RESUMEN
A double-blind parallel group comparison design clinical study was conducted in Japanese patients with mild to moderate erectile dysfunction to investigate the efficacy of a supplement containing Pycnogenol® and L-arginine. Subjects were instructed to take a supplement (Pycnogenol® 60 mg/day, L-arginine 690 mg/day and aspartic acid 552 mg/day) or an identical placebo for 8 weeks, and the results were assessed using the five-item erectile domain (IIEF-5) of the International Index of Erectile Function. Additionally, blood biochemistry, urinalysis and salivary testosterone were measured. Eight weeks of supplement intake improved the total score of the IIEF-5. In particular, a marked improvement was observed in 'hardness of erection' and 'satisfaction with sexual intercourse'. A decrease in blood pressure, aspartate transaminase and γ-glutamyl transpeptidase (γ-GTP), and a slight increase in salivary testosterone were observed in the supplement group. No adverse reactions were observed during the study period. In conclusion, Pycnogenol® in combination with L-arginine as a dietary supplement is effective and safe in Japanese patients with mild to moderate erectile dysfunction.
Asunto(s)
Arginina/uso terapéutico , Disfunción Eréctil/tratamiento farmacológico , Flavonoides/uso terapéutico , Adulto , Pueblo Asiatico , Aspartato Aminotransferasas/metabolismo , Presión Sanguínea , Método Doble Ciego , Humanos , Masculino , Persona de Mediana Edad , Satisfacción del Paciente , Erección Peniana , Extractos Vegetales , Testosterona/análisis , gamma-Glutamiltransferasa/metabolismoRESUMEN
We investigated the molecular mechanism underlying the neuroprotective effect of theanine, a green tea component, using primary cultured rat cortical neurons, focusing on group I metabotropic glutamate receptors (mGluRs). Theanine and a group I mGluR agonist, DHPG, inhibited the delayed death of neurons caused by brief exposure to glutamate, and this effect of theanine was abolished by group I mGluR antagonists. Although the administration of glutamate alone decreased the neuronal expression of phospholipase C (PLC)-beta1 and -gamma1, which are linked to group I mGluRs, their expression was equal to the control levels on cotreatment with theanine. Treatment with theanine or DHPG alone for 5-7 days resulted in increased expression of PLC-beta1 and -gamma1, and the action of theanine was completely abolished by group I mGluR antagonists. These findings indicate that group I mGluRs might be involved in neuroprotective effect of theanine by increasing the expression levels of PLC-beta1 and -gamma1.
Asunto(s)
Glutamatos/farmacología , Metoxihidroxifenilglicol/análogos & derivados , Neuronas/efectos de los fármacos , Neuronas/metabolismo , Fármacos Neuroprotectores/farmacología , Receptores de Glutamato Metabotrópico/antagonistas & inhibidores , Receptores de Glutamato Metabotrópico/metabolismo , Animales , Apoptosis/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Corteza Cerebral/citología , Corteza Cerebral/efectos de los fármacos , Corteza Cerebral/embriología , Corteza Cerebral/metabolismo , Relación Dosis-Respuesta a Droga , Ácido Glutámico/farmacología , Isoenzimas/metabolismo , Metoxihidroxifenilglicol/farmacología , Neuronas/citología , Fosfolipasa C beta , Fosfolipasa C gamma , Ratas , Fosfolipasas de Tipo C/metabolismoRESUMEN
Adipocyte dysfunction is strongly associated with the development of obesity and insulin resistance. It is accepted that the regulation of adipocytokine secretion or the adipocyte-specific gene expression is one of the most important targets for the prevention of obesity and amelioration of insulin sensitivity. In this study, we demonstrated that anthocyanins (cyanidin or cyanidin 3-glucoside) have the potency of a unique pharmacological function in isolated rat adipocytes. Treated adipocytes with anthocyanins enhanced adipocytokine (adiponectin and leptin) secretion and up-regulated the adipocyte specific gene expression without activation of PPARgamma in isolated rat adipocytes. The gene expression of adiponectin was also up-regulated in white adipose tissue in mice fed an anthocyanin supplemented diet. As one of the possible mechanisms, AMP-activated protein kinase activation would be associated with these changes, nevertheless, the AMP:ATP ratio was significantly decreased by administration of the anthocyanins. These data suggest that anthocyanins have a potency of unique therapeutic advantage and also have important implications for preventing obesity and diabetes.
