Yamada H
Oriental Medicine Research Center, Kitasato Institute, Tokyo, Japan.
Nihon Yakurigaku Zasshi. 1995 Sep;106(3):229-37. doi: 10.1254/fpj.106.229.
Several pharmacological activities have been observed in pectic polysaccharides which were isolated from Chinese herbs containing Kampo medicines. We found two different bioactive pectic polysaccharides, bupleuran 2IIb and 2IIc, from the roots of Bupleurum falcatum. These bioactive pectic polysaccharides were comprised of an alpha (1-->4) linked galacturonan region, a ramified region that consists of a rhamnogalacturonan core substituted neutral sugar chains as the side chains and a rhamnogalacturonan II (RG II)-like region containing unique sugars such as 3-deoxy-manno-2-octulosonic acid (KDO). In order to understand the pharmacological activity of pectic polysaccharides on the molecular level, we have elucidated the essential carbohydrate structure for the expression of each pharmacological activity and their mode of actions. The ramified region in bupleuran 2IIb induced Fc receptor up-regulation in macrophages by a mechanism dependent on an increase of intracellular Ca2+, followed by the enhancement of immune complex clearance, whereas bupleuran 2IIc, which mainly consists of a partially branched galacturonan region, showed potent anti-ulcer activity. The major mechanism of its mucosal protection was suggested to be due to anti-secretory activity on acid and pepsin, its ability to provide a protective coating and radical scavenging effect. The future problems were also discussed in order to develop pectic polysaccharides as medicines.
从含有汉方药物的中药材中分离得到的果胶多糖具有多种药理活性。我们从柴胡的根部发现了两种不同的生物活性果胶多糖，柴胡多糖2IIb和2IIc。这些生物活性果胶多糖由一个α(1→4)连接的半乳糖醛酸区域、一个分支区域（该区域由鼠李半乳糖醛酸核心取代的中性糖链作为侧链组成）以及一个含有3-脱氧甘露-2-辛酮糖酸（KDO）等独特糖类的鼠李半乳糖醛酸II（RG II）样区域组成。为了从分子水平上理解果胶多糖的药理活性，我们阐明了每种药理活性表达所需的碳水化合物结构及其作用方式。柴胡多糖2IIb中的分支区域通过一种依赖于细胞内Ca2+增加的机制诱导巨噬细胞中Fc受体上调，随后增强免疫复合物清除能力，而主要由部分分支的半乳糖醛酸区域组成的柴胡多糖2IIc则表现出强大的抗溃疡活性。其黏膜保护的主要机制被认为是由于对酸和胃蛋白酶的抗分泌活性、提供保护涂层的能力以及自由基清除作用。为了将果胶多糖开发成药物，还讨论了未来存在的问题。
