RESUMO
In the last years, proteomic investigation provided a powerful tool in molecular characterization of complex allergen sources with relevant implications in both diagnosis and immunotherapic treatment of allergies. We followed a proteomic approach to characterize ryegrass (Lolium perenne) pollen, a common cause of seasonal allergic diseases affecting an increasing part of world population. Peptide shotgun experiments performed on nanoLiquid Ultra Pressure Chromatography coupled with fast Q-TOF MS-MS/MS acquisition protocols (MS(E)) and 2-DE immunoblot combined with MALDI-TOF-TOF analysis allowed the detection of all previously identified ryegrass allergens. Comparative analysis of immunoblot highlighted a class of patients characterized by a more complex 2-DE pattern associated with increased levels of IgE antibodies and by higher susceptibility to multiple sensitization toward different allergen sources. Cluster analysis revealed that all these patients recognized profilin, considered the main cross-reactive allergen in grass pollen. Furthermore, mass spectrometry analysis revealed the presence of other IgE reactive components in ryegrass pollen that might be involved in polysensitization, such as cyclophilin, fructosyltransferase and legumin-like protein.
Assuntos
Imunoglobulina E/imunologia , Lolium/imunologia , Pólen/imunologia , Proteômica/métodos , Rinite Alérgica Sazonal/imunologia , Análise por Conglomerados , Estudos de Coortes , Eletroforese em Gel Bidimensional , Humanos , Immunoblotting , Imunoglobulina E/química , Imunoglobulina E/metabolismo , Lolium/química , Análise Multivariada , Pólen/química , Pólen/metabolismo , Rinite Alérgica Sazonal/metabolismo , Estatísticas não ParamétricasRESUMO
A bioassay-guided separation of a methanolic extract obtained from the roots of Boerhaavia diffusa L. (Nyctaginaceae) allowed us to isolate five compounds belonging to the class of rotenoids: the known boeravinone D ( 1), boeravinone E ( 2), compound 5 and two novel compounds that we have named boeravinone G ( 3) and boeravinone H ( 4). The structures of the new molecules have been determined on the basis of their HR-EI-MS, (1)H- and (13)C-NMR and 2D-NMR (HMQC, HMBC) data. All the isolated rotenoids have been evaluated for their effect on intestinal motility in vitro. Three of them (boeravinone G, boeravinone E and compound 5) exhibited spasmolytic activity. Preliminary structure-activity relationships have been established highlighting the effect of substitutions on rings B and D.
Assuntos
Motilidade Gastrointestinal/efeitos dos fármacos , Nyctaginaceae , Parassimpatolíticos/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Animais , Relação Dose-Resposta a Droga , Cobaias , Masculino , Parassimpatolíticos/administração & dosagem , Parassimpatolíticos/uso terapêutico , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Raízes de PlantasRESUMO
Chemical investigation of Santolina insularis afforded 11 germacrane sesquiterpenes (1-11), four of which (2, 3, 10, and 11) are new. The stereostructures of these compounds have been established by a combination of spectroscopic techniques (mainly NMR), chemical transformations, and application of the modified Mosher method. Compounds 8 and 10 showed a potent and selective cytotoxic activity against the human colon carcinoma cell line.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Asteraceae/química , Plantas Medicinais/química , Sesquiterpenos de Germacrano/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Itália , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Sesquiterpenos de Germacrano/química , Sesquiterpenos de Germacrano/farmacologia , EstereoisomerismoRESUMO
Investigation of the bark of Croton eluteria Bennett for biologically active compounds has led to the isolation of the new prenylbisabolane 3, whose structure was assessed by spectroscopic methods. The corresponding known enone 4 and the eudesmane sesquiterpene 2 were also obtained. Compound 3 proved active in selectively inhibiting the induction of NF-kappaB by tumor necrosis factor-alpha in T cells.
Assuntos
Croton/química , Diterpenos/metabolismo , NF-kappa B/antagonistas & inibidores , NF-kappa B/metabolismo , Extratos Vegetais/metabolismo , Sesquiterpenos/metabolismo , Ciclo Celular/efeitos dos fármacos , Núcleo Celular/metabolismo , Diterpenos/química , Diterpenos/isolamento & purificação , Repetição Terminal Longa de HIV/genética , Humanos , Luciferases/metabolismo , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Linfócitos T/efeitos dos fármacos , Linfócitos T/metabolismo , Fator de Necrose Tumoral alfa/farmacologiaRESUMO
Three new diterpenoids belonging to the clerodane (2-3) and halimane (4) structural types have been isolated from the bark of Croton eluteria Bennet, commonly known as cascarilla. Their structures have been fully characterized by spectroscopic means. Cascarilla extract and its major component, cascarillin, were found to significantly increase histamine-induced gastric acid secretion in the mouse stomach. These preliminary results provide the first rationale for the use of cascarilla in bitter preparations aimed at improving digestion.