RESUMEN
In continuation of development of bioactive inositol derivatives, a 1-O-methyl derivative of 5-amino-5-deoxy-L-talo-quercitol was designed and synthesized as an analogue of the strong alpha-fucosidase inhibitor, 5a-carba-alpha-L-fucopyranosylamine, the methyl branch being replaced with methoxyl, and demonstrated to be a moderate alpha-fucosidase inhibitor. The present approach provides a possible route to apply alkyl ethers of aminodeoxyinositols as hexopyranose mimics of biological interest.
Asunto(s)
Ciclohexanos/síntesis química , Ciclohexanos/farmacología , Diseño de Fármacos , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/farmacología , Glicósido Hidrolasas/antagonistas & inhibidores , alfa-L-Fucosidasa/antagonistas & inhibidores , Animales , Bovinos , Café/enzimología , Ciclohexanos/química , Inhibidores Enzimáticos/química , Riñón/enzimología , Hígado/enzimología , Estructura Molecular , Prunus/enzimología , Relación Estructura-ActividadRESUMEN
The effect of powdered green tea on the lipid metabolism was studied in male Zucker rats fed a 50% sucrose diet containing 15% butter. The oral treatment of 130 mg powdered green tea per day depressed body weight increase and various adipose tissue weights but food intake was unaffected. The treatment also slightly increased the plasma triglycerides. These effects were likely mediated by the inhibition of lipogenesis in the adipose tissues. The experimental group had a higher concentration of liver total lipid, triglycerides and plasma protein, and lower liver weights than the controls. This may be due to lipid deposition in the liver because of the reduction in adipose tissue weights. It was found that powdered green tea lowered the plasma total cholesterol but liver total cholesterol was unaffected. The results indicate that the hypocholesterolemic activity of powdered green tea might be due to the inhibition of the synthesis of cholesterol in the liver.
Asunto(s)
Tejido Adiposo/efectos de los fármacos , Anticolesterolemiantes/farmacología , Bebidas , Extractos Vegetales/farmacología , Tejido Adiposo/crecimiento & desarrollo , Animales , Peso Corporal/efectos de los fármacos , Colesterol/biosíntesis , Colesterol/sangre , Grasas de la Dieta/administración & dosificación , Hígado/efectos de los fármacos , Hígado/crecimiento & desarrollo , Hígado/metabolismo , Masculino , Tamaño de los Órganos/efectos de los fármacos , Ratas , Ratas ZuckerRESUMEN
We studied the effect of powdered green tea on intracellular superoxide dismutase activity in the adipose conversion of 3T3-L1 cells. By the 14 days of culture with insulin, the triglyceride concentration was increased. When powdered green tea and insulin were added simultaneously, the increased triglyceride content was decreased (p < 0.05), and the superoxide dismutase activities were significantly enhanced (p < 0.05). These data suggest that green tea may have an antilipogenic activity due to its radical scavenging activity mechanism.