RefDoc
Haut

Faire une nouvelle recherche
Make a new search
Lancer la recherche


Titre du document / Document title

In vitro studies indicate that miquelianin (Quercetin 3-o-β-d-glucuronopyranoside) is able to reach the CNS from the small intestine

Auteur(s) / Author(s)

JUERGENLIEMK Guido (1) ; BOJE Kerstin (1) ; HUEWEI Sabine (2) ; LOHMANN Christina (2) ; GALLA Hans-Joachim (2) ; NAHRSTEDT Adolf (1) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) Institute of Pharmaceutical Biology and Phytochemistry, Westf. Wilhelms-University, Muenster, ALLEMAGNE
(2) Institute of Biochemistry, Westf. Wilhelms-University, Muenster, ALLEMAGNE

Résumé / Abstract

Miquelianin (quercetin 3-O-β-D-glucuronopyranoside) is one of the flavonoids of St. John's wort (Hypericum perforatum L.) whose antidepressant activity has been shown by the forced swimming test, an in vivo pharmacological model with rats. However, nothing is known about its ability to reach the CNS after oral administration. We examined the pathway of miquelianin from the small intestine to the central nervous system using three in vitro membrane barrier cell systems. In the Caco-2 cell line, miquelianin showed a higher uptake (1.93 ± 0.9 pmol × min-1 x cm-2) than hyperoside (quercetin 3-O-β-D-galactopyranoside; 0.55 ± 0.18 pmol × min-1 × cm-2) and quercitrin (quercetin 3-O-α-L-rhamnopyranoside; 0.22 ± 0.08 pmol × min-1 × cm-2). The permeability coefficient of miquelianin (Pc = 0.4 ± 0.19 × 10-6cm/ sec) was in the range of orally available drugs assuming sufficient absorption from the small intestine. Uptake and permeability of the examined compounds was increased by the MRP-2 inhibitor MK-571 indicating a backwards transport by this membrane protein. Porcine cell cultures of brain capillary endothelial cells were used as a model of the blood-brain barrier (bbb) and epithelial cells of the plexus chorioidei as a model of the blood-CSF barrier (bcb). Results indicate no active transport in one direction. Although moderate, the permeability coefficients (bbb: Pc = 1.34 ± 0.05 × 10-6cm/sec; bcb: Pc = 2.0 ± 0.33×10-6cm/ sec) indicate the ability of miquelianin to cross both barriers to finally reach the CNS.

Revue / Journal Title

Planta medica    ISSN  0032-0943   CODEN PLMEAA 

Source / Source

2003, vol. 69, no11, pp. 1013-1017 [5 page(s) (article)] (22 ref.)

Langue / Language

Anglais

Editeur / Publisher

Thieme, Stuttgart, ALLEMAGNE  (1953) (Revue)

Mots-clés anglais / English Keywords

Vertebrata

;

Mammalia

;

Ungulata

;

Artiodactyla

;

Spermatophyta

;

Angiospermae

;

Dicotyledones

;

Guttiferae

;

Pig

;

Human

;

Blood capillary

;

Cell culture

;

Animal

;

Gut

;

Established cell line

;

Pharmacognosy

;

Plant origin

;

Medicinal plant

;

In vitro

;

Encephalon

;

Central nervous system

;

Distribution

;

Bioavailability

;

Pharmacokinetics

;

Permeability

;

Transport

;

Absorption

;

Blood brain barrier

;

Flavonoid

;

Choroid plexus

;

Endothelial cell

;

Hypericum perforatum

;

Mots-clés français / French Keywords

Vertebrata

;

Mammalia

;

Ungulata

;

Artiodactyla

;

Spermatophyta

;

Angiospermae

;

Dicotyledones

;

Guttiferae

;

Lignée CACO2

;

Porc

;

Homme

;

Capillaire sanguin

;

Culture cellulaire

;

Animal

;

Intestin

;

Lignée cellulaire établie

;

Pharmacognosie

;

Origine végétale

;

Plante médicinale

;

In vitro

;

Encéphale

;

Système nerveux central

;

Distribution

;

Biodisponibilité

;

Pharmacocinétique

;

Perméabilité

;

Transport

;

Absorption

;

Barrière hématoencéphalique

;

Flavonoïde

;

Plexus choroïde

;

Cellule endothéliale

;

Hypericum perforatum

;

Mots-clés espagnols / Spanish Keywords

Vertebrata

;

Mammalia

;

Ungulata

;

Artiodactyla

;

Spermatophyta

;

Angiospermae

;

Dicotyledones

;

Guttiferae

;

Cerdo

;

Hombre

;

Capilar sanguíneo

;

Cultivo celular

;

Animal

;

Intestino

;

Línea celular establecida

;

Farmacognosia

;

Origen vegetal

;

Planta medicinal

;

In vitro

;

Encéfalo

;

Sistema nervioso central

;

Distribución

;

Biodisponibilidad

;

Farmacocinética

;

Permeabilidad

;

Transporte

;

Absorción

;

Barrera hematoencefálica

;

Flavonoide

;

Plexo coroideo

;

Célula endotelial

;

Hypericum perforatum

;

Mots-clés d'auteur / Author Keywords

Caco-2 cells

;

blood-brain barrier blood-CSF barrier ·flavonol glycosides

;

miquelianin

;

St. John's wort

;

Hypericum perforatum

;

Clusiaceae

;

Localisation / Location

INIST-CNRS, Cote INIST : 9624, 35400011615367.0090

Nº notice refdoc (ud4) : 15349178



Faire une nouvelle recherche
Make a new search
Lancer la recherche
Bas