.1080/10837450.2016.1221430


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[PMID]:27019055
[Au] Autor:Rajpoot K
[Ad] Endereço:a Pharmaceutical Research Project Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour Vishwavidyalaya , Sagar , Madhya Pradesh , India.
[Ti] Título:Acyclovir-loaded sorbitan esters-based organogel: development and rheological characterization.
[So] Source:Artif Cells Nanomed Biotechnol;45(3):551-559, 2017 May.
[Is] ISSN:2169-141X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Herein, a nanoemulsion-based organogel (NEOG) system loaded with acyclovir has been developed for the effective treatment of herpes simplex virus infection via topical delivery. Pseudo-ternary phase diagram exhibited increase in non-birefrigent, optically isotropic region of organogel with Smix (K ) ratio. The NEOG C showed good storage (G') and loss moduli (G″), and more compact network structures. Gel-sol transition temperature (Tg) and fractal dimension (D ) of NEOG system revealed increased density of the tubular network with K . Hence, high gelling ability of the developed NEOG system may attribute to the combination of sustained and site-specific delivery of drugs.
[Mh] Termos MeSH primário: Aciclovir/metabolismo
Antivirais/metabolismo
Géis/química
Hexoses/química
Miristatos/química
[Mh] Termos MeSH secundário: Aciclovir/química
Aciclovir/farmacologia
Animais
Antivirais/química
Antivirais/farmacologia
Transporte Biológico
Portadores de Fármacos
Composição de Medicamentos
Liberação Controlada de Fármacos
Emulsões
Ésteres
Hexoses/metabolismo
Concentração de Íons de Hidrogênio
Cinética
Miristatos/metabolismo
Permeabilidade
Transição de Fase
Reologia
Pele/efeitos dos fármacos
Pele/metabolismo
Suínos
Técnicas de Cultura de Tecidos
Viscosidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Drug Carriers); 0 (Emulsions); 0 (Esters); 0 (Gels); 0 (Hexoses); 0 (Myristates); 0RE8K4LNJS (isopropyl myristate); NVZ4I0H58X (sorbitan monostearate); X4HES1O11F (Acyclovir)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170224
[Lr] Data última revisão:
170224
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160329
[St] Status:MEDLINE
[do] DOI:10.3109/21691401.2016.1161639


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[PMID]:26983378
[Au] Autor:Ploutz M; Aliku T; Bradley-Hewitt T; Dantin A; Lemley B; Gillespie CW; Lwabi P; Sable C; Beaton A
[Ad] Endereço:1Division of Cardiology,Children's National Health System,Washington,District of Columbia,United States of America.
[Ti] Título:Child and teacher acceptability of school-based echocardiographic screening for rheumatic heart disease in Uganda.
[So] Source:Cardiol Young;27(1):82-89, 2017 Jan.
[Is] ISSN:1467-1107
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Introduction Rheumatic heart disease causes substantial morbidity in children in low-income countries. School-based echocardiographic screening has been suggested as a means to identify children with latent disease; however, little is known about the experience of children and teachers participating in screenings. The aim of our study was to assess students' and teachers' experience of school-based echocardiographic screening and identify areas for improvement. Materials and methods A school-based echocardiographic screening programme was conducted in five schools in Northern Uganda in 2013. After 8 months, an age- and gender-stratified population that included 5% of the participating students and teachers completed a questionnaire via an in-person interview. Responses were reviewed by question and coded to identify key themes. RESULTS: A total of 255 students (mean 10.7 years; 48% male) and 35 teachers participated in our study. In total, 95% of the students and 100% of the teachers were happy to have participated in the screening; however, students reported feeling scared (35%) and nervous (48%) during the screening process. Programmatic strengths included the following: knowing one's health status, opportunity to receive treatment, and staff interactions. Although 43% of the patients did not suggest a change with open-ended questioning, concerns regarding privacy, fear of the screening process, and a desire to include others in the community were noted. Discussion School-based echocardiographic rheumatic heart disease screening was well received by students and teachers. Future programmes would likely benefit from improved pre-screening education regarding the screening process and diagnosis of rheumatic heart disease. Furthermore, education of teachers and students could improve screening perception and establish realistic expectations regarding the scope of screening.
[Mh] Termos MeSH primário: Atitude Frente à Saúde
Ecocardiografia/métodos
Programas de Rastreamento/métodos
Cardiopatia Reumática/diagnóstico
Instituições Acadêmicas
Estudantes
[Mh] Termos MeSH secundário: Adolescente
Compostos de Cetrimônio
Criança
Pré-Escolar
Combinação de Medicamentos
Feminino
Seres Humanos
Masculino
Miristatos
Ácidos Nicotínicos
Estudos Retrospectivos
Cardiopatia Reumática/epidemiologia
Simeticone
Ácidos Esteáricos
Inquéritos e Questionários
Uganda/epidemiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cetrimonium Compounds); 0 (Drug Combinations); 0 (Myristates); 0 (Nicotinic Acids); 0 (Stearic Acids); 135583-60-7 (Prevasore); 8050-81-5 (Simethicone)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170321
[Lr] Data última revisão:
170321
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160318
[St] Status:MEDLINE
[do] DOI:10.1017/S1047951116000159


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[PMID]:26738443
[Au] Autor:Üstündag Okur N; Çaglar ES; Arpa MD; Karasulu HY
[Ad] Endereço:a Department of Pharmaceutical Technology , School of Pharmacy, Istanbul Medipol University , Beykoz , Istanbul , Turkey and.
[Ti] Título:Preparation and evaluation of novel microemulsion-based hydrogels for dermal delivery of benzocaine.
[So] Source:Pharm Dev Technol;22(4):500-510, 2017 Jun.
[Is] ISSN:1097-9867
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The purpose of the current research was to prepare and evaluate the potential use of microemulsion-based hydrogel (MBH) formulations for dermal delivery of benzocaine (BZN). The pseudoternary-phase diagrams were constructed for various microemulsions composed of isopropyl myristate (IPM) as oil phase, Span 20, Tween 20, Tween 80, cremophor EL and cremophor RH40 as surfactants, ethanol as cosurfactant and distilled water as aqueous phase. Finally, concentration of BZN in microemulsions was 2% (w/w). The physicochemical properties, such as conductivity, viscosity, pH, droplet size, polydispersity index and zeta potential of microemulsions, were measured. Carbopol 940 was used to convert BZN-loaded microemulsions into gel form without affecting their structure. Furthermore, excised rat abdominal skin was used to compare permeation and penetration properties of BZN loaded M3 and M3BHs with BZN solution. According to ex vivo study results, BZN-loaded M3BH1 showed highest flux values and high release rate values, and furthermore, this gel formulation had low surfactant content. Finally, in order to learn the localization of formulations within the dermal penetration, formulations and BZN solution were labeled with red oil O and subjected to fluorescence observation. In conclusion, BZN-loaded MBHs could be offered as a promising strategy for dermal drug delivery.
[Mh] Termos MeSH primário: Anestésicos Locais/administração & dosagem
Anestésicos Locais/farmacocinética
Benzocaína/administração & dosagem
Benzocaína/farmacocinética
Emulsões/química
Hidrogéis/química
Absorção Cutânea
[Mh] Termos MeSH secundário: Resinas Acrílicas/química
Administração Cutânea
Animais
Portadores de Fármacos/química
Masculino
Miristatos/química
Polietilenoglicóis/química
Polissorbatos/química
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acrylic Resins); 0 (Anesthetics, Local); 0 (Drug Carriers); 0 (Emulsions); 0 (Hydrogels); 0 (Myristates); 0 (Polysorbates); 0RE8K4LNJS (isopropyl myristate); 30IQX730WE (Polyethylene Glycols); 39279-69-1 (cremophor); 4Q93RCW27E (carbopol 940); U3RSY48JW5 (Benzocaine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170413
[Lr] Data última revisão:
170413
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160108
[St] Status:MEDLINE
[do] DOI:10.3109/10837450.2015.1131716


