RESUMO
Aerobic exercise training is a promising complementary treatment option in migraine and can reduce migraine days and improve retinal microvascular function. Our aim was to elucidate whether different aerobic exercise programs at high vs moderate intensities distinctly affect migraine days as primary outcome and retinal vessel parameters as a secondary. In this randomized controlled trial, migraine days were recorded by a validated migraine diary in 45 migraineurs of which 36 (female: 28; age: 36 (SD:10)/BMI: 23.1 (5.3) completed the training period (dropout: 20%). Participants were assigned (Strata: age, gender, fitness and migraine symptomatology) to either high intensity interval training (HIT), moderate continuous training (MCT), or a control group (CON). Intervention groups trained twice a week over a 12-week intervention period. Static retinal vessel analysis, central retinal arteriolar (CRAE) and venular (CRVE) diameters, as well as the arteriolar-to-venular diameter ratio (AVR) were obtained for cerebrovascular health assessment. Incremental treadmill testing yielded maximal and submaximal fitness parameters. Overall, moderate migraine day reductions were observed (ηP2 = .12): HIT revealed 89% likely beneficial effects (SMD = 1.05) compared to MCT (SMD = 0.50) and CON (SMD = 0.59). Very large intervention effects on AVR improvement (ηP2 = 0.27), slightly favoring HIT (SMD=-0.43) over CON (SMD=0), were observed. HIT seems more effective for migraine day reduction and improvement of cerebrovascular health compared to MCT. Intermittent exercise programs of higher intensities may need to be considered as an additional treatment option in migraine patients.
Assuntos
Terapia por Exercício , Transtornos de Enxaqueca/prevenção & controle , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Vasos Retinianos/anatomia & histologiaRESUMO
The permeation of essential oils through SkinEthic reconstructed human epidermis, (RHE), was studied in vitro to establish a convenient tool to monitor the kinetics of release of active principles from cosmetic formulations. Twelve days old human epidermis held on polycarbonate disks was revitalized by addition of growth medium and incubated at 37 degrees C in 5% CO(2) atmosphere for five days prior to investigation. A system of six custom designed glass Franz-type diffusion cells were used for the permeation studies at 34 degrees C. The diffusion kinetic for 8 selected terpenes (camphor, carvone, 1,8-cineole, linalool, menthol, alpha-thujone, menthone, t-anethole), chosen as analytical markers of a mixture of plant essential oils contained in a cosmetic formulation, was probed by HS/SPME-GC-MS analysis and elaborated according to Fick's first law to obtain skin permeability coefficients (P(S) = 1.51, 1.47, 1.36, 0.80, 0.62, 0.40 and 0.14x10(-3) cm/h, respectively). The method proved to be sensitive, simple and reproducible, and RHE represents a convenient model for safety/quality assessment of cosmetic formulations.
Assuntos
Cosméticos/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Óleos Voláteis/farmacocinética , Terpenos/farmacocinética , Cultura em Câmaras de Difusão , Epiderme/metabolismo , Humanos , Permeabilidade , Controle de Qualidade , Reprodutibilidade dos Testes , Absorção CutâneaRESUMO
Crude methanolic extracts from both root and cell cultures of Euphorbia calyptrata were investigated and found to be active on the CNS. An active fraction was isolated from the methanolic extract of suspension cultures; this possesses significant depressant activity on the CNS. When compared with the crude methanolic root extract, this fraction showed the presence of some common products, four of which were isolated and characterized as helioscopinolides A, C, D, and E. The pure products, administered intraperitoneally to mice, showed different activities on the CNS. Helioscopinolide C showed a clear depressant activity, helioscopinolide E a mild, short depressant effect, while helioscopinolides A and D had an opposite excitatory effect.
Assuntos
Sistema Nervoso Central/efeitos dos fármacos , Diterpenos/farmacologia , Extratos Vegetais/farmacologia , Animais , Células Cultivadas , Diterpenos/isolamento & purificação , CamundongosRESUMO
1. Ribosome-inactivating proteins were found in high amounts in one line of cells of Phytolacca americana (pokeweed) cultured in vitro and, in less quantity, in lines of Saponaria officinalis (soapwort) and of Zea mays (corn) cells. 2. The main ribosome-inactivating protein from pokeweed cells was purified to homogeneity. It is a protein with Mr 29,000 and basic pI, similar to the 'pokeweed antiviral protein' (PAP), a ribosome-inactivating protein from pokeweed leaves. We propose to call the pokeweed antiviral protein isolated from pokeweed cells PAP-C. 3. PAP-C inactivates ribosomes in a less-than-equimolar ratio, thus inhibiting protein synthesis by a rabbit reticulocyte lysate with an IC50 (concentration causing 50% inhibition) of 0.067 nM (2 ng/ml), and modifies rRNA in a manner apparently identical to that of ricin and other ribosome-inactivating proteins. It inhibits protein synthesis by intact cells with an IC50 of 0.7-3.4 microM, and is toxic to mice with an LD50 of 0.95 mg/kg.
