Hui Yu-Jing, Yu Jin-Gao, Tang Zhi-Shu, Wang Mei, Song Zhong-Xing, Liu Hong-Na, Zhou Jian-Ping, Cao Zhao-Jun
Shaanxi Collaborative Innovation Center of Chinese Medicine Resources Industrialization/State Key Laboratory of Research& Development of Characteristic Qin Medicine Resources (Cultivation)/Shaanxi Innovative Drug Research Center, Shaanxi University of Chinese Medicine Xianyang 712046, China.
Shaanxi Collaborative Innovation Center of Chinese Medicine Resources Industrialization/State Key Laboratory of Research& Development of Characteristic Qin Medicine Resources (Cultivation)/Shaanxi Innovative Drug Research Center, Shaanxi University of Chinese Medicine Xianyang 712046, China China Academy of Chinese Medical Sciences Beijing 100700, China.
Zhongguo Zhong Yao Za Zhi. 2022 Dec;47(23):6380-6390. doi: 10.19540/j.cnki.cjcmm.20220128.301.
Wuling Capsules is one of the commonly used drugs for the clinical treatment of chronic hepatitis B with the syndrome of liver Qi stagnation, spleen deficiency, and blood stasis. However, the present preparation method of Wuling Capsules ignores some macromolecules like polysaccharides. In this study, the influences of different ethanol concentrations in the preparation process on the extraction rates of macro-and micro-molecules were investigated. Further, the therapeutic efficacy of Wuling Capsules was evaluated with the reserpine-induced rat model of liver Qi stagnation, spleen deficiency, and blood stasis. When 50% ethanol was used for the last time of extraction, the concentrations of polysaccharides, salvianolic acid B, and schisandrin in the extract, as well as the dry extract yield, increased significantly compared with those of the original preparation method. However, the fingerprints of micro-molecules showed little difference between the two methods, with a similarity of 0.862. The study then set the 50% ethanol extraction as the new preparation method. The pharmacodynamics evaluation showed that the Wuling Capsules prepared with the original and new methods both significantly alleviated the emotional depression and metabolic disturbance in model rats, demonstrating good performance in protecting the rats against gastric mucosal injuries, modulating intestinal function, and activating blood circulation. The mechanism of action may be related to the regulation of gastrointestinal hormone secretion, reduction of inflammation, and promotion of dopamine synthesis in cortex and hippocampus. At the same dose, the Wuling Capsules prepared with the original and new methods showed roughly the same overall therapeutic efficacy. However, the Wuling Capsules prepared with the new method had stronger effect in activating blood circulation and modulating inflammation, but weaker effects in regulating gastrin and dopamine. The present study provides basis data for optimizing the preparation process of Wuling Capsules and deciphering the mechanism of its therapeutic effect on liver Qi stagnation, spleen deficiency, and blood stasis.
五灵胶囊是临床治疗肝郁脾虚血瘀型慢性乙型肝炎常用药物之一。然而，目前五灵胶囊的制备方法忽略了一些大分子物质，如多糖。本研究考察了制备过程中不同乙醇浓度对大分子和小分子提取率的影响。此外，采用利血平诱导的肝郁脾虚血瘀大鼠模型对五灵胶囊的治疗效果进行了评价。当最后一次提取采用50%乙醇时，提取物中多糖、丹酚酸B和五味子醇甲的含量以及干浸膏得率较原制备方法均显著提高。然而，两种方法的小分子指纹图谱差异不大，相似度为0.862。研究随后将50%乙醇提取设定为新的制备方法。药效学评价表明，采用原方法和新方法制备的五灵胶囊均能显著缓解模型大鼠的情绪低落和代谢紊乱，在保护大鼠胃黏膜损伤、调节肠道功能和活血化瘀方面表现良好。作用机制可能与调节胃肠激素分泌、减轻炎症以及促进皮质和海马中多巴胺合成有关。在相同剂量下，采用原方法和新方法制备的五灵胶囊总体治疗效果大致相同。然而，新方法制备的五灵胶囊在活血化瘀和调节炎症方面作用较强，但在调节胃泌素和多巴胺方面作用较弱。本研究为优化五灵胶囊的制备工艺及阐明其治疗肝郁脾虚血瘀证的作用机制提供了基础数据。
