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新型功能性可生物降解聚合物:聚(γ-谷氨酸)磺酸盐(γ-PGA-磺酸盐)的合成与抗凝血活性

Novel functional biodegradable polymer: synthesis and anticoagulant activity of poly(gamma-glutamic acid)sulfonate (gamma-PGA-sulfonate).

作者信息

Matsusaki Michiya, Serizawa Takeshi, Kishida Akio, Endo Takeshi, Akashi Mitsuru

机构信息

Department of Applied Chemistry and Chemical Engineering, Faculty of Engineering, Kagoshima University, I-21-40 Korimoto, Kagoshima 890-0065, Japan.

出版信息

Bioconjug Chem. 2002 Jan-Feb;13(1):23-8. doi: 10.1021/bc010008d.

DOI:10.1021/bc010008d
PMID:11792175
Abstract

gamma-Poly(glutamic acid) (gamma-PGA), which is produced by Bacillus subtilis, was sulfonated using 2-aminoethane-1-sulfonic acid (taurine) in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (WSC) to give sulfonated gamma-PGA (gamma-PGA-sulfonate). From (1)H NMR spectroscopy and IR spectroscopy, it was confirmed that taurine was introduced to the side chain of gamma-PGA via an amide linkage. By altering the synthetic conditions, it was possible to control the content of sulfonate in gamma-PGA-sulfonate. Anticoagulant activity was investigated in order to evaluate the biological activity of gamma-PGA-sulfonate by the Lee-White test. The clotting time was prolonged when the concentration of gamma-PGA-sulfonate on the degree of sulfonation was increased. It becomes clear that gamma-PGA-sulfonate is potentially useful for various medical applications, such as drug delivery, tissue engineering, and medical materials.

摘要

γ-聚谷氨酸(γ-PGA)由枯草芽孢杆菌产生,在1-乙基-3-(3-二甲基氨基丙基)碳二亚胺(WSC)存在下,使用2-氨基乙烷-1-磺酸(牛磺酸)对其进行磺化,得到磺化γ-聚谷氨酸(γ-PGA-磺酸盐)。通过核磁共振氢谱(¹H NMR)和红外光谱(IR)证实,牛磺酸通过酰胺键引入到γ-聚谷氨酸的侧链上。通过改变合成条件,可以控制γ-PGA-磺酸盐中磺酸盐的含量。为了通过Lee-White试验评估γ-PGA-磺酸盐的生物活性,对其抗凝活性进行了研究。当γ-PGA-磺酸盐浓度和磺化程度增加时,凝血时间延长。γ-PGA-磺酸盐在药物递送、组织工程和医疗材料等各种医学应用中具有潜在用途,这一点变得清晰起来。

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