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曾琼丽, 王玉凤, 张恒, 肖炜婷, 杨蒂, 韩越, 王雄龙, 李顺祥, 欧阳文.土牛膝总皂苷的提取、成分鉴定及抗炎活性研究[J].湖南中医药大学学报英文版,2024,44(6):1009-1017.[Click to copy
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| 土牛膝总皂苷的提取、成分鉴定及抗炎活性研究 |
| 曾琼丽,王玉凤,张恒,肖炜婷,杨蒂,韩越,王雄龙,李顺祥,欧阳文 |
| (湖南中医药大学药学院, 湖南 长沙 410208;湖南省普通高等学校中药现代化研究重点实验室, 湖南 长沙 410208;湖南中医药大学附属第二中西医结合医院, 湖南 浏阳 410300;湖南时代阳光药业股份有限公司, 湖南 永州 410116;浏阳市中医医院, 湖南 浏阳 410300) |
| 摘要: |
| 目的 对土牛膝总皂苷进行体内外抗炎活性与分离鉴定研究，为其治疗炎症提供实验依据。方法 采用十八烷基硅烷键合硅胶-AQ柱色谱法（ODS-AQ）纯化制备土牛膝总皂苷；建立氨水诱导的急性咽炎大鼠模型，灌胃给药评价粗毛牛膝提取物及总皂苷抗炎活性；采用柱层析、核磁共振谱、质谱等技术对土牛膝总皂苷中的主要化合物进行分离、纯化和结构鉴定；建立脂多糖诱导的巨噬细胞炎症模型，评价各皂苷单体化合物的抗炎活性。结果 制备的粗毛牛膝总皂苷含量达到81.8%；在急性咽炎大鼠模型中，粗毛牛膝总皂苷及水煎液具有良好抗炎疗效，能显著降低血清IL-6、IL-1β、TNF-α细胞因子水平；总皂苷中鉴定出6个齐墩果烷型三萜皂苷，分别为竹节参皂苷Ⅳa（1）、竹节参皂苷Ⅳa丁酯（2）、金盏花皂苷E（3）、金盏花皂苷E丁酯（4）、竹节参皂苷I（5）、竹节参皂苷Ⅴ（6）；体外炎症模型表明，分离得到的三萜皂苷类单体化合物均有不同程度的抗炎作用。结论 首次系统证明了皂苷类成分是粗毛牛膝发挥抗炎活性的药效物质基础；从牛膝属植物中首次分离得到化合物2和4，并证实其具有抗炎作用。 |
| 关键词: 粗毛牛膝 抗炎 咽炎 三萜皂苷 化学成分 分离鉴定 |
| DOI：10.3969/j.issn.1674-070X.2024.06.011 |
| Received:December 30, 2023 |
| 基金项目:湖南省教育厅重点课题（23A0303）；湖南省普通高等学校教学改革研究项目（HNJG-2021-0577）；湖南中医药大学研究生科研创新项目（CX20210709，2023CX72）；湖南中医药大学学位与研究生教育教学改革研究课题（2021JG04）；湖南中医药大学中药学一流建设学科（校行科字〔2018〕3号）。 |
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| Extraction, composition identification, and anti-inflammatory activity of total saponins from Achyranthes aspera L. |
| ZENG Qiongli, WANG Yufeng, ZHANG Heng, XIAO Weiting, YANG Di, HAN Yue, WANG Xionglong, LI Shunxiang, OUYANG Wen |
| (School of Pharmacy, Hunan University of Chinese Medicine, Changsha, Hunan 410208, China;Key Laboratory of Modern Research of TCM, Education Department of Hunan Province, Changsha, Hunan 410208, China;The Second Integrated Chinese and Western Medicine Hospital of Hunan University of Chinese Medicine, Liuyang, Hunan 410300, China;Hunan Time Sun Pharmaceutical Co. Ltd., Yongzhou, Hunan 410116, China;Liuyang Hospital of Chinese Medicine, Liuyang, Hunan 410300, China) |
| Abstract: |
| Objective To study the in vivo and in vitro anti-inflammatory activity, as well as isolation and identification of total saponins from Achyranthes aspera L., providing experimental evidence for its treatment of inflammation. Methods The total saponins of Achyranthes aspera L. were purified and prepared by ODS-AQ; after modeling of ammonia-induced acute pharyngitis, rats were treated with corresponding drugs by gavage to evaluate the anti-inflammatory activities of the extract and total saponins of Achyranthes aspera L.; column chromatography, nuclear magnetic resonance spectroscopy (NMR), mass spectrometry (MS), and other techniques were used to isolate, purify, and identify the main compounds in the total saponins of Achyranthes aspera L.; a lipopolysaccharide-induced macrophage inflammation model was established to evaluate the anti-inflammatory activity of various saponin monomers. Results The prepared total saponins of Achyranthes aspera L. reached a content of 81.8%; in the acute pharyngitis rat model, the total saponins and aqueous extract of Achyranthes aspera L. showed good anti-inflammatory effects, significantly reducing the serum levels of IL-6, IL-1β, and TNF-α; six oleanane-type triterpenoid saponins were identified as chikusetsusaponin Ⅳa (1), chikusetsusaponin Ⅳa butyl ester (2), calendulaside E (3), calendulaside E butyl ester (4), chikusetsusaponin I (5), and chikusetsusaponin Ⅴ (6). In vitro inflammation model indicated that the isolated triterpenoid saponin monomers all exhibited varying degrees of anti-inflammatory effects. Conclusion This paper systematically demonstrates for the first time that saponin components are the pharmacological material basis for the anti-inflammatory activity of Achyranthes aspera L.. Compounds 2 and 4 with anti-inflammatory effects are ester first isolated from Achyranthes plants |
| Key words: Achyranthes aspera L. antiinflammation pharyngitis triterpenoid saponin chemical composition isolation and identification |
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