Preparation and anticoagulant activity of the phosphosulfomannan PI-88

被引：72
作者：
Yu, GL
Gunay, NS
Linhardt, RJ
Toida, T
Fareed, J
Hoppensteadt, DA
Shadid, H
Ferro, V
Li, CP
Fewings, K
Palermo, MC
Podger, D
机构：
[1] Univ Iowa, Dept Chem, Div Med & Nat Prod Chem, Dept Chem & Biochem Engn, Iowa City, IA 52242 USA
[2] Chiba Univ, Sch Pharmaceut Sci, Chiba, Japan
[3] Loyola Univ, Med Ctr, Dept Pathol & Pharmacol, Maywood, IL 60153 USA
[4] Progen Ind Ltd, Dept Res & Dev, Brisbane, Qld 4076, Australia
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 37卷 / 10期
关键词：
phosphomarman; phosphosulfomannan; anticoagulant; capillary electrophoresis; PI-88;
D O I：
10.1016/S0223-5234(02)01347-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A yeast-derived phosphomannan mixture was chemically sulfonated and the composition and structure of the product mixture was studied. This phosphosulfomannan mixture, PI-88, is currently under clinical evaluation as an anti-cancer agent. Analysis using capillary electrophoresis demonstrated that PI-88 was a multi-component mixture. Gel permeation chromatography provided four fractions of PI-88 that contained components which differed in size from disaccharide to hexasaccharide, and by degree of sulfation. These fractions were characterised by spectroscopic and chromatographic methods and the structure of PI-88 is that expected based On the structure of the phosphomannan starting material. The anticoagulant activity of these fractions was evaluated and the structural requirements for,activity are described. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
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收藏
页码：783 / 791
页数：9
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