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[PMID]:27556271
[Au] Autor:Manosroi J; Chankhampan C; Chaikul P; Manosroi W; Manosroi A
[Ad] Endereço:a Department of Pharmaceutical Science, Faculty of Pharmacy , Chiang Mai University , Chiang Mai , Thailand.
[Ti] Título:Transfollicular enhancement of methyl myristate loaded in cationic niosomes incorporated in hair lotion.
[So] Source:J Microencapsul;33(6):585-594, 2016 Sep.
[Is] ISSN:1464-5246
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Hair lotion containing methyl myristate loaded in cationic niosomes (HL-MMnio) composed of Brij72/cholesterol/DDAB at 7:3:0.65 molar ratio was developed. The remaining percentages of MM loaded in cationic niosomes in hair lotion were higher than free MM in hair lotion of about 1.2 times. The cumulative amounts in porcine skin and the receiver compartment of MM loaded in cationic niosomes incorporated in hair lotion were higher than those of free MM in hair lotion of 1.45 and 1.32 times, respectively. HL-MMnio showed very slightly irritation on rabbit skin, which was disappeared after 4 d. For melanogenesis induction in C57BL/6 mice with aged-induced grey body coat hairs, the highest pigmentation scores of HL-MMnio applied on the dorsal area were observed after 21 days, while hair lotion containing the free MM indicated after 35 days. This study has suggested that HL-MMnio was the high potential formulation for canities treatment.
[Mh] Termos MeSH primário: Colesterol
Cosméticos
Folículo Piloso/metabolismo
Miristatos
Polietilenoglicóis
Compostos de Amônio Quaternário
[Mh] Termos MeSH secundário: Animais
Colesterol/química
Colesterol/farmacologia
Cosméticos/química
Cosméticos/farmacologia
Lipossomos
Masculino
Camundongos
Miristatos/química
Miristatos/farmacologia
Polietilenoglicóis/química
Polietilenoglicóis/farmacologia
Compostos de Amônio Quaternário/química
Compostos de Amônio Quaternário/farmacologia
Coelhos
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cosmetics); 0 (Liposomes); 0 (Myristates); 0 (Quaternary Ammonium Compounds); 13146-86-6 (didodecyldimethylammonium); 30IQX730WE (Polyethylene Glycols); 97C5T2UQ7J (Cholesterol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170330
[Lr] Data última revisão:
170330
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160825
[St] Status:MEDLINE


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[PMID]:27447836
[Au] Autor:Yee SW; Giacomini MM; Hsueh CH; Weitz D; Liang X; Goswami S; Kinchen JM; Coelho A; Zur AA; Mertsch K; Brian W; Kroetz DL; Giacomini KM
[Ad] Endereço:Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA.
[Ti] Título:Metabolomic and Genome-wide Association Studies Reveal Potential Endogenous Biomarkers for OATP1B1.
[So] Source:Clin Pharmacol Ther;100(5):524-536, 2016 Nov.
[Is] ISSN:1532-6535
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Transporter-mediated drug-drug interactions (DDIs) are a major cause of drug toxicities. Using published genome-wide association studies (GWAS) of the human metabolome, we identified 20 metabolites associated with genetic variants in organic anion transporter, OATP1B1 (P < 5 × 10 ). Of these, 12 metabolites were significantly higher in plasma samples from volunteers dosed with the OATP1B1 inhibitor, cyclosporine (CSA) vs. placebo (q-value < 0.2). Conjugated bile acids and fatty acid dicarboxylates were among the metabolites discovered using both GWAS and CSA administration. In vitro studies confirmed tetradecanedioate (TDA) and hexadecanedioate (HDA) were novel substrates of OATP1B1 as well as OAT1 and OAT3. This study highlights the use of multiple datasets for the discovery of endogenous metabolites that represent potential in vivo biomarkers for transporter-mediated DDIs. Future studies are needed to determine whether these metabolites can serve as qualified biomarkers for organic anion transporters. Quantitative relationships between metabolite levels and modulation of transporters should be established.
[Mh] Termos MeSH primário: Ácidos e Sais Biliares/sangue
Ácidos Dicarboxílicos/sangue
Ácidos Graxos/sangue
Estudo de Associação Genômica Ampla
Metabolômica
Membro 1b1 da Família de Transportadores de Ânion Orgânico Carreador de Soluto/genética
Membro 1b1 da Família de Transportadores de Ânion Orgânico Carreador de Soluto/metabolismo
[Mh] Termos MeSH secundário: Biomarcadores/metabolismo
Ciclosporina/farmacologia
Interações Medicamentosas/genética
Células HEK293
Seres Humanos
Miristatos/metabolismo
Proteína 1 Transportadora de Ânions Orgânicos/metabolismo
Transportadores de Ânions Orgânicos Sódio-Independentes/metabolismo
Ácidos Palmíticos/metabolismo
Pravastatina/farmacologia
Membro 1b1 da Família de Transportadores de Ânion Orgânico Carreador de Soluto/antagonistas & inibidores
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bile Acids and Salts); 0 (Biomarkers); 0 (Dicarboxylic Acids); 0 (Fatty Acids); 0 (Myristates); 0 (Organic Anion Transport Protein 1); 0 (Organic Anion Transporters, Sodium-Independent); 0 (Palmitic Acids); 0 (SLCO1B1 protein, human); 0 (Solute Carrier Organic Anion Transporter Family Member 1b1); 0 (organic anion transport protein 3); 505-54-4 (hexadecanedioic acid); 83HN0GTJ6D (Cyclosporine); KXO2KT9N0G (Pravastatin)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171017
[Lr] Data última revisão:
171017
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:160723
[St] Status:MEDLINE
[do] DOI:10.1002/cpt.434



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