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1.
J Ethnopharmacol ; 245: 112174, 2019 Dec 05.
Artículo en Inglés | MEDLINE | ID: mdl-31442620

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Propolis has been employed extensively in many cultures since ancient times as antiseptic, wound healing, anti-pyretic and others due to its biological and pharmacological properties, such as immunomodulatory, antitumor, anti-inflammatory, antioxidant, antibacterial, antiviral, antifungal, antiparasite activities. But despite its broad and traditional use, there is little knowledge about its potential interaction with prescription drugs. AIM OF THE STUDY: The main objective of this work was to study the potential herbal-drug interactions (HDIs) of EPP-AF® using an in vivo assay with a cocktail approach. MATERIALS AND METHODS: Subtherapeutic doses of caffeine, losartan, omeprazole, metoprolol, midazolam and fexofenadine were used. Sixteen healthy adult volunteers were investigated before and after exposure to orally administered 125 mg/8 h (375 mg/day) EPP-AF® for 15 days. Pharmacokinetic parameters were calculated based on plasma concentration versus time (AUC) curves. RESULTS: After exposure to EPP-AF®, it was observed decrease in the AUC0-∞ of fexofenadine, caffeine and losartan of approximately 18% (62.20 × 51.00 h.ng/mL), 8% (1085 × 999 h.ng/mL) and 13% (9.01 × 7.86 h.ng/mL), respectively, with all 90% CIs within the equivalence range of 0.80-1.25. On the other hand, omeprazole and midazolam exhibited an increase in AUC0-∞ of, respectively, approximately 18% (18.90 × 22.30 h.ng/mL) and 14% (1.25 × 1.43 h.ng/mL), with the upper bounds of 90% CIs slightly above 1.25. Changes in pharmacokinetics of metoprolol or its metabolite α-hydroxymetoprolol were not statistically significant and their 90% CIs were within the equivalence range of 0.80-1.25. CONCLUSIONS: In conclusion, our study shows that EPP-AF® does not clinically change CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A activities, once, despite statistical significant, the magnitude of the changes in AUC values after EPP-AF® were all below 20% and therefore may be considered safe regarding potential interactions involving these enzymes. Besides, to the best of our knowledge this is the first study to assess potential HDIs with propolis.


Asunto(s)
Cafeína/farmacocinética , Losartán/farmacocinética , Metoprolol/farmacocinética , Midazolam/farmacocinética , Omeprazol/farmacocinética , Própolis , Terfenadina/análogos & derivados , Subfamilia B de Transportador de Casetes de Unión a ATP/metabolismo , Adulto , Cafeína/sangre , Estudios Cruzados , Sistema Enzimático del Citocromo P-450/genética , Sistema Enzimático del Citocromo P-450/metabolismo , Interacciones Farmacológicas , Femenino , Humanos , Losartán/sangre , Masculino , Metoprolol/sangre , Midazolam/sangre , Omeprazol/sangre , Terfenadina/sangre , Terfenadina/farmacocinética
2.
Toxicon ; 112: 59-67, 2016 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-26829652

RESUMEN

Africanized Apis mellifera bees, also known as killer bees, have an exceptional defensive instinct, characterized by mass attacks that may cause envenomation or death. From the years 2000-2013, 77,066 bee accidents occurred in Brazil. Bee venom comprises several substances, including melittin and phospholipase A2 (PLA2). Due to the lack of antivenom for bee envenomation, this study aimed to produce human monoclonal antibody fragments (single chain fragment variable; scFv), by using phage display technology. These fragments targeted melittin and PLA2, the two major components of bee venom, to minimize their toxic effects in cases of mass envenomation. Two phage antibody selections were performed using purified melittin. As the commercial melittin is contaminated with PLA2, phages specific to PLA2 were also obtained during one of the selections. Specific clones for melittin and PLA2 were selected for the production of soluble scFvs, named here Afribumabs: prefix: afrib- (from Africanized bee); stem/suffix: -umab (fully human antibody). Afribumabs 1 and 2 were tested in in vitro and in vivo assays to assess their ability to inhibit the toxic actions of purified melittin, PLA2, and crude bee venom. Afribumabs reduced hemolysis caused by purified melittin and PLA2 and by crude venom in vitro and reduced edema formation in the paws of mice and prolonged the survival of venom-injected animals in vivo. These results demonstrate that Afribumabs may contribute to the production of the first non-heterologous antivenom treatment against bee envenomation. Such a treatment may overcome some of the difficulties associated with conventional immunotherapy techniques.


