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从核盘菌IFO 9395培养滤液中获得的6-支链(1→3)-β-D-葡聚糖SSG的羟乙基化衍生物的制备及其抗肿瘤活性

Preparation and antitumor activity of hydroxyethylated derivatives of 6-branched (1----3)-beta-D-glucan, SSG, obtained from the culture filtrate of Sclerotinia sclerotiorum IFO 9395.

作者信息

Kurachi K, Ohno N, Yadomae T

机构信息

Lab. Immunopharmacology of Microbial Products, Tokyo College of Pharmacy, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1990 Sep;38(9):2527-31. doi: 10.1248/cpb.38.2527.

Abstract

SSG is an antitumor branched (1----3)-beta-D-glucan obtained from the culture filtrate of Sclerotinia sclerotiorum IFO 9395. Hydroxyethylation of SSG higher than MS 0.45 (MS value represents molar ratio of hydroxyethyl group vs. glucosyl group) by ethyleneoxide in aqueous sodium hydroxide lose the antitumor activity. Degradation of branching point of hydroxyethylated SSG (HE-SSG) by the sequential treatments of periodate oxidation, borohydride reduction, and mild acid hydrolysis of these derivatives regenerated the antitumor activity. These results directly demonstrated that the branching point covered, at least a part of, the dormant active site of SSG.

摘要

SSG是一种从核盘菌IFO 9395的培养滤液中获得的抗肿瘤支链(1----3)-β-D-葡聚糖。在氢氧化钠水溶液中用环氧乙烷对SSG进行羟乙基化,当取代度高于0.45(取代度值代表羟乙基与葡糖基的摩尔比)时,会失去抗肿瘤活性。通过对这些衍生物依次进行高碘酸盐氧化、硼氢化物还原和温和酸水解来降解羟乙基化SSG(HE-SSG)的分支点,可使抗肿瘤活性再生。这些结果直接表明,分支点至少覆盖了SSG的部分休眠活性位点。

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