Polymer-phloridzin conjugates as an anti-diabetic drug that Inhibits glucose absorption through the Na(+)/glucose cotransporter (SGLT1) in the small intestine.

Polymer-phloridzin conjugates as an anti-diabetic drug that Inhibits glucose absorption through the Na(+)/glucose cotransporter (SGLT1) in the small intestine. Research Abstract Details 

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Polymer-phloridzin conjugates as an anti-diabetic drug that Inhibits glucose absorption through the Na(+)/glucose cotransporter (SGLT1) in the small intestine. Abstract Text:

Yusuke Ikumi,Toshiyuki Kida,Shinji Sakuma,Shinji Yamashita,Mitsuru Akashi,Yusuke Ikumi,Toshiyuki Kida,Shinji Sakuma,Shinji Yamashita,Mitsuru Akashi,Yusuke Ikumi,Toshiyuki Kida,Shinji Sakuma,Shinji Yamashita,Mitsuru Akashi,

Poly(gamma-glutamic acid)s (gamma-PGA) modified with phloridzin, which is an inhibitor of the Na(+)/glucose cotransporter (SGLT1), via a omega-amino triethylene glycol linker were synthesized. The potential of gamma-PGA-phloridzin conjugates (PGA-PRZs) obtained as a novel oral anti-diabetic drug was examined by in vitro and in vivo experiments. A PGA-PRZ with a 15% phloridzin content inhibited glucose transport from mucosal to serosal sides of the everted rat's small intestine, and its inhibitory effect was as strong as that of intact phloridzin. When the PGA-PRZ was given orally to rats before glucose administration, the glucose-induced hyperglycemic effect was significantly suppressed. On the other hand, reduction of an increase in the blood glucose concentration was scarcely observed when the PGA-PRZ was substituted with a double amount of intact phloridzin. This difference in the biological activity between PGA-PRZ and intact phloridzin might have resulted from the improved stability of a glucoside bond of phloridzin through the conjugation with gamma-PGA. These results suggest that the gamma-PGA-phloridzin conjugates have potential as oral anti-diabetic drugs.

Polymer-phloridzin conjugates as an anti-diabetic drug that Inhibits glucose absorption through the Na(+)/glucose cotransporter (SGLT1) in the small intestine. Publishing Authors By Initials

Y Ikumi,T Kida,S Sakuma,S Yamashita,M Akashi,Y Ikumi,T Kida,S Sakuma,S Yamashita,M Akashi,Y Ikumi,T Kida,S Sakuma,S Yamashita,M Akashi,

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Polymer-phloridzin conjugates as an anti-diabetic drug that Inhibits glucose absorption through the Na(+)/glucose cotransporter (SGLT1) in the small intestine. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Journal of controlled release : official journal o

VOLUME: 125

Page Numbers: 42-9

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ISSN: 1873-4995

DAY: 13

MONTH: 10

YEAR: 2007

Polymer-phloridzin conjugates as an anti-diabetic drug that Inhibits glucose absorption through the Na(+)/glucose cotransporter (SGLT1) in the small intestine. Information

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LANGUAGE: eng

NlmUniqueID: 8607908

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Grant and Affiliation Information for Polymer-phloridzin conjugates as an anti-diabetic drug that Inhibits glucose absorption through the Na(+)/glucose cotransporter (SGLT1) in the small intestine.

AFFILIATION: Department of Applied Chemistry, Graduate School of Engineering, Osaka University, 2-1 Yamadaoka, Suita, Osaka 565-0871, Japan.

Country: Netherlands

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MEDLINETA: J Control Release

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