Chen Yaping, Wen Qiuqi, Lin Meng, Yang Bing, Feng Liang, Jia Xiaobin
School of Traditional Chinese Pharmacy, Innovation Center for Industry-Education Integration of Pediatrics and Traditional Chinese Medicine, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 211198, China.
Pharmaceuticals (Basel). 2024 Dec 12;17(12):1675. doi: 10.3390/ph17121675.
Traditional Chinese Medicine (TCM) is recognized for its complex composition and multiple therapeutic targets. However, current pharmacological research often concentrates on extracts or individual components. The former approach faces numerous challenges, whereas the latter oversimplifies and disregards the synergistic effects among TCM components. This study aims to investigate the scientific validity of focusing on the active constituent in TCM efficacy research, using () as a case study. Through spectrum-effect correlation analysis, network pharmacology, and molecular docking, five active ingredients of were identified: puerarin, formononetin, tuberosin, 4',7-dihdroxy-3'-methoxyisoflavone, and Daidzein-4,7-diglucoside. These ingredients were combined to form an active constituent, which was subsequently tested in vitro and in vivo. In in vitro, the active constituent exhibited superior effects in enhancing glucose consumption and glycogen synthesis compared to both the extract and individual components. In vivo experiments demonstrated that medium and high doses of the active constituent were significantly more effective than extract, with effects comparable to those of metformin in reducing blood sugar levels. The active constituent effectively improves T2DM by lowering blood glucose levels, promoting glycogen synthesis, and modulating glycolipid metabolism. Both in vitro and in vivo studies indicate that it outperformed the extract and individual components. This study establishes the scientific validity and feasibility of utilizing the active constituent as the focus for investigating the efficacy of TCM, thereby offering novel insights and a new research paradigm for future TCM investigations.
中药因其成分复杂和具有多种治疗靶点而受到认可。然而,目前的药理学研究往往集中在提取物或单个成分上。前一种方法面临诸多挑战,而后一种方法则过于简化,忽视了中药成分之间的协同作用。本研究旨在以()为例,探讨在中药疗效研究中聚焦活性成分的科学合理性。通过谱效关系分析、网络药理学和分子对接,确定了()的五种活性成分:葛根素、芒柄花素、块茎糖、4',7-二羟基-3'-甲氧基异黄酮和大豆苷元-4,7-二葡萄糖苷。将这些成分组合形成一种活性成分,随后在体外和体内进行测试。在体外,与()提取物和单个成分相比,该活性成分在增强葡萄糖消耗和糖原合成方面表现出更优的效果。体内实验表明,中高剂量的活性成分比()提取物显著更有效,在降低血糖水平方面的效果与二甲双胍相当。该活性成分通过降低血糖水平、促进糖原合成和调节糖脂代谢有效地改善了2型糖尿病。体外和体内研究均表明,它优于()提取物和单个成分。本研究确立了以活性成分为重点研究中药疗效的科学合理性和可行性,从而为未来的中药研究提供了新的见解和新的研究范式。