RESUMEN
BACKGROUND: Allium hookeri is widely consumed as a vegetable and herbal medicine in Asia. A. hookeri has been reported anti-inflammatory, anti-obesity, osteoblastic, anti-oxidant, and anti-diabetic effects in animal studies. We investigated the anti-diabetic effects of A. hookeri aqueous extract (AHE) in the Korean subjects. METHODS: Prediabetic subjects (100 ≤ fasting plasma glucose (FPG) < 126 mg/dL) who met the inclusion criteria were recruited for this study. The enrolled subjects (n = 30) were randomly divided into either an AHE (n = 15, 486 mg/day) or placebo (n = 15) group. Outcomes were measurements of FPG, glycemic response to an oral glucose tolerance test (OGTT), insulin, C-peptide, hemoglobin A1c (HbA1c), total cholesterol, triglyceride, HDL-cholesterol, and LDL-cholesterol. The t-test was used to assess differences between the groups. A p-value < 0.05 was considered statistically significant. RESULTS: Eight weeks after AHE supplementation, HbA1c level was significantly decreased in the AHE group compared with the placebo group. No clinically significant changes in any safety parameter were observed. CONCLUSION: The findings suggest that AHE can be effective in reducing HbA1c, indicating it as an adjunctive tool for improving glycemic control. TRIAL REGISTRATION: The study protocol was retrospectively registered at www.clinicaltrials.gov ( NCT03330366 , October 30, 2017).
Asunto(s)
Allium , Glucemia/efectos de los fármacos , Hemoglobina Glucada/metabolismo , Extractos Vegetales/uso terapéutico , Estado Prediabético/tratamiento farmacológico , Adulto , Anciano , Biomarcadores/sangre , Péptido C/sangre , Estudios Cruzados , Método Doble Ciego , Femenino , Prueba de Tolerancia a la Glucosa , Humanos , Insulina/sangre , Masculino , Persona de Mediana Edad , República de CoreaRESUMEN
BACKGROUND: Water extract from the root of Allium hookeri (AH) shows anti-inflammatory, antioxidant, and free radical scavenging effects. In this study, the ameliorating effects of AH on oxidative stress-induced inflammatory response and ß-cell damage in the pancreas of streptozotocin (STZ)-induced type 1 diabetic rats were investigated. METHODS: AH (100 mg/kg body weight/day) was orally administered every day for 2 weeks to STZ-induced diabetic rats. After the final administration of AH, biochemical parameters including glucose, insulin, reactive oxygen species levels, and protein expressions related to antioxidant defense system in the pancreas of STZ-induced diabetic rats. RESULTS: The diabetic rats showed loss of body weight and increased pancreatic weight, while the oral administration of AH attenuated body and pancreatic weight changes. Moreover, the administration of AH caused a slightly decrease in the serum glucose level and a significant increase in the serum and pancreatic insulin levels in the diabetic rats. AH also significantly reduced the enhanced levels of reactive oxygen species, oxidative stress biomarker, in the serum and pancreas. The diabetic rats exhibited a down-regulation of the protein expression related to antioxidant defense system in the pancreas, but AH administration significantly up-regulated the expression of the heme oxygenase-1 (HO-1). Furthermore, AH treatment was reduced the overexpression of nuclear factor-kappa B (NF-кB)p65 and NF-кBp65-induced inflammatory cytokines such as tumor necrosis factor-α and interleukin-6. In addition, AH treatment was less pancreatic ß-cell damaged compared with those of the diabetic rats. CONCLUSION: These results provide important evidence that AH has a HO-1 activity on the oxidative stress conditions showing pancreato-protective effects against the development of inflammation in the diabetic rats. This study provides scientific evidence that AH protects the inflammatory responses by modulated NF-кBp65 signaling pathway through activation of HO-1 in the pancreas of STZ-induced diabetic rats.
