Enhancement of heparin and heparin disaccharide absorption by the Phytolacca americana saponins

We studied the effects of phytolaccosides, saponins from Phytolacca americana, on the intestinal absorption of heparin in vitro and in vivo. The absorption enhancing activity of these compounds (phytolaccosides B, D2, E, F, G and I) was determined by changes in transepithelial electrical resistance...

Full description

Saved in:
Bibliographic Details
Published in:Archives of pharmacal research 2003-12, Vol.26 (12), p.1102
Main Authors: Cho, So Yean, Sim, Joon-Soo, Kang, Sam Sik, Jeong, Choon-Sik, Linhardt, Robert J, Kim, Yeong Shik
Format: Article
Language:English
Subjects:
Adjuvants, Pharmaceutic - pharmacokinetics
Adjuvants, Pharmaceutic - toxicity
Animals
Caco-2 Cells
Disaccharides - pharmacokinetics
Drug Synergism
Gastric Mucosa - drug effects
Gastric Mucosa - physiology
Heparin - analogs & derivatives
Heparin - pharmacokinetics
Humans
Intestinal Absorption - physiology
Male
Mice
Mice, Inbred ICR
Phytolacca americana
Plant Roots
Saponins - chemistry
Saponins - isolation & purification
Saponins - pharmacokinetics
Saponins - toxicity
Swine
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:We studied the effects of phytolaccosides, saponins from Phytolacca americana, on the intestinal absorption of heparin in vitro and in vivo. The absorption enhancing activity of these compounds (phytolaccosides B, D2, E, F, G and I) was determined by changes in transepithelial electrical resistance (TEER) and the transport amount of heparin disaccharide, the major repeating unit of heparin, across Caco-2 cell monolayers. With the exception of phytolaccoside G, all of them decreased TEER values and increased the permeability in a dose-dependent and time-dependent manner. In vitro, phytolaccosides B, D2, and E showed significant absorption enhancing activities, while effects by phytolaccoside F and I were mild. In vivo, phytolaccoside E increased the activated partial thromboplastin time (APTT) and thrombin time, indicating that phytolaccoside E modulated the transport of heparin in intestinal route. Our results suggest that a series of phytolaccosides from Phytolacca americana can be applied as pharmaceutical excipients to improve the permeability of macromolecules and hydrophilic drugs having difficulty in absorption across the intestinal epithelium.
ISSN:0253-6269
DOI:10.1007/BF02994765