Asunto(s)
Adipocitos/efectos de los fármacos , Antocianinas/farmacología , Péptidos y Proteínas de Señalización Intercelular , Proteínas Quinasas Activadas por AMP , Nucleótidos de Adenina/metabolismo , Adipocitos/metabolismo , Adiponectina , Animales , Antocianinas/química , Células Cultivadas , Citocinas/metabolismo , Expresión Génica/efectos de los fármacos , Glucósidos/química , Glucósidos/farmacología , Leptina/genética , Leptina/metabolismo , Ligandos , Masculino , Complejos Multienzimáticos/metabolismo , Proteínas Serina-Treonina Quinasas/metabolismo , Proteínas/genética , Proteínas/metabolismo , ARN Mensajero/metabolismo , Ratas , Ratas Wistar , Receptores Citoplasmáticos y Nucleares/metabolismo , Factores de Transcripción/metabolismoRESUMEN
Modifying potential of annatto extract (norbixin) on liver carcinogenesis was investigated in male F344/DuCrj rats initially treated with N-nitrosodiethylamine (DEN). Two weeks after a single dose of DEN (200 mg/kg, intraperitoneally), rats were given annatto extract at dietary levels of 0, 0.03, 0.1 and 0.3%, or phenobarbital sodium at 0.05% as a positive control for 6 weeks. All animals were subjected to partial hepatectomy at week 3, and were killed at week 8. There were no deaths related to annatto extract ingestion, and the treatment had no effects on body weights, or food and water consumption. Statistically significant increases of absolute and relative liver weights were apparent in the 0.1 and 0.3% groups. However, annatto extract did not significantly increase the quantitative values for glutathione S-transferase placental form positive liver cell foci observed after DEN initiation, in clear contrast to the positive control case. The results thus demonstrate that annatto extract at a dietary level of 0.3% (200 mg/kg/day) lacks modifying potential for liver carcinogenesis in our medium-term bioassay system.
Asunto(s)
Carcinógenos/toxicidad , Carotenoides/toxicidad , Neoplasias Hepáticas/patología , Fenobarbital/toxicidad , Animales , Peso Corporal/efectos de los fármacos , Pruebas de Carcinogenicidad , Modelos Animales de Enfermedad , Colorantes de Alimentos , Hígado/anatomía & histología , Hígado/efectos de los fármacos , Neoplasias Hepáticas/inducido químicamente , Masculino , Tamaño de los Órganos/efectos de los fármacos , Ratas , Ratas Endogámicas F344RESUMEN
Anthocyanins, which are used as a food coloring, are widely distributed in human diets, suggesting that we ingest large amounts of anthocyanins from plant-based foods. Mice were fed control, cyanidin 3-glucoside-rich purple corn color (PCC), high fat (HF) or HF + PCC diet for 12 wk. Dietary PCC significantly suppressed the HF diet-induced increase in body weight gain, and white and brown adipose tissue weights. Feeding the HF diet markedly induced hypertrophy of the adipocytes in the epididymal white adipose tissue compared with the control group. In contrast, the induction did not occur in the HF + PCC group. The HF diet induced hyperglycemia, hyperinsulinemia and hyperleptinemia. These perturbations were completely normalized in rats fed HF + PCC. An increase in the tumor necrosis factor (TNF)-alpha mRNA level occurred in the HF group and was normalized by dietary PCC. These results suggest that dietary PCC may ameliorate HF diet-induced insulin resistance in mice. PCC suppressed the mRNA levels of enzymes involved in fatty acid and triacylglycerol synthesis and lowered the sterol regulatory element binding protein-1 mRNA level in white adipose tissue. These down-regulations may contribute to triacylglycerol accumulation in white adipose tissue. Our findings provide a biochemical and nutritional basis for the use of PCC or anthocyanins as a functional food factor that may have benefits for the prevention of obesity and diabetes.
Asunto(s)
Antocianinas/administración & dosificación , Dieta , Glucósidos/administración & dosificación , Hiperglucemia/tratamiento farmacológico , Obesidad/prevención & control , Factores de Transcripción , Tejido Adiposo , Animales , Antocianinas/uso terapéutico , Secuencia de Bases , Peso Corporal , Proteínas Potenciadoras de Unión a CCAAT/genética , Cartilla de ADN , Proteínas de Unión al ADN/genética , Ingestión de Energía , Glucósidos/uso terapéutico , Resistencia a la Insulina , Lípidos/biosíntesis , Lípidos/sangre , Hígado/enzimología , Hígado/metabolismo , Masculino , Ratones , Ratones Endogámicos BALB C , Tamaño de los Órganos , Proteína 1 de Unión a los Elementos Reguladores de EsterolesRESUMEN
This study was designed to evaluate and characterize any subacute toxicity of 1-carboxy-5,7-dibromo-6-hydroxy-2,3,4-trichloroxanthone (HXCA), an impurity of Phloxine B (Food Red No. 104 in Japan, D&C Red No. 28 in the USA), when administered to both sexes of F344 rats at dietary levels of 0 (control), 0.005, 0.05 and 0.5%. During the study, the treatment had no effects on clinical signs, survival, urinalysis or ophthalmology. Hematology, blood biochemistry, gross pathology, organ weights, organ to body weight ratios and histopathology exhibited no differences of toxicological significance between control and treated rats. Reactions to treatment may be summarized as follows: there was a tendency for increased food and water consumption and decreased food efficiency in both sexes of the 0.5% group. Thus, these results indicated the no-observed-adverse-effect level (NOAEL) of HXCA to be 0.05% (39.3 mg/kg/day for males, and 41.0 mg/kg/day for females).
