Beijing Hospital of Traditional Chinese Medicine, Capital Medical University, Beijing 100010, China.
Beijing Institute of Chinese Medicine, Beijing 100010, China.
Molecules. 2022 Jun 6;27(11):3643. doi: 10.3390/molecules27113643.
Arimisia annua L. is an important anticancer herb used in traditional Chinese medicine. The molecular basis underpinning the anticancer activity is complex and not fully understood, but the herbal polysaccharides, broadly recognised as having immunomodulatory, antioxidant and anticancer activities, are potential key active agents. To examine the functions of polysaccharides from A. annua, their immunomodulatory and antioxidant potentials were evaluated, as well as their structural characterization. The water-soluble polysaccharides (AAPs) were fractionated using size-exclusion chromatography to obtain three dominant fractions, AAP-1, AAP-2 and AAP-3, having molecular masses centered around 1684, 455 and 5.8kDa, respectively. The antioxidant potentials of the isolated polysaccharides were evaluated by measuring radical scavenging activities against DPPH● (2,2-diphenyl-1-picrylhydrazyl radical), ABTS●+ (2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid radical ion), and the OH● (hydroxyl radical). AAP-1 displayed high antioxidant activities against these radicals, which were 68%, 73% and 78%, respectively. AAP-2 displayed lower scavenging activities than the other two fractions. Immunostimulatory activities of AAPs were measured using mouse macrophages. The three polysaccharide fractions displayed significant antioxidant activities and stimulated the production of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). AAP-1 showed significant immunostimulatory activity (16-fold increase in the production of IL-6 compared to the control and 13-fold increase in the production of TNF-α) with low toxicity (>60% cell viability at 125 μg/mL concentration). Preliminary structural characterization of the AAPs was carried out using gas chromatography (GC) and FTIR techniques. The results indicate that AAP-1 and AAP-2 are pyranose-containing polysaccharides with β-linkages, and AAP-3 is a β-fructofuranoside. The results suggest that these polysaccharides are potential candidates for immunotherapy and cancer treatment.
青蒿素是一种重要的抗癌草药，用于传统中药。抗癌活性的分子基础复杂且尚未完全理解，但草药多糖，广泛认为具有免疫调节、抗氧化和抗癌活性，是潜在的关键活性物质。为了研究青蒿多糖的功能，评估了其免疫调节和抗氧化潜力，并对其结构进行了表征。采用凝胶渗透色谱法对水溶性多糖（AAPs）进行了分级，得到了三个主要的级分，AAP-1、AAP-2 和 AAP-3，分子量分别集中在 1684、455 和 5.8 kDa 左右。通过测量对 DPPH●（2,2-二苯基-1-苦基肼自由基）、ABTS●+（2,2′-偶氮-双（3-乙基苯并噻唑啉-6-磺酸自由基）和 OH●（羟基自由基）的自由基清除活性来评估分离多糖的抗氧化潜力。AAP-1 对这些自由基显示出高抗氧化活性，分别为 68%、73%和 78%。AAP-2 显示出比其他两个级分更低的清除活性。使用小鼠巨噬细胞测量 AAPs 的免疫刺激活性。这三个多糖级分均显示出显著的抗氧化活性，并刺激肿瘤坏死因子-α（TNF-α）和白细胞介素-6（IL-6）的产生。与对照组相比，AAP-1 表现出显著的免疫刺激活性（IL-6 的产量增加了 16 倍），而 TNF-α 的产量增加了 13 倍），且毒性较低（在 125μg/mL 浓度下细胞存活率>60%）。使用气相色谱（GC）和傅里叶变换红外（FTIR）技术对 AAPs 进行了初步结构表征。结果表明，AAP-1 和 AAP-2 是含有吡喃糖的多糖，具有β键，AAP-3 是β-果糖呋喃糖苷。这些结果表明，这些多糖可能是免疫疗法和癌症治疗的候选药物。