Assuntos
Proteínas de Plantas/metabolismo , Proteínas Ribossômicas/antagonistas & inibidores , Sequência de Aminoácidos , Animais , Sistema Livre de Células , Células Cultivadas , Dados de Sequência Molecular , Extratos Vegetais , RNA Ribossômico , Coelhos , Ribossomos/metabolismoRESUMO
Labelled 2-oxo-2H-1,3-benzoxazine-3(4H)-acetamide (caroxazone), has been synthesized by condensing N-(2-hydroxylbenzyl/glycinamide with 14C phosgene. Metabolic studies were performed administering the labelled drug to man and recovering metabolites from the urines. Beside the unchanged drug, five metabolites were identified and confirmed by synthesis, namely (3,4-dihydro-3-carboxamidomethyl-2-oxo-2H-1,3-benzoxazin-4-yl)urea (IX), N-carboxamidomethyl o-hydroxymethylphenyl carbamate (V), 4-methoxy-2-oxo-2H-1,3-benzoxazine-3(4H)acetamide (VIIIa), 2-oxo-2H-1,3-benzoxazine-3(4H)acetic acid (III) and 4-hydroxy-2-oxo-2H-1,3-benzoxazine-3(4H)acetamide (IV).
Assuntos
Antidepressivos/metabolismo , Oxazinas/metabolismo , Amidas/metabolismo , Amidas/urina , Antidepressivos/urina , Biotransformação , Humanos , Oxazinas/urinaRESUMO
Analogues of peptide ergot alkaloids can be obtained by feeding a producing culture of Claviceps purpurea with an analogue of one of the amino acids of the peptide chain of the alkaloid.
Assuntos
Claviceps/metabolismo , Alcaloides de Claviceps/biossíntese , Aminoácidos/metabolismo , Ergolinas/análogos & derivados , Ergolinas/biossínteseRESUMO
An enzyme immunoassay (EIA) for a penicillin derivative is described with a sensitivity at least at the nanogram level. The label, E. coli beta-galactosidase is a macromolecule of 540 000 daltons: the size of the enzyme and the ease of linking penicilloyl residues to it make it an interesting model to study the effect of the degree of haptenic substitution (DS) in the tracer on the parameters of EIA. Our results show that the affinity of the binding reaction between antibody and tracer is proportional to the DS but the sensitivity of inhibition is not affected, at least not between 1 and 10 penicilloyl residues per GZ molecule. The theoretical consequences and practical applications of multivalent tracers in EIA are discussed.
Assuntos
Penicilinas/análise , Reações Antígeno-Anticorpo , Galactosidases , Técnicas Imunoenzimáticas , Imunoglobulina GAssuntos
Doxorrubicina/síntese química , Vírus AKR da Leucemia Murina , Acilação , Animais , Carcinoma/tratamento farmacológico , Células Cultivadas , Daunorrubicina/síntese química , Daunorrubicina/farmacologia , Daunorrubicina/uso terapêutico , Doxorrubicina/farmacologia , Doxorrubicina/uso terapêutico , Embrião de Mamíferos , Ésteres/síntese química , Feminino , Fibroblastos/efeitos dos fármacos , Células HeLa/efeitos dos fármacos , Leucemia Experimental/tratamento farmacológico , Masculino , Neoplasias Mamárias Experimentais/tratamento farmacológico , Camundongos , Camundongos Endogâmicos C3H , Vírus da Leucemia Murina de Moloney/efeitos dos fármacos , Transplante de Neoplasias , Sarcoma 180/tratamento farmacológico , Sarcoma Experimental/tratamento farmacológicoAssuntos
Pregnadienos/metabolismo , Tecido Adiposo/metabolismo , Animais , Encéfalo/metabolismo , Cães , Fezes/análise , Feminino , Formaldeído/administração & dosagem , Formaldeído/metabolismo , Vida Livre de Germes , Cobaias , Hidroxicorticosteroides/administração & dosagem , Hidroxicorticosteroides/metabolismo , Injeções Intradérmicas , Rim/metabolismo , Fígado/metabolismo , Masculino , Músculos/metabolismo , Hipófise/metabolismo , Pregnadienos/administração & dosagem , Coelhos , Ratos , Ratos Endogâmicos , Pele/metabolismo , Especificidade da Espécie , Esteroides Fluorados/administração & dosagem , Esteroides Fluorados/metabolismo , Timo/metabolismo , Fatores de Tempo , TrítioRESUMO
Distamycin A inhibits deoxyribonucleic acid (DNA)-mediated transformation and transfection in Bacillus subtilis at doses with little or no antibacterial effect. The inhibition of transformation parallels the inhibition of DNA uptake; further-more, during the transformation process, donor DNA molecules become distamycin and deoxyribonuclease resistant at the same time. This demonstrates that the drug acts by inhibiting DNA uptake. Although the drug is known to bind DNA, the inhibition is not related to affinity of the drug for DNA. This is shown by the lack of dependence of the extent of inhibition on DNA concentration, whereas the degree of inhibition depends upon cell concentration. Supporting this view is the fact that transformation by single-stranded DNA was also inhibited, even though the drug does not bind to denatured DNA. Distamycin A probably interferes with transformation by competing with DNA for some unknown bacterial component involved in transport of DNA into the cell.