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Studies on the Syntheses of Bioactive Chitin Derivatives.

生物活性甲壳素衍生物的合成研究。

基本信息

批准号：
60430025
负责人：
TOKURA Seiichi
金额：
$ 13.44万
依托单位：
Hokkaido University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (A)
财政年份：
1985
资助国家：
日本
起止时间：
1985 至 1988
项目状态：
已结题

项目摘要

Various chitin derivatives were prepared to investigate the artificial control of antigenicity, biodegradabillity and blood compatibility for a biomedical applications. A relatively long-acting immunoadjuvant activity was achieced by 70% deacetylated chitin(DAC-70) among variously deacetylated chitins, and a short-acting immunoadjuvant was found in 80% carboxymethylated chitin(substituted at C-6 position of the GLcNAc residues) and also among variously substituted carboxymethyl(CM)-chitins. The immunoadjuvant activity of DACs seems to disappear upon carboxymethylation or O-N-sulfations. The immunoadjuvant property of CM-chitins was assumed to be fairly different from those of DACs and also disappeared by deacetylation, further carboxymethylation at the C-3 position, or by O-sulfation. CM-chitin was demonstrated to act as a hapten carrier which induced hapten specific antibody production in the presence of Freund's complete adjuvant, and as a controlled-release drug carrier in the absence of Freund's complete sdjuvant.A 70% deacetylated-60%-CM-chitin was converted to a blood compatible, nonbiodegradable material when it was sulfated on the hydroxyl groups at C-6 and on some of the C-3 position. A preliminary test found no toxicity of these CM-chitin heparinoids, when they were injected into rat veins.

制备了各种甲壳素衍生物，以研究人工控制的抗原性，生物降解性和血液相容性的生物医学应用。在各种脱乙酰甲壳素中，70%脱乙酰甲壳素（DAC-70）具有较长的免疫佐剂活性，80%羧甲基甲壳素（取代在GLcNAc残基的C-6位）和各种取代的羧甲基（CM）甲壳素具有较短的免疫佐剂活性。DAC的免疫佐剂活性似乎在羧甲基化或O-N-硫酸化后消失。CM-几丁质的免疫佐剂性质被认为与DAC的免疫佐剂性质相当不同，并且也通过脱乙酰化、C-3位的进一步羧甲基化或O-硫酸化而消失。羧甲基甲壳素（CM-chitin）是一种半抗原载体，在弗氏完全佐剂存在下可诱导半抗原特异性抗体的产生，在弗氏完全佐剂不存在下可作为药物控释载体。脱乙酰基70%-60%-CM-chitin在C-6位和部分C-3位的羟基上硫酸化后，可转化为血液相容性、非生物降解材料。初步试验发现，这些CM-甲壳素类肝素注射到大鼠静脉时没有毒性。