| 引用本文: |
关晓娴, 于兴泰, 张馨雨, 王浩捷, 胡哲铭, 闫丽文, 王文艺, 孙萌, 陆洋.化橘红水提物与醇提物药效差异比较及水煎工艺增效物质基础初步研究[J].湖南中医药大学学报,2026,46(7):1387-1396[点击复制] |
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| 化橘红水提物与醇提物药效差异比较及水煎工艺增效物质基础初步研究 |
| 关晓娴,于兴泰,张馨雨,王浩捷,胡哲铭,闫丽文,王文艺,孙萌,陆洋 |
| (北京中医药大学中药学院, 北京 102488) |
| 摘要: |
| 目的 比较化橘红水提物与醇提物的药效差异及化学成分组成，初步探讨传统水煎工艺增效的物质基础。方法 建立氨水诱导小鼠咳嗽模型和气管酚红排泄模型，将小鼠随机分为模型对照组、阳性药物组及水/醇提物低、中、高剂量组（200、400、800 mg/kg）。评价镇咳祛痰活性；采用UPLC-MS分析成分组成；HPLC测定柚皮苷含量；以人工胃液为溶出介质，小杯法比较水提物、醇提物及果胶多糖-醇提物混合物的体外溶出；使用动态光散射法、扫描电子显微镜法、荧光显微镜观察微观形貌，激光粒度仪测定粒径分布与Zeta电位。结果 水提物低剂量组镇咳效果优于醇提物低剂量组（P<0.05）；水提物低、高剂量组祛痰效果均优于醇提物低、高组（P<0.05或P<0.01）。化橘红水/醇提物的化学成分谱相似，但水提物中柚皮苷含量较低；体外溶出结果表明，醇提物中柚皮苷释放快速，添加果胶多糖的醇提物混合物溶出行为趋近于化橘红水提物（f2>50），均呈现缓慢持续释放特征；微观形貌及粒径提示，水提物可形成稳定均一的纳米复合物，而醇提物稳定性较差；果胶修饰后醇提物颗粒特性接近水提物，但均一性稍逊。结论 化橘红水提物镇咳祛痰药效优于醇提物，可能与果胶多糖和柚皮苷在水煎过程中形成自组装纳米复合物有关，该纳米复合物改变柚皮苷释放速率以及改善其分散状态。 |
| 关键词: 化橘红|镇咳祛痰|柚皮苷|果胶|分子间相互作用 |
| DOI：10.3969/j.issn.1674-070X.2026.07.009 |
| 投稿时间：2026-01-12 |
| 基金项目:中国原子能科学研究院稳定性支持经费科研项目（CNNCWZ-2023002）；国家中医药管理局高水平中医药重点学科建设项目（zyyzdxk-2023272）。 |
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| Comparative study on pharmacological differences between aqueous and ethanolic extracts of Huajuhong (Citri Grandis Exocarpium) and preliminary investigation of material basis for efficacy-enhancement of water decoction process |
| GUAN Xiaoxian, YU Xingtai, ZHANG Xinyu, WANG Haojie, HU Zheming, YAN Liwen, WANG Wenyi, SUN Meng, LU Yang |
| (School of Chinese Medicine, Beijing University of Chinese Medicine, Beijing 102488, China) |
| Abstract: |
| Objective To compare the pharmacological differences and chemical composition between aqueous and ethanolic extracts of Huajuhong (Citri Grandis Exocarpium), and to preliminarily investigate the material basis for the efficacy-enhancement of the traditional water decoction process. Methods An ammonia-induced cough model and a tracheal phenol red excretion model were established in mice. The mice were randomly divided into model control group, positive drug group, and low-, medium-, and high-dose groups (200, 400, 800 mg/kg) of the aqueous or ethanolic extracts, and the antitussive and expectorant activities were evaluated. Chemical composition was analyzed by UPLC-MS, and the content of naringin was determined by HPLC. Using simulated gastric fluid as the dissolution medium, the in vitro dissolution of the aqueous extract, the ethanolic extract, and a mixture of pectin polysaccharide and the ethanolic extract was compared by the small-cup method. The microscopic morphology was observed by dynamic light scattering, scanning electron microscopy, and fluorescence microscopy, while the particle size distribution and zeta potential were measured with a laser particle size analyzer. Results The low-dose aqueous extract group showed significantly better antitussive effects than the ethanolic extract group at the same dose (P<0.05). Both the low- and high-dose aqueous extract groups exhibited significantly superior expectorant effects compared to the corresponding ethanolic extract groups (P<0.05 or P<0.01). The chemical composition profiles of the aqueous and ethanolic extracts were similar, but the naringin content in the aqueous extract was lower. In vitro dissolution results indicated that naringin was released rapidly from the ethanolic extract, whereas the dissolution behavior of the ethanolic extract supplemented with pectin polysaccharide approached that of the aqueous extract (similarity factor f2>50), with both showing slow and sustained release characteristics. Microscopic morphology and particle size analysis suggested that the aqueous extract could form stable and uniform nanocomplexes, while the ethanolic extract exhibited poor stability. After pectin modification, the particle characteristics of the ethanolic extract became similar to those of the aqueous extract, albeit with slightly inferior uniformity. Conclusion The superior antitussive and expectorant efficacy of the aqueous extract of Huajuhong (Citri Grandis Exocarpium) over the ethanolic extract may be attributed to the formation of self-assembled nanocomplexes between pectin polysaccharide and naringin during the water decoction process, which alter the release rate of naringin and improve its dispersion state. |
| Key words: Huajuhong (Citri Grandis Exocarpium)|antitussive and expectorant|naringin|pectin|intermolecular interactions |
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