Asunto(s)
Alpinia , Antiinflamatorios/uso terapéutico , Antipruriginosos/uso terapéutico , Edema/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Prurito/tratamiento farmacológico , Enfermedades de la Piel/tratamiento farmacológico , Administración Tópica , Animales , Antiinflamatorios/administración & dosificación , Antipruriginosos/administración & dosificación , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Oído , Edema/inducido químicamente , Indometacina , Medicina Tradicional China , Ratones , Ratones Endogámicos ICR , Fitoterapia , Extractos Vegetales/administración & dosificación , Prurito/inducido químicamente , Enfermedades de la Piel/inducido químicamenteRESUMEN
Two kaempferol glycosides were isolated from green tea seed extract (GTSE). After conducting a structure analysis, these two compounds were identified as kaempferol-3-O-[2-O-beta-D-galactopyranosyl-6-O-alpha-L-rhamnopyranosyl]-beta-D-glucopyranoside (compound 1) and kaempferol-3-O-[2-O-beta-D-xylopyranosyl-6-O-alpha-L-rhanmopyranosyl]-beta-D-glucopyranoside (compound 2). These two compounds were hydrolysed by o-glycolytic enzymes for the production of kaempferol. After performing several reactions, we found the optimum enzyme combination, a reaction with beta-galactosidase and hesperidinase. Finally, we produced kaempferol of above 95% purity. The 5alpha-reductase inhibition activities of GTSE hydrolysate (GTSE-H) containing kaempferol were evaluated by the contact cell-based metabolic method using a stable HEK 293 cell line. GTSE-H showed a good inhibition effect on HEK 293 cell lines both type 1 and type 2 on 5alpha-reductase. Especially, GTSE-H inhibited type 2 with kaempferol content dependency. The results indicate that the inhibition activity of hydrolysate on 5alpha-reductase type 2 increases in accordance with kaempferol content.
Asunto(s)
Inhibidores Enzimáticos/farmacología , Oxidorreductasas/antagonistas & inhibidores , Semillas/química , Té/química , Línea Celular , Cromatografía Líquida de Alta Presión , Color , Flavonoides/química , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Glicosilación/efectos de los fármacos , Humanos , Hidrólisis , Estructura Molecular , Oxidorreductasas/genética , Oxidorreductasas/metabolismo , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/metabolismo , Extractos Vegetales/farmacologíaRESUMEN
Ginsenosides, the major active ingredients of ginseng, show a variety of biomedical efficacies such as antiaging and antioxidation. Here, we investigate the protective activity of the ginsenoside F1, an enzymatically modified derivative of ginsenoside Rg1, against ultraviolet-B-induced damage in human HaCaT keratinocytes. Ginsenoside F1 significantly reduced ultraviolet-B-induced cell death and protected HaCaT cells from apoptosis caused by ultraviolet B irradiation. Furthermore, ginsenoside F1 prevented ultraviolet-B-induced cleavage of poly(ADP-ribose) polymerase in HaCaT cells. In search of the molecular mechanism responsible for the antiapoptotic effect of ginsenoside F1, we find that protection from ultraviolet-B-induced apoptosis is tightly correlated with ginsenoside-F1-mediated inhibition of ultraviolet-B-induced downregulation of Bcl-2 and Brn-3a expression.
