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KMID : 0043320030260121102
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Archives of Pharmacal Research
2003 Volume.26 No. 12 p.1102 ~ p.1108
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Enhancement of Heparin and Heparin Disaccharide Absorption by the Phytolacca americana Saponins
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Cho So-Yean
Sim Joon-Soo
Kang Sam-Sik
Jeong Choon-Sik
Linhardt Robert-J
Kim Yeong-Shik
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Abstract
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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, , 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,, 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.
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KEYWORD
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Phytolaccosides, Heparin, Heparin disaccharide, Caco-2 cells, Absorption enhancer
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