Asunto(s)
Eosina I Azulada/toxicidad , Colorantes de Alimentos/toxicidad , Xantonas/toxicidad , Animales , Seguridad de Productos para el Consumidor , Dieta , Relación Dosis-Respuesta a Droga , Ingestión de Líquidos/efectos de los fármacos , Contaminación de Medicamentos , Ingestión de Alimentos/efectos de los fármacos , Eosina I Azulada/química , Femenino , Concentración de Iones de Hidrógeno , Masculino , Nivel sin Efectos Adversos Observados , Ratas , Ratas Endogámicas F344 , Factores de Tiempo , Pruebas de Toxicidad , Orina/química , Xantonas/química , Xantonas/metabolismoRESUMEN
Acid-stable carmine has recently been distributed in the U.S. market because of its good acid stability, but it is not permitted in Japan. We analyzed and determined the structure of the major pigment in acid-stable carmine, in order to establish an analytical method for it. Carminic acid was transformed into a different type of pigment, named acid-stable carmine, through amination when heated in ammonia solution. The features of the structure were clarified using a model compound, purpurin, in which the orientation of hydroxyl groups on the A ring of the anthraquinone skeleton is the same as that of carminic acid. By spectroscopic means and the synthesis of acid-stable carmine and purpurin derivatives, the structure of the major pigment in acid-stable carmine was established as 4-aminocarminic acid, a novel compound.
Asunto(s)
Antraquinonas , Carmín/química , Colorantes de Alimentos/química , Ácidos , Cromatografía Líquida de Alta Presión , Estabilidad de Medicamentos , Lectinas/química , Metilación , Análisis EspectralRESUMEN
The potential of purple sweet potato color (PSPC) and red cabbage color (RCC), natural anthocyanin food colors, to modify colorectal carcinogenesis was investigated in male F344/DuCrj rats, initially treated with 1,2-dimethylhydrazine (DMH) and receiving 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in the diet. After DMH initiation, PSPC and RCC were given at a dietary level of 5.0% in combination with 0.02% PhIP until week 36. No PSPC or RCC-treatment-related changes in clinical signs and body weight were found. Incidences and multiplicities of colorectal adenomas and carcinomas in rats initiated with DMH were clearly increased by PhIP. In contrast, lesion development was suppressed by RCC, or tended to be inhibited by PSPC administration. Furthermore, in the non-DMH initiation groups, induction of aberrant crypt foci (ACF) by PhIP was significantly decreased by RCC supplementation. The results thus demonstrate that while PhIP clearly exerts promoting effects on DMH-induced colorectal carcinogenesis, these can be reduced by 5.0% PSPC or 5.0% RCC in a diet under the present experimental conditions.
Asunto(s)
Adenoma/prevención & control , Antocianinas/uso terapéutico , Anticarcinógenos/uso terapéutico , Brassica/química , Carcinoma/prevención & control , Neoplasias Colorrectales/prevención & control , Ipomoea batatas/química , Preparaciones de Plantas/uso terapéutico , 1,2-Dimetilhidrazina/toxicidad , Adenoma/inducido químicamente , Adenoma/patología , Administración Oral , Animales , Antocianinas/administración & dosificación , Anticarcinógenos/administración & dosificación , Carcinógenos/toxicidad , Carcinoma/inducido químicamente , Carcinoma/patología , Cocarcinogénesis , Colon/efectos de los fármacos , Colon/patología , Neoplasias Colorrectales/inducido químicamente , Neoplasias Colorrectales/patología , Dieta , Hiperplasia/inducido químicamente , Hiperplasia/patología , Imidazoles/toxicidad , Mucosa Intestinal/efectos de los fármacos , Mucosa Intestinal/patología , Masculino , Preparaciones de Plantas/administración & dosificación , Lesiones Precancerosas/inducido químicamente , Lesiones Precancerosas/patología , Lesiones Precancerosas/prevención & control , Ratas , Ratas Endogámicas F344RESUMEN
The carotenoids in Gac fruit (Momordica Cochinchinensis spreng) were analysed by high-performance liquid chromatography (HPLC), and the concentrations of beta-carotene, lycopene, zeaxanthin and beta-cryptoxanthin were measured. Lycopene was found to be predominantly present in the Gac seed membrane at a concentration of up to 380 microg/g of seed membrane. The concentration of lycopene in the Gac seed membrane was about ten-fold higher than that in known lycopene-rich fruit and vegetables, indicating that Gac fruit could be a new and potentially valuable source of lycopene.