Effect of oligofucose derivatives on acetic acid-induced gastric ulcer in rats.
This study attempted to enhance the anti-ulcer activity of fucoidan from Cladosiphon okamuranus TOKIDA by chemical modification with a hydrophobic group. The suitable number of fucose residues in the effective compound was also clarified to obtain a compound of constant quality. Degraded fucoidans were coupled with several hydrophobic groups via Schiff bases, and their anti-ulcer activities were determined by acetic acid-induced ulcer models in rats. Size-fractionated oligofucose was also modified and assayed for anti-ulcer activity. Among the modified oligofucoses, only the oligofucose-dodecylaniline combination (OFDA) significantly promoted ulcer healing. The effective dose was 0.2 mg/kg/d. The most suitable number of fucose residues in the compound for the anti-ulcer activity was determined to be around 12. We succeeded in enhancing the anti-ulcer activity of Cladosiphon fucoidan by modification with dodecylaniline. The activity of this compound was comparable or greater than that of typical anti-ulcer agents. By determination of the optimal OF chain length for the anti-ulcer activity of OFDA, it became possible to obtain OFDA of constant quality.
Yakult Central Institute for Microbiological Research, Kunitachi, Tokyo, Japan. hideyuki-shibata@yakult.co.jp
H
H
Shibata
M
M
Nagaoka
I K
IK
Takagi
S
S
Hashimoto
R
R
Aiyama
T
T
Yokokura
D019342:Acetic Acid; D000818:Animals; D000897:Anti-Ulcer Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D004195:Disease Models, Animal; D004353:Drug Evaluation, Preclinical; D008297:Male; D008970:Molecular Weight; D011134:Polysaccharides / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012624:Seaweed / Q000737:chemistry; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy*
D000897:Anti-Ulcer Agents; D011134:Polysaccharides; C007789:fucoidan; D019342:Acetic Acid