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不溶性磺化聚苯乙烯树脂的肝素样活性。第一部分:取代阴离子基团的表面密度、性质及结合的影响。

Heparin-like activity of insoluble sulphonated polystyrene resins. Part I: Influence of the surface density, nature and binding of substituted anionic groups.

作者信息

Kanmangne F M, Labarre D, Serne H, Jozefowicz M

出版信息

Biomaterials. 1985 Sep;6(5):297-302. doi: 10.1016/0142-9612(85)90085-7.

Abstract

It was previously demonstrated that copolystyrene (sulphonate-amino acid sulphamide) resins possessed an anticoagulant heparin-like activity in the presence of blood plasma. Taking into account the variable surfaces of swollen resins developed by these dry resins, it is now shown that the antithrombic activity of crosslinked sulphonated polystyrene is linearly dependent on the surface density of the sulphonate groups. This fact implies that the presence of such isolated groups is sufficient to obtain a catalytic site for increasing the rate of inactivation of thrombin by plasmatic proteins. It is also shown that replacing sulphonate groups either by directly backbone-bonded carboxylate groups or by methionine linked by amide bonds to polystyrene backbone is not sufficient to endow the resulting resins with a significant anticoagulant activity.

摘要

先前已证明,聚苯乙烯(磺酸盐 - 氨基酸磺酰胺)树脂在血浆存在下具有类似肝素的抗凝血活性。考虑到这些干燥树脂形成的溶胀树脂具有可变表面,现在表明交联磺化聚苯乙烯的抗血栓活性与磺酸根基团的表面密度呈线性相关。这一事实意味着这些孤立基团的存在足以获得一个催化位点,以提高血浆蛋白使凝血酶失活的速率。还表明,用直接与主链键合的羧酸盐基团或通过酰胺键与聚苯乙烯主链相连的甲硫氨酸取代磺酸根基团,不足以赋予所得树脂显著的抗凝血活性。

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