RESUMEN
The aims of this study were to investigate the potential benefits of antioxidant, anti-inflammatory, anti-hepatotoxic, and anti-tyrosinase activities of a methanolic extract of fresh tea leaves (FTE) (Camellia sinensis L.). The antioxidant capacity was investigated using three different methods at different temperatures. The anti-inflammatory activity was studied in vitro by the inhibition of 5-lipoxygenase assay. The anti-hepatotoxic effect was investigated in CCl4-induced liver injury in rats. The anti-tyrosinase activities of the FTE and its principal phenolic compounds were investigated in l-3,4-dihydroxyphenylalanine (l-DOPA) oxidation by a mushroom tyrosinase. A molecular docking study was conducted to determine how the FTE's principal catechins interact with the tyrosinase. The FTE exhibited the best shelf life at low temperatures and demonstrated concentration-dependent antioxidant, anti-inflammatory, anti-hepatotoxic, and anti-tyrosinase effects compared to positive references. Treatment of rats with the FTE at 2000 mg/kg/day for 28 consecutive days reversed CCl4-induced oxidative damage in hepatic tissues by lowering the levels of alanine aminotransferase by 69% and malondialdehyde by 90%. Our findings suggest that the FTE has the capacity to scavenge free radicals and can protect against oxidative stress induced by CCl4 intoxication. The docking results were consistent with our in vitro data, indicating the anti-tyrosinase potency of the principal catechins.
Asunto(s)
Camellia sinensis/química , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Monofenol Monooxigenasa/antagonistas & inhibidores , Extractos Vegetales/administración & dosificación , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antioxidantes/administración & dosificación , Antioxidantes/química , Antioxidantes/farmacología , Modelos Animales de Enfermedad , Inhibidores Enzimáticos/administración & dosificación , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Masculino , Simulación del Acoplamiento Molecular , Monofenol Monooxigenasa/química , Estrés Oxidativo/efectos de los fármacos , Fenoles/administración & dosificación , Fenoles/química , Fenoles/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , RatasRESUMEN
Pectinate gel beads containing Thai mango seed kernel extract (MSKE, cultivar 'Fahlun') were developed and characterised for the purpose of colon-targeted delivery. The MSKE-loaded pectinate beads were prepared using ionotropic gelation with varying pectin-to-MSKE ratios, MSKE concentrations, and concentrations of two cross-linkers (calcium chloride and zinc acetate). The formulated beads were spherical in shape and ranged in size between 1.13 mm and 1.88 mm. Zinc-pectinate (ZPG) beads containing high amounts of MSKE showed complete entrapment efficiency (EE) of MSKE (100%), while calcium-pectinate (CPG) beads demonstrated 70% EE. The in vitro release tests indicated that MSKE-loaded CPG beads were unstable in both simulated gastric medium (SGM) and simulated intestinal medium (SIM), while MSKE-loaded ZPG beads were stable in SIM but unable to prevent the release of MSKE in SGM. The protection of ZPG beads with gastro-resistant capsules (Eudragit® L 100-55) resulted in stability in both SGM and SIM; they disintegrated immediately in simulated colonic medium containing pectinolytic enzymes. MSKE-loaded ZPG beads were stable at 4, 25 and 45 °C during the study period of four months. The present study revealed that ZPG beads in enteric-coated capsules might be a promising carrier for delivering MSKE to the colon.
Asunto(s)
Sistemas de Liberación de Medicamentos , Mangifera/química , Microesferas , Extractos Vegetales/química , Semillas/química , Calcio/química , Cápsulas/química , Portadores de Fármacos/química , Geles/química , Tamaño de la Partícula , Zinc/químicaRESUMEN
Three polyphenolic principles, 1,2,3,4,6-penta- O-galloyl-beta-D-glucopyranose (PGG), methyl gallate (MG), and gallic acid (GA), were isolated from the ethanolic extract of seed kernels of Thai mango (MSKE) ( MANGIFERA INDICA L. cv. "Fahlun") and quantified using a TLC scanning densitometric method. The MSKE and its isolates were investigated by studying their antioxidant capacities using four different methods, by determining their IN VITRO anti-inflammatory activities, and by evaluating their hepatoprotective potential against liver injury in rats induced by carbon tetrachloride (CCl (4)). The hepatoprotective effect of MSKE is clearly supported by its polyphenolic nature of the main principle, PGG, which exhibited potent antioxidant and anti-inflammatory activities.
Asunto(s)
Antioxidantes/farmacología , Hígado/efectos de los fármacos , Mangifera/embriología , Extractos Vegetales/farmacología , Semillas/química , Animales , Cromatografía Líquida de Alta Presión , Cromatografía en Capa Delgada , Inhibidores de la Lipooxigenasa , Hígado/enzimología , Hígado/patología , Masculino , Extractos Vegetales/normas , Ratas , Ratas Wistar , Análisis Espectral/métodosRESUMEN
Aqueous extracts from seeds of Areca catechu L. (Arecaceae) (AC) and nutgalls of Quercus infectoria Oliv. (Fagaceae) (QI) were investigated for their hepatoprotective potential by studying their antioxidant capacity using four different methods, by determining their in vitro anti-inflammatory activity against 5-lipoxygenase, and by evaluating their hepatoprotective potential against liver injury induced by carbon tetrachloride (CCl(4)) in rats. AC and QI extracts exhibited potent antioxidant and anti-inflammatory activities. Treatment of rats with AC and QI extracts reversed oxidative damage in hepatic tissues induced by CCl(4). It is suggested that extracts rich in either condensed or hydrolysable tannins and known for their potent antioxidant and anti-inflammatory activities, may potentially confer protection against oxidative stress-induced liver injury. These data should contribute to evidence-based traditional medicines for anti-inflammatory and hepatoprotective effects of both extracts.
Asunto(s)
Areca/embriología , Hígado/efectos de los fármacos , Extractos Vegetales/farmacología , Quercus/embriología , Semillas/química , Animales , Masculino , Ratas , Ratas WistarRESUMEN
The alcoholic extract from seed kernels of Thai mango (Mangifera indica L. cv. 'Fahlun') (Anacardiaceae) and its major phenolic principle (pentagalloylglucopyranose) exhibited potent, dose-dependent inhibitory effects on tyrosinase with respect to L-DOPA. Molecular docking studies revealed that the binding orientations of the phenolic principles were in the tyrosinase binding pocket and their orientations were located in the hydrophobic binding pocket surrounding the binuclear copper active site. The results indicated a possible mechanism for their anti-tyrosinase activity which may involve an ability to chelate the copper atoms which are required for the catalytic activity of tyrosinase.