RESUMEN
2-O-α-d-Glucopyranosyl-l-ascorbic acid (AA-2G) is one of the stable ascorbic acid (AA) derivatives known as provitamin C agents. We have previously synthesized two types of monoacylated derivatives of AA-2G, 6-O-acyl-2-O-α-d-glucopyranosyl-l-ascorbic acids having a straight-acyl chain of varying length from C4 to C18 (6-sAcyl-AA-2G) and a branched-acyl chain of varying length from C6 to C16 (6-bAcyl-AA-2G) in order to improve the bioavailability of AA-2G. In this study, 6-sAcyl-AA-2G and 6-bAcyl-AA-2G per se showed the inhibitory effects on hyaluronidase activity and degranulation. 6-sAcyl-AA-2G exhibited strong inhibitory effects on hyaluronidase activity and degranulation in a concentration-dependent manner, and the inhibitory effects tended to become stronger with increasing length of the acyl chain. 2-O-α-d-Glucopyranosyl-6-O-hexadecanoyl-l-ascorbic acid (6-sPalm-AA-2G), which has a straight C16 acyl chain, was the most potent effective for inhibition of hyaluronidase activity and for inhibition of degranulation among the 6-sAcyl-AA-2G derivatives and the two isomers of 6-sPalm-AA-2G. Furthermore, percutaneous administration of 6-sPalm-AA-2G significantly inhibited IgE-mediated passive cutaneous anaphylaxis reaction in mice. These findings suggest that 6-sPalm-AA-2G will be useful for treatment of allergies.
Asunto(s)
Antialérgicos/química , Antialérgicos/farmacología , Ácido Ascórbico/análogos & derivados , Hialuronoglucosaminidasa/antagonistas & inhibidores , Animales , Antialérgicos/administración & dosificación , Ácido Ascórbico/administración & dosificación , Ácido Ascórbico/química , Ácido Ascórbico/farmacología , Degranulación de la Célula , Línea Celular , Humanos , Hipersensibilidad/tratamiento farmacológico , Masculino , Ratones Endogámicos ICR , Azúcares Ácidos/química , Azúcares Ácidos/farmacologíaRESUMEN
Quercetin, luteolin and chrysoeriol were identified from rooibos tea as degranulation inhibitors in rat basophilic leukaemia cells. The degranulation inhibitory activity of chrysoeriol was first discovered in the present study. When quercetin, luteolin and chrysoeriol were mixed in the ratio that occurs in rooibos tea extract, the mixture inhibited antigen- and calcium ionophore-stimulated degranulation to the same degree as that by the whole rooibos tea extract. These findings indicate that these three flavonoids are the key factors underlying the degranulation inhibitory activity of rooibos tea.
Asunto(s)
Aspalathus/química , Degranulación de la Célula/efectos de los fármacos , Tés de Hierbas , Animales , Antialérgicos/farmacología , Basófilos/patología , Ionóforos de Calcio/farmacología , Línea Celular Tumoral , Flavonas/farmacología , Leucemia/patología , Luteolina/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Quercetina/farmacología , Ratas , Tés de Hierbas/análisisRESUMEN
The purpose of our study was to assess the mechanical effect on tattoo seals and eye makeup caused by a spatial magnetic gradient in the magnetic resonance imaging (MRI) system. Seven kinds of tattoo seals and three kinds of eye makeup, i.e., mascara, eye shadow, and eyeliner were used. On a 3.0-Tesla MRI, we determined these deflection angles according to a method established by the American Society for Testing and Materials (ASTM) at the position that produced the greatest magnetically induced deflection. Eighty-five percent of the tattoo seals showed deflection angles greater than 45 degrees of the ASTM guidelines, and the mascara and eye shadow showed over 40 degrees. This was because these contained ferromagnetic pigments such as an iron oxide, but those translational forces were very small owing to slight mass. However, it is desirable that these should be removed before MRI examination to prevent secondary problems.