In VitroStudies Indicate that Miquelianin (Quercetin 3-O-ß-D -Glucuronopyranoside) is Able to Reach the CNS from the Small Intestine
| Autor: | Adolf Nahrstedt, Guido Juergenliemk, Hans-Joachim Galla, Christina Lohmann, Kerstin Boje, Sabine Huewel |
|---|---|
| Rok vydání: | 2003 |
| Předmět: |
Swine
Administration Oral Biological Availability Pharmaceutical Science Hyperoside Biology Blood–brain barrier Analytical Chemistry chemistry.chemical_compound Glucosides In vivo Drug Discovery medicine Animals Humans Intestinal Mucosa Miquelianin Cells Cultured Pharmacology Organic Chemistry Brain Quercitrin Molecular biology Multidrug Resistance-Associated Protein 2 Small intestine medicine.anatomical_structure Intestinal Absorption Complementary and alternative medicine chemistry Biochemistry Blood-Brain Barrier Caco-2 Molecular Medicine Quercetin Plant Preparations Caco-2 Cells Hypericum Phytotherapy |
| Zdroj: | Planta Medica. 69:1013-1017 |
| ISSN: | 1439-0221 0032-0943 |
| DOI: | 10.1055/s-2003-45148 |
| Popis: | Miquelianin (quercetin 3-O-beta-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 x min(-1) x cm(-2)) than hyperoside (quercetin 3-O-beta-D-galactopyranoside; 0.55 +/- 0.18 pmol x min(-1) x cm(-2)) and quercitrin (quercetin 3-O-alpha-L-rhamnopyranoside; 0.22 +/- 0.08 pmol x min(-1) x cm(-2)). The permeability coefficient of miquelianin (Pc = 0.4 +/- 0.19 x 10(-6) cm/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 x 10(-6) cm/sec; bcb: Pc = 2.0 +/- 0.33 x 10(-6) cm/sec) indicate the ability of miquelianin to cross both barriers to finally reach the CNS. |
| Databáze: | OpenAIRE |
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