Synthesis, enzymatic hydrolysis, and anti-HIV activity of AZT-spacer-curdlan sulfates

被引：23
作者：
Gao, Y
Katsuraya, K
Kaneko, Y
Mimura, T
Nakashima, H
Uryu, T
机构：
[1] Univ Tokyo, Inst Ind Sci, Minato Ku, Tokyo 1068558, Japan
[2] Kagoshima Univ, Sch Dent, Kagoshima 8908544, Japan
[3] Ajinomoto Co Inc, Chuo Ku, Tokyo 1040031, Japan
[4] Teikyo Univ Sci & Technol, Yamanashi 4090193, Japan
来源：
MACROMOLECULES | 1999年 / 32卷 / 25期
关键词：
D O I：
10.1021/ma990782k
中图分类号：
O63 [高分子化学（高聚物）];
学科分类号：
070305 ; 080501 ; 081704 ;
摘要：
An AIDS (acquired immunodeficiency syndrome) drug, azidothymidine (AZT), was bound by an ester bond onto curdlan sulfate having both anti-HIV activity and the property of accumulating in lymphoid tissues to produce a series of biodegradable AZT-aliphatic-dicarboxylate-curdlan sulfates (designated as AZT-spacer-curdlan sulfates). When the carbon number of the alkylene group was 2-12, AZT-spacer-curdlan sulfates exhibited high anti-HIV activities in the EC50 range of 0.04-0.21 mu g/mL and low cytotoxicities of CC50 of more than 1000 mu g/mL. AZT-dodecanedicarboxylate-curdlan sulfate with the highest anti-HIV activity was easily hydrolyzed by esterase-enzymatic hydrolysis to release free AZT. Furthermore, an acidically released AZT from curdlan sulfate exhibited its high anti-HIV activity. AZT-dodecanedicarboxylate-curdlan sulfate showed a low anticoagulant activity of 7 unit/mg.
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收藏
页码：8319 / 8324
页数：6
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