RESUMEN
Morin (2´,3, 4´,5,7-pentahydroxyflavone) is a flavonoid with several beneficial health effects. However, its poor water solubility and it sensitivity to several environmental factors avoid its use in applications like pharmaceutical and cosmetic. In this work, we synthetized morin-modified mesoporous silica nanoparticles (AMSNPs-MOR) as useful material to be used as potential nanoantioxidant. To achieve this, we characterized its adsorption kinetics, isotherm and the antioxidant capacity as hydroxyl radical (HOâ¢) scavenger and singlet oxygen (1O2) quencher. The experimental data could be well fitted with Langmuir, Freundlich and Temkin isotherm models, besides the pseudo-second order kinetics model. The total quenching rate constant obtained for singlet oxygen deactivation by AMSNPs-MOR was one order of magnitude lower than the morin rate constant reported previously in neat solvents and lipid membranes. The AMSNPs-MOR have good antioxidant properties by itself and exhibit a synergic effect with morin on the antioxidant property against hydroxyl radical. This effect, in the range of concentrations studied, was increased when the amount of morin adsorbed increased.
Asunto(s)
Antioxidantes/química , Flavonoides/química , Nanopartículas/química , Dióxido de Silicio/química , Adsorción , Radical Hidroxilo/química , Cinética , Tamaño de la Partícula , Porosidad , Oxígeno Singlete/químicaRESUMEN
OBJECTIVES: Aristotelia chilensis leaves (Elaeocarpaceae) are used in Chilean folk medicine to treat pain and inflammation. A bioguided study was carried out on serial extracts (hexane, dichloromethane, methanol, aqueous extract (INFU) and a crude mixture of alkaloids (ALK-MIX). All extracts were evaluated for (1) topical administration against both arachidonic acid and 12-deoxyphorbol-13-decanoate (TPA)-induced inflammation in mice and (2) per-os administration against inflammation by λ-carrageenan-induced paw oedema in guinea-pigs and (3) topical analgesia in tail flick and formalin models and per-os writhing test in mice. METHODS: Greater anti-inflammatory effects were obtained against TPA with dichloromethane extract and methanol extract (63.9 and 66.0%, respectively). INFU showed the most potent effect (56.2%) against arachidonic acid. Greater effects were obtained in the writhing test with hexane and dichloromethane extracts (89.2% both). In the topical analgesia models, all the extracts and ALK-MIX were active with exception of the hexane extract in the formalin assay. In tail flick test, ALK-MIX and the methanol extract were the most active (58.2 and 55.2%, respectively). In relation to the tail formalin assay, the methanol extract (74.1%) was the most active. Concerning antioxidant activity, both INFU and the methanol extract were the most active either in the inhibition of xanthine oxidase (52.9 and 62.7%, respectively) or in the DPPH free radical scavenging activity (EC50 (concentration that produced 50% of activity) = 12.1 and 9.7 µg/ml, respectively). KEY FINDINGS: Aristoteline, aristone, serratoline and hobartinol were isolated from ALK-MIX. Ursolic acid, friedelin and quercetin 5,3'-dimethyl ether were present in the dichloromethane extract while quercetin 3-O-ß-D-glucoside and kaempferol were present in the methanol extract. From INFU were isolated protopine, aristoteline and caffeic and ferulic acids. CONCLUSIONS: The effects of A. chilensis are herein demonstrated, validating its use in traditional medicine. Protopine is reported for the first time in Elaeocarpaceae.
Asunto(s)
Alcaloides/uso terapéutico , Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Antioxidantes/farmacología , Elaeocarpaceae/química , Fitoterapia , Extractos Vegetales/uso terapéutico , Administración Tópica , Alcaloides/farmacología , Analgesia/métodos , Analgésicos/farmacología , Animales , Antiinflamatorios/farmacología , Ácido Araquidónico/antagonistas & inhibidores , Conducta Animal/efectos de los fármacos , Compuestos de Bifenilo/metabolismo , Carragenina , Chile , Edema/tratamiento farmacológico , Femenino , Formaldehído , Cobayas , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Masculino , Medicina Tradicional , Ratones , Ratones Endogámicos , Dolor/tratamiento farmacológico , Ésteres del Forbol , Picratos/metabolismo , Extractos Vegetales/farmacología , Hojas de la Planta/química , Xantina Oxidasa/antagonistas & inhibidoresRESUMEN
El objetivo de este trabajo fue evaluar la irritación y el efecto hidratante de los ésteres de AHA´s. Se evaluó el efecto irritante de los ésteres málico, láctico y salicílico en comparación a sus respectivos ácidos utilizando dos grupos de voluntarios. Las concentraciones de ésteres y AHA´s evaluadas en el primer grupo fueron 1 por ciento, 2,5 por ciento y 5 por ciento en aceite mineral como vehículo. En el segundo grupo se aplicaron ésteres y AHA´s a una concentración de 4 por ciento, 6 por ciento y 8 por ciento en carbomer al 1 por ciento como vehículo. Se determinó el efecto hidratante agudo de los ésteres málico, láctico y salicílico incluidos en una emulsión mediante utilización de un Corneómetro CM 820. Las mediciones se realizaron a los 0,60 y 120 minutos sobre los brazos de voluntarios sanos con piel normal. Los resultados obtenidos, a partir de la Prueba del Parche, fueron sometidos a un análisis estadístico con el que se concluyó que no existieron diferencias estadísticamente significativas entre el potencial de irritación de los ésteres de ácido láctico (EAL), málico (EAM) y salicílico (EAS) en relación a sus respectivos ácidos. Los valores obtenidos en la evaluación del efecto hidratante se analizaron por un método estadístico sin obtener diferencias significativas entre las mediciones (AU)