Asunto(s)
Allium , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/uso terapéutico , Células Secretoras de Insulina/efectos de los fármacos , Extractos Vegetales/uso terapéutico , Raíces de Plantas , Allium/química , Animales , Peso Corporal , Diabetes Mellitus Experimental/patología , Ingestión de Alimentos , Mediadores de Inflamación/metabolismo , Insulina/sangre , Células Secretoras de Insulina/patología , Tamaño de los Órganos , Estrés Oxidativo/efectos de los fármacos , Páncreas/efectos de los fármacos , Raíces de Plantas/química , Sustancias Protectoras/uso terapéutico , Ratas , Especies Reactivas de Oxígeno/metabolismoRESUMEN
Three compounds were isolated from the ethyl acetate soluble fraction of the methanolic extract of the leaves of Catalpa ovata (Bignoniaceae) through repeated column chromatography. We investigated the effects of these compounds on T cell-mediated responses for tumor surveillance and proliferation in U937, HL60, and Molt-4 leukemia cells. Compounds 1-3 inhibited proliferation of those cells in a dose-dependent manner. Compound 3 showed mild effect in Molt-4 cell cytotoxicity. Compound 3 enhanced gene expressions of p53 and IL-4, but decreased IL-2 and IFN-Gamma genes in Molt-4 cell. Our findings indicate that compound 3 may enhance T cell-mediated immune responses and anticancer properties.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Bignoniaceae/química , Inmunidad Celular/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Linfocitos T/efectos de los fármacos , Antineoplásicos Fitogénicos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Apoptosis/genética , Apoptosis/inmunología , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Citocinas/biosíntesis , Citocinas/inmunología , Relación Dosis-Respuesta a Droga , Ensayo de Inmunoadsorción Enzimática , Expresión Génica/efectos de los fármacos , Células HeLa , Humanos , Inmunidad Celular/inmunología , Medicina Tradicional Coreana , Estructura Molecular , Hojas de la Planta/química , Reacción en Cadena de la Polimerasa de Transcriptasa Inversa , Linfocitos T/inmunología , Células U937RESUMEN
The methanolic extract of the aerial parts of Centipeda minima was found to show inhibitory activity on farnesyl protein transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of 6-O-angeloylprenolin, as an inhibitor on FPTase. This compound inhibited FPTase activity in a dose-dependent manner, and the IC50 value of 6-O-angeloylprenolin was 18.8 microM.
Asunto(s)
Asteraceae/química , Inhibidores Enzimáticos/aislamiento & purificación , Inhibidores Enzimáticos/farmacología , Farnesiltransferasa/antagonistas & inhibidores , Compuestos Heterocíclicos con 3 Anillos/química , Compuestos Heterocíclicos con 3 Anillos/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Cromatografía de Afinidad , Cromatografía Líquida de Alta Presión , Cromatografía en Capa Delgada , Compuestos Heterocíclicos con 3 Anillos/aislamiento & purificación , Lactonas , Espectroscopía de Resonancia Magnética , Metanol , Extractos Vegetales/aislamiento & purificación , Sesquiterpenos , SolventesRESUMEN
In a bioassay-guided search for acetylcholinesterase inhibitors from Korean natural resources, four isoquinoline alkaloids, corynoxidine (1), protopine (2), palmatine (3), and berberine (4) have been isolated from the methanolic extract of the aerial parts of Corydalis speciosa. Structures of these compounds were elucidated on the basis of spectroscopic techniques. These compounds inhibited acetylcholinesterase activity in a dose-dependent manner, and the IC50 values of compounds 1-4 were 89.0, 16.1, 5.8, and 3.3 microM, respectively.
Asunto(s)
Inhibidores de la Colinesterasa/aislamiento & purificación , Corydalis/química , Extractos Vegetales/aislamiento & purificación , Acetilcolinesterasa/metabolismo , Animales , Benzofenantridinas , Berberina/química , Berberina/farmacología , Alcaloides de Berberina/química , Alcaloides de Berberina/aislamiento & purificación , Alcaloides de Berberina/farmacología , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/farmacología , Relación Dosis-Respuesta a Droga , Cinética , Espectroscopía de Resonancia Magnética/métodos , Masculino , Ratones , Ratones Endogámicos ICR , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Tallos de la Planta/químicaRESUMEN
In the course of finding Korean natural products with acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the twigs of Vaccinium oldhami significantly inhibited AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two compounds, taraxerol (1) and scopoletin (2), as active constituents. These compounds inhibited AChE activity in a dose-dependent manner, and the IC50 values of compounds 1 and 2 were 33.6 (79 microM) and 10.0 (52 microM) microg/mL, respectively.
Asunto(s)
Inhibidores de la Colinesterasa/aislamiento & purificación , Inhibidores de la Colinesterasa/farmacología , Ácido Oleanólico/análogos & derivados , Tallos de la Planta/química , Vaccinium , Acetilcolina/aislamiento & purificación , Acetilcolina/metabolismo , Animales , Berberina/química , Berberina/farmacología , Bioensayo , Encéfalo/enzimología , Inhibidores de la Colinesterasa/química , Evaluación Preclínica de Medicamentos/métodos , Corea (Geográfico) , Masculino , Medicina Tradicional de Asia Oriental , Metanol/química , Ratones , Estructura Molecular , Ácido Oleanólico/química , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/farmacología , Fitoterapia , Extractos Vegetales/química , Plantas Medicinales , Escopoletina/química , Escopoletina/aislamiento & purificación , Escopoletina/farmacología , Tacrina/análogos & derivados , Tacrina/química , Tacrina/farmacologíaRESUMEN
In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dose-dependent manner, and the IC50 values of compounds 1-3 were 74.6, 63.7 and 89.1 microM, respectively.