RESUMEN
OBJECTIVE: To observe the clinical efficacy and safety of electroacupuncture (EA) combined with herbal acupoint sticking in the treatment of Bell's palsy and provide optimizations for the clinic. METHODS: One hundred and two cases of Bell's palsy were randomized into an EA combined with herbal acupoint sticking group (group A, 50 cases) and an EA group (group B, 52 cases), EA at Cuanzhu (BL 2), Yangbai (GB 14), Taiyang (EX-HN 5), Quanliao (SI 18),Xiaguan (ST 7), Yingxiang (LI 20), etc. were applied in both groups and "facial paralys No.I " was applied at Yifeng (TE 17) in group A, once daily and 10 times totally were needed. The score of facial nerve function, clinical efficacy were compared before and after treatment. At 1 and 3 month follow up visit, the quality of life scale( WHOQOL-BREF) and the occurrence of complication were observed. RESULTS: The scores of facial nerve function in group A and group B were all significantly improved compared with those before treatment (48. 2+/- 2. 9 vs 25. 7 +/- 4. 9, 45. 9 +/- 6. 2 vs 25. 8 +/- 5. 5, both P
Asunto(s)
Puntos de Acupuntura , Parálisis de Bell/terapia , Medicamentos Herbarios Chinos/administración & dosificación , Electroacupuntura , Administración Cutánea , Adolescente , Adulto , Anciano , Parálisis de Bell/tratamiento farmacológico , Terapia Combinada , Femenino , Humanos , Masculino , Persona de Mediana Edad , Resultado del Tratamiento , Adulto JovenRESUMEN
Sulfation and glucuronidation are the principal metabolic pathways of flavonoids, and extensive phase II metabolism is the main reason for their poor bioavailabilities. The purpose of this study was to compare the similarities and differences in the positional preference of glucuronidation versus sulfation in the mouse liver S9 fraction. The conjugating rates of seven monohydroxyflavones (HFs) (i.e., 2'-, 3'-, 4'-, 3-, 5-, 6-, and 7-HF), and five dihydroxyflavones (diHFs) (i.e., 6,7-, 4',7-, 3,7-, 5,7-, and 3,4'-diHF) were determined in three separate enzymatic reaction systems: (A) sulfation only, (B) glucuronidation only, or (C) simultaneous sulfation and glucuronidation (i.e., Sult-Ugt coreaction). In general, glucuronidation rates were much faster than sulfation rates. Among the HFs, 7-HF was the best substrate for both conjugation reactions, whereas 3-HF was rapidly glucuronidated but was not sulfated. As a result, the rank order of sulfation was very different from that of glucuronidation. Among the diHFs, regiospecific glucuronidation was limited to 7-OH and 3-OH positions, whereas regiospecific sulfation was limited to 7-OH and 4'-OH positions. Other positions (i.e., 6-OH and 5-OH) in diHFs were not conjugated. The positional preferences were essentially maintained in a Sult-Ugt coreaction system, although sulfation was surprisingly enhanced. Lastly, sulfation and glucuronidation displayed different regiospecific- and substrate-dependent characteristics. In conclusion, glucuronidation and sulfation shared the same preference for 7-OH position (of flavonoids) but displayed unique preference in other positions in that glucuronidation preferred the 3-OH position whereas sulfation preferred the 4'-OH position.
Asunto(s)
Flavonoides/química , Flavonoides/metabolismo , Glucurónidos/metabolismo , Hígado/metabolismo , Sulfatos/metabolismo , Animales , Flavonas/análisis , Flavonas/química , Flavonas/metabolismo , Cinética , Hígado/enzimología , Masculino , RatonesRESUMEN
OBJECTIVES: Sulfation via sulfotransferases is an important metabolic pathway contributing to the low bioavailability of flavonoids. This study aims to characterize the sulfation of mono-hydroxyflavones (MHFs) to obtain useful information on structure-metabolizing relationships in animal species and gender differences. METHODS: Three representative MHFs, namely, 7-, 6- and 4'-MHF, were studied by incubating each MHF at different concentrations with various liver S9 fractions (mouse, rat, dog and human). KEY FINDINGS: One mono-sulfate was identified for each MHF. 7-MHF and 4'-MHF usually have greater sulfations than 6-MHF. Regardless of whether the S9 fraction came from a male or female, there was a difference in sulfation in the species observed for all MHFs; the highest activity of sulfotransferases was in dog S9. Furthermore, gender differences affect sulfation of MHFs significantly. In rats, all sulfations for the three MHFs were higher in males than that in females while the opposite was observed in mice. CONCLUSIONS: Regiospecific, species and gender dependence exist in the sulfonation of all selected MHFs.
Asunto(s)
Citosol/enzimología , Flavonas/metabolismo , Microsomas Hepáticos/enzimología , Sulfotransferasas/metabolismo , Animales , Citosol/metabolismo , Perros , Femenino , Flavonas/química , Flavonoides/química , Flavonoides/metabolismo , Humanos , Hidroxilación , Isomerismo , Masculino , Ratones , Microsomas Hepáticos/metabolismo , Concentración Osmolar , Ratas , Ratas Endogámicas F344 , Caracteres Sexuales , Especificidad de la Especie , Especificidad por SustratoRESUMEN
OBJECTIVE: To determine the concentration of ginsenoside Rb(2) and study the absorption characteristics of ginsenoside Rb(2) in Caco-2 cell monolayer. METHODS: LC-MS-MS was used to determine the concentration of ginsenoside Rb(2), and the apparent permeability coefficient (P(app)) of ginsenoside Rb(2) was calculated. RESULTS: P(app(AP-BL)) was 3.27 x 10(-7) cm.s(-1), P(app(BL-AP)) was 3.16 x 10(-6) cm.s(-1), and the efflux ratio (P(app(BL-AP))/P(app(AP-BL))) was 9.63. CONCLUSION: The absorption characteristics of ginsenoside Rb(2) in Caco-2 cell model have been demonstrated.