As a special traditional Chinese medicine, Astragalus polysaccharides for injection (APS, batch no. Zhunzi Z20040086) includes complex polysaccharide macromolecules that may increase the risk upon application. Although fingerprints for quality control are available, the specific active ingredients are unclear. Identifying the active components is the key to reduce the risk of adverse reactions of the drug. In this work, APS was mainly separated into two components, namely, macromolecular component (APS-I) and small molecular components (APS-II). The molecular weight measurement revealed that the average molecular weight of APS-I exceeded 500 kDa, and that of APS-II was 10 kDa. Monosaccharide-composition analysis revealed that APS-I consisted of glucose, galactose, arabinose, rhamnose, and galacturonic acid, with a ratio of approximately 1.5:1:5.4:0.08:0.1. Meanwhile, APS-II consisted of glucose, galactose, arabinose, rhamnose, and galacturonic acid, with a molar ratio of 9:1:1.4:0.04:0.001. Methylation, FT-IR, and NMR analysis indicated that the APS-I monosaccharide residue was linked as follows: D-Glcp-(1→, →4)-D-Glcp-(1→, →2)-L-Rhap-(1→, D-Araf-(1→, →5)-D-Araf-(1→, →2,5)-D-Araf-(1→, →4)-D-Galp-(1 → . Meanwhile, the APS-II monosaccharide residue was connected as follows: α-D-Glcp-(1→, →4)-α-D-Glcp-(1→, →6)-α-D-Glcp-(1→, →4,6)-α-D-Glcp-(1→, →3,4,6)-α-D-Glcp-(1→, →2)-α-L-Rhap-(1→, α-D-Araf-(1→, →5)-α-D-Araf-(1→, →4)-β-D-Galp-(1 → . Screening experiments on their in vitro immunological activity showed that APS-II had stronger effect on innate and adaptive immunities than APS-I. In vivo animal experiments showed that APS-II can increase the leukocyte level of cyclophosphamide immunosuppressed mice and improve their immunomodulatory ability. Therefore, APS-II is the main active ingredient of APS and is expected to become a new generation of APS products.

作为一种特殊的中药，黄芪注射液（APS，批号准字Z20040086）包含复杂的多糖大分子，使用时可能会增加患病风险。尽管有用于质量控制的指纹，但尚不清楚具体的活性成分。鉴定活性成分是降低药物不良反应风险的关键。在这项工作中，APS主要分为两个成分，即大分子成分（APS-I）和小分子成分（APS-II）。分子量测量表明，APS-I的平均分子量超过500kDa，而APS-II的平均分子量为10kDa。单糖组成分析表明，APS-1由葡萄糖，半乳糖，阿拉伯糖，鼠李糖和半乳糖醛酸组成，比率约为1.5：1：5.4：0.08：0.1。同时，APS-II由葡萄糖，半乳糖，阿拉伯糖，鼠李糖和半乳糖醛酸组成，摩尔比为9：1：1.4：0.04：0.001。甲基化，FT-IR和NMR分析表明APS-1单糖残基的连接方式如下：D-Glcp - （1→，→4）-D-GLC p - （1→，→2）-L-鼠李p - （1→，d-阿糖胞苷˚F - （1→，→5）-D-阿糖胞苷˚F - （1→，→2,5）-D-Ara f-（1→，→4）-D-Gal p-（1→。）同时，APS-II单糖残基的连接方式如下：α-D-Glc p - （1→，→4）-α-d-GLC p - （1→，→6）-α-d-GLC p - （1→，→4,6）-α-d-GLC p - （ 1→，→3,4,6-）-α-d-GLC p - （1→，→2）-α-L-鼠李糖p - （1→，α-d-阿糖胞苷˚F - （1→，→5 ）-α-d-阿糖胞苷˚F - （1→，→4）-β-d-Gal的p-（1→。对其体外免疫活性的筛选实验表明，APS-II对先天免疫和适应性免疫的作用要强于APS-I；体内动物实验表明，APS-II可以增加被环磷酰胺免疫抑制的小鼠的白细胞水平，并且因此，APS-II是APS的主要活性成分，有望成为新一代APS产品。