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Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats

Fucus vesiculosus L., known as bladderwrack, belongs to the brown seaweeds, which are widely distributed throughout northern Russia, Atlantic shores of Europe, the Baltic Sea, Greenland, the Azores, the Canary Islands, and shores of the Pacific Ocean. Fucoidan is a major fucose-rich sulfated polysac...

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Autores principales: Pozharitskaya, Olga N., Shikov, Alexander N., Faustova, Natalya M., Obluchinskaya, Ekaterina D., Kosman, Vera M., Vuorela, Heikki, Makarov, Valery G.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5923419/
https://www.ncbi.nlm.nih.gov/pubmed/29669995
http://dx.doi.org/10.3390/md16040132
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author Pozharitskaya, Olga N.
Shikov, Alexander N.
Faustova, Natalya M.
Obluchinskaya, Ekaterina D.
Kosman, Vera M.
Vuorela, Heikki
Makarov, Valery G.
author_facet Pozharitskaya, Olga N.
Shikov, Alexander N.
Faustova, Natalya M.
Obluchinskaya, Ekaterina D.
Kosman, Vera M.
Vuorela, Heikki
Makarov, Valery G.
author_sort Pozharitskaya, Olga N.
collection PubMed
description Fucus vesiculosus L., known as bladderwrack, belongs to the brown seaweeds, which are widely distributed throughout northern Russia, Atlantic shores of Europe, the Baltic Sea, Greenland, the Azores, the Canary Islands, and shores of the Pacific Ocean. Fucoidan is a major fucose-rich sulfated polysaccharide found in Fucus (F.) vesiculosus. The pharmacokinetic profiling of active compounds is essential for drug development and approval. The aim of the study was to evaluate the pharmacokinetics and tissue distribution of fucoidan in rats after a single-dose oral administration. Fucoidan was isolated from F. vesiculosus. The method of measuring anti-activated factor X (anti-Xa) activity by amidolytic assay was used to analyze the plasma and tissue concentrations of fucoidan. The tissue distribution of fucoidan after intragastric administration to the rats was characterized, and it exhibited considerable heterogeneity. Fucoidan preferentially accumulates in the kidneys (AUC(0–t) = 10.74 µg·h/g; C(max) = 1.23 µg/g after 5 h), spleen (AUC(0–t) = 6.89 µg·h/g; C(max) = 0.78 µg/g after 3 h), and liver (AUC(0–t) = 3.26 µg·h/g; C(max) = 0.53 µg/g after 2 h) and shows a relatively long absorption time and extended circulation in the blood, with a mean residence time (MRT) = 6.79 h. The outcome of this study provides additional scientific data for traditional use of fucoidan-containing plants and offers tangible support for the continued development of new effective pharmaceuticals using fucoidan.
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spelling pubmed-59234192018-05-03 Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats Pozharitskaya, Olga N. Shikov, Alexander N. Faustova, Natalya M. Obluchinskaya, Ekaterina D. Kosman, Vera M. Vuorela, Heikki Makarov, Valery G. Mar Drugs Article Fucus vesiculosus L., known as bladderwrack, belongs to the brown seaweeds, which are widely distributed throughout northern Russia, Atlantic shores of Europe, the Baltic Sea, Greenland, the Azores, the Canary Islands, and shores of the Pacific Ocean. Fucoidan is a major fucose-rich sulfated polysaccharide found in Fucus (F.) vesiculosus. The pharmacokinetic profiling of active compounds is essential for drug development and approval. The aim of the study was to evaluate the pharmacokinetics and tissue distribution of fucoidan in rats after a single-dose oral administration. Fucoidan was isolated from F. vesiculosus. The method of measuring anti-activated factor X (anti-Xa) activity by amidolytic assay was used to analyze the plasma and tissue concentrations of fucoidan. The tissue distribution of fucoidan after intragastric administration to the rats was characterized, and it exhibited considerable heterogeneity. Fucoidan preferentially accumulates in the kidneys (AUC(0–t) = 10.74 µg·h/g; C(max) = 1.23 µg/g after 5 h), spleen (AUC(0–t) = 6.89 µg·h/g; C(max) = 0.78 µg/g after 3 h), and liver (AUC(0–t) = 3.26 µg·h/g; C(max) = 0.53 µg/g after 2 h) and shows a relatively long absorption time and extended circulation in the blood, with a mean residence time (MRT) = 6.79 h. The outcome of this study provides additional scientific data for traditional use of fucoidan-containing plants and offers tangible support for the continued development of new effective pharmaceuticals using fucoidan. MDPI 2018-04-18 /pmc/articles/PMC5923419/ /pubmed/29669995 http://dx.doi.org/10.3390/md16040132 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Pozharitskaya, Olga N.
Shikov, Alexander N.
Faustova, Natalya M.
Obluchinskaya, Ekaterina D.
Kosman, Vera M.
Vuorela, Heikki
Makarov, Valery G.
Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats
title Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats
title_full Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats
title_fullStr Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats
title_full_unstemmed Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats
title_short Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats
title_sort pharmacokinetic and tissue distribution of fucoidan from fucus vesiculosus after oral administration to rats
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5923419/
https://www.ncbi.nlm.nih.gov/pubmed/29669995
http://dx.doi.org/10.3390/md16040132
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