RESUMEN
The methanolic extract of the roots of Polygonum multiflorum (Polygonaceae) was found to show inhibitory activity towards farnesyl protein transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two anthraquinone glycosides, as inhibitors of FPTase. These compounds inhibited the FPTase activity in a dose-dependent manner.
Asunto(s)
Transferasas Alquil y Aril/antagonistas & inhibidores , Antraquinonas/farmacología , Inhibidores Enzimáticos/farmacología , Glicósidos/farmacología , Polygonum , Antraquinonas/química , Antraquinonas/aislamiento & purificación , Bioensayo , Fraccionamiento Químico , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Glicósidos/química , Glicósidos/aislamiento & purificación , Metanol/química , Estructura Molecular , Raíces de Plantas , Polygonum/química , Solventes/químicaRESUMEN
We have isolated a new prenylated chalcone from the roots of Sophora flavescens (Leguminosae). We determined that structure of this compound is 7,9,2',4'-tetrahydroxy-8-isopentenyl-5-methoxychalcone (1) on the basis of spectroscopic analysis (1D and 2D NMR data). Compound 1 exhibited potent cytotoxicity against human acute promyelocytic (HL60), mouse lymphocytic (L1210) and human histiocytic (U937) leukemia cells.
Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Chalconas/aislamiento & purificación , Sophora/química , Animales , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Chalconas/química , Chalconas/farmacología , Humanos , Espectroscopía de Resonancia Magnética , Ratones , Prenilación de ProteínaRESUMEN
Three known isoquinoline alkaloids were isolated from the chloroform-soluble fraction of the methanolic extract of the aerial parts of Corydalis incisa (Papaveraceae) through repeated column chromatography. Their chemical structures were elucidated as corynoline (1), corynoloxine (2) and 6-oxocorynoline (3) using spectroscopic analysis. Compounds 1-3 exhibited cytotoxicity against human A549, SK-OV-3, SK-MEL-2 and HCT15 tumor cells.
Asunto(s)
Alcaloides/farmacología , Antineoplásicos Fitogénicos/farmacología , Corydalis/química , Isoquinolinas/farmacología , Alcaloides/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Adhesión Celular/efectos de los fármacos , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Isoquinolinas/aislamiento & purificación , Estructura Molecular , Neutrófilos/citología , Componentes Aéreos de las Plantas/química , Relación Estructura-ActividadRESUMEN
Eight compounds were isolated from the methanolic extract of the twigs of Celtis sinensis through repeated silica gel and Sephadex LH-20 column chromatography. Their chemical structures were elucidated as two triterpenoids, germanicol and epifriedelanol, two amide compounds, trans-N-caffeoyltyramine and cis-N-coumaroyltyramine, two lignan glycoside, pinoresinol glycoside and pinoresinol rutinoside, and two steroids by spectroscopic analysis.
Asunto(s)
Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/aislamiento & purificación , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Ulmaceae , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Tallos de la PlantaRESUMEN
The methanolic extract of the aerial parts of Persicaria thunbergii was found to show inhibitory activity on Farnesyl Protein Transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of isorhamnetin, as an inhibitor on FPTase. This compound inhibited FPTase activity in a dose-dependent manner, and the IC50 value of isorhamnetin was 37.5 microM.
Asunto(s)
Transferasas Alquil y Aril/antagonistas & inhibidores , Inhibidores Enzimáticos/farmacología , Flavonoles/farmacología , Polygonaceae/química , Cromatografía en Capa Delgada , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/aislamiento & purificación , Farnesiltransferasa , Flavonoles/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Extractos Vegetales/farmacología , Quercetina/análogos & derivadosRESUMEN
All ten compounds were isolated from the methanolic extract of the whole plants of Diodia teres through repeated silica gel and Sephadex LH-20 column chromatography. Their chemical structures were elucidated as three iridoid glycosides, asperuloside, geniposidic acid and asperulosidic acid, a coumarin glycoside, scopolin, and six flavonoids, rutin, kaempferol-3-O-rutinoside, quercitrin, astragalin, isoquercitrin and quercetin by spectroscopic analysis.
Asunto(s)
Estructuras de las Plantas/química , Plantas Medicinales/química , Rubiaceae/química , Química Farmacéutica/métodos , Cromatografía Liquida/métodos , Cumarinas/química , Cumarinas/aislamiento & purificación , Flavonoides/química , Flavonoides/aislamiento & purificación , Glucósidos/química , Glucósidos/aislamiento & purificación , Glicósidos/química , Glicósidos/aislamiento & purificación , Glucósidos Iridoides , Iridoides/química , Iridoides/aislamiento & purificación , Quempferoles/química , Quempferoles/aislamiento & purificación , Metanol/química , Extractos Vegetales/químicaRESUMEN
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
A new (3) and three known germacrane-type sesquiterpenoids were isolated from the chloroform-soluble fraction of the methanolic extract of the bark of Magnolia kobus (Magnoliaceae) through repeated silica gel and Sephadex LH-20 column chromatography. Their chemical structures were elucidated as costunolide (1), parthenolide (2), isobisparthenolidine (3), and bisparthenolidine (4) by spectroscopic analysis. Compounds 1-4 exhibited cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells.