Anticoagulant supramolecular-structured polymers: Synthesis and anticoagulant activity of taurine-conjugated carboxyethylester-polyrotaxanes
Joung, Yoon Ki; Sengoku, Yoichi; Ooya, Tooru; Park, Ki Dong; Yui, Nobuhiko; Joung, Yoon Ki; School of Materials Science, Japan Advanced Institute of Science and Technology, 1-1 Asahidai, Tatsunokuchi, Ishikawa 923-1292, Japan; Sengoku, Yoichi; School of Materials Science, Japan Advanced Institute of Science and Technology, 1-1 Asahidai, Tatsunokuchi, Ishikawa 923-1292, Japan; Ooya, Tooru; School of Materials Science, Japan Advanced Institute of Science and Technology, 1-1 Asahidai, Tatsunokuchi, Ishikawa 923-1292, Japan; Park, Ki Dong; Department of Molecular Science and Technology, Ajou University, 5 Wonchon, Youngtong, Suwon 442-749, South Korea; Yui, Nobuhiko; School of Materials Science, Japan Advanced Institute of Science and Technology, 1-1 Asahidai, Tatsunokuchi, Ishikawa 923-1292, Japan;
Журнал:
Science and Technology of Advanced Materials
Дата:
2005-07-31
Аннотация:
Polyrotaxanes with both sulfonyl and carboxyl groups were synthesized and characterized for mimicking the anticoagulant activity of heparin. A polyrotaxane consisting of α-cyclodextrins (α-CDs) and poly(ethylene glycol) (PEG) was synthesized, and carboxyethylester (CEE) groups and taurine were successively conjugated with the polyrotaxane to obtain taurine-conjugated carboxyethylester-polyrotaxanes (TAU-CEE-PRxs). The number of α-CDs and the anionic groups could be varied by synthetic conditions. The structural factors of TAU-CEE-PRxs affecting anticoagulant activity were suggested as following: (i) relatively lower threading percentage of α-CDs, (ii) the ratio of anionic groups similar to heparin, and (iii) lower molecular weight of PEG. The TAU-CEE-PRx that sufficiently meet the mentioned requirements showed enhanced antithrombin III (AT III) activity, indicating that the TAU-CEE-PRx interacts with AT III and/or thrombin. From these results, it is suggested that the sliding and rotation of free α-CDs with anionic groups are related with enhancing anticoagulant activity.
142.4Кб