Asunto(s)
Antivenenos/uso terapéutico , Venenos de Abeja/antagonistas & inhibidores , Diseño de Fármacos , Mordeduras y Picaduras de Insectos/tratamiento farmacológico , Proteínas de Insectos/antagonistas & inhibidores , Meliteno/antagonistas & inhibidores , Anticuerpos de Cadena Única/uso terapéutico , Animales , Antivenenos/genética , Antivenenos/metabolismo , Antivenenos/farmacología , Venenos de Abeja/química , Venenos de Abeja/enzimología , Venenos de Abeja/toxicidad , Técnicas de Visualización de Superficie Celular , Células Clonales , Quimioterapia Combinada , Edema/etiología , Edema/prevención & control , Hemólisis/efectos de los fármacos , Humanos , Mordeduras y Picaduras de Insectos/fisiopatología , Proteínas de Insectos/análisis , Proteínas de Insectos/toxicidad , Masculino , Meliteno/análisis , Meliteno/toxicidad , Ratones , Inhibidores de Fosfolipasa A2/farmacología , Inhibidores de Fosfolipasa A2/uso terapéutico , Fosfolipasas A2 Secretoras/antagonistas & inhibidores , Fosfolipasas A2 Secretoras/toxicidad , Proteínas Recombinantes/aislamiento & purificación , Proteínas Recombinantes/metabolismo , Proteínas Recombinantes/farmacología , Proteínas Recombinantes/uso terapéutico , Anticuerpos de Cadena Única/genética , Anticuerpos de Cadena Única/metabolismo , Anticuerpos de Cadena Única/farmacología , Tejido Subcutáneo/efectos de los fármacos , Análisis de Supervivencia
3.
Phytother Res ; 28(12): 1816-21, 2014 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-25132112

RESUMEN

Type-2 diabetes mellitus (DM) is a highly prevalent disease with significant morbidity and mortality around the world. However, there is no universally effective treatment, because response to different treatment regimens can vary widely among patients. In this study, we aimed to investigate whether the use of the powdered dried leaves of Eugenia punicifolia (Kunth) DC. (Myrtaceae) is effective as an adjuvant to the treatment of patients with type-2 DM. Fifteen patients were enrolled in a pilot, non-controlled study, and received E. punicifolia for 3 months. After treatment, we observed a significant decrease in glycosylated hemoglobin, basal insulin, thyroid-stimulating hormone, C-reactive protein, and both systolic and diastolic blood pressure. There were no changes in fasting and postprandial glycemia. The compounds myricetin-3-O-rhamnoside, quercetin-3-O-galactoside, quercetin-3-O-xyloside, quercetin-3-O-rhamnoside, kaempferol-3-O-rhamnoside, phytol, gallic acid, and trans-caryophyllene present in the powdered dried leaves of E. punicifolia may be responsible for the therapeutic effect. In conclusion, the powdered leaves of E. punicifolia are promising as an adjuvant in the treatment of type-2 DM and deserve further investigation.


Asunto(s)
Diabetes Mellitus Tipo 2/tratamiento farmacológico , Fitoterapia , Syzygium/química , Anciano , Glucemia/metabolismo , Proteína C-Reactiva/metabolismo , Femenino , Hemoglobina Glucada/metabolismo , Humanos , Insulina/sangre , Masculino , Persona de Mediana Edad , Proyectos Piloto , Hojas de la Planta/química
4.
Nurs Ethics ; 20(4): 392-400, 2013 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-23361148

RESUMEN

College students have become more representative as blood donors, mainly to help other people. This study ascertained the association between spirituality and adherence or intention to donate blood in post-graduate students. In this quantitative and cross-sectional study, participants were 281 students from a post-graduate programme at a Brazilian public university. After complying with ethical requirements, data were collected through a questionnaire for sociodemographic characterization and identification of blood donation practices, followed by the Spiritual Well-Being Scale. Descriptive statistics and parametric tests were used for data analysis. A total of 74% of the participants were female and 26% were male. Previous experience and/or intention to donate blood were found in 75.3%; 14.3% donated blood periodically. In addition, 12.2% were not adept to donation and 12.5% were inapt. Spiritual Well-Being scores were similar between individuals who are not adept and those who donate periodically. In conclusion, in the sample, spirituality and blood donation are not associated, but spiritual well-being and gender are. To enhance blood donation, further research is needed.


Asunto(s)
Donantes de Sangre/psicología , Espiritualidad , Estudiantes/psicología , Adulto , Actitud Frente a la Salud , Brasil , Estudios Transversales , Femenino , Conocimientos, Actitudes y Práctica en Salud , Estado de Salud , Humanos , Masculino , Persona de Mediana Edad , Satisfacción Personal , Adulto Joven
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