摘要
五灵胶囊是临床上治疗慢性乙型肝炎属肝郁脾虚挟瘀证的常用药物之一,但其现有的提取制备工艺忽视了多糖等大分子活性成分。该研究考察了不同浓度乙醇提取对五灵胶囊中大分子和小分子活性成分提取率的影响,并采用利血平致肝郁脾虚挟瘀证大鼠模型对其药效进行评价和比较。结果表明,相较于原工艺,以50%乙醇进行末次提取时,提取液中多糖、丹酚酸B和五味子醇甲的浓度大幅上升,同时提取干膏率也明显增加;但成品粉末的小分子指纹图谱未发生显著变化(相似度达0.862)。以50%乙醇提取作为新工艺条件,原、新工艺条件下五灵胶囊均能显著改善利血平诱导的肝郁脾虚挟瘀证大鼠情绪抑郁和消化代谢异常,具有显著的保护胃黏膜、调节胃肠道功能以及活血化瘀等作用;其作用机制可能与调节胃肠道激素分泌,降低系统炎症水平,促进大脑皮层和海马中多巴胺合成等过程有关。在同等剂量下,原、新工艺条件下的五灵胶囊整体药效相当;但新工艺条件下五灵胶囊活血化瘀和调节免疫炎症水平的作用相对增强,而对胃泌素和多巴胺的调节作用相对变弱。该研究为五灵胶囊制备工艺的优化调整及其药效作用机制的深入研究提供了基础数据支撑。
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.
作者
惠玉晶
于金高
唐志书
王梅
宋忠兴
刘红娜
周建平
曹兆军
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;China Academy of Chinese Medical Sciences,Beijing 100700,China;Tsing Hua De Ren Xi'an Happiness Pharmaceutical Co.,Ltd.,Xi'an 710043,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2022年第23期6380-6390,共11页
China Journal of Chinese Materia Medica
基金
中药大品种品牌价值提升示范研究项目(202190025)
财政部和农业农村部:国家现代农业产业技术体系项目(CARS-21)
咸阳市2020重大科技专项(2020K01-20)。
关键词
五灵胶囊
制备工艺
利血平
肝郁脾虚挟瘀证
胃泌素
多巴胺
Wuling Capsules
preparation process
reserpine
syndrome of liver Qi stagnation
spleen deficiency
and blood stasis
gastrin
dopamine