三七“生打熟补”效用关联的物质基础及个体化质控方法研究

During hundreds of years of medication, there was a saying for Notoginseng Radix that “the crude drugs hit and the cooked ones tonify”. The so-called “hit” means Notoginseng Radix can stop bleeding, promote blood circulation, diminish swelling and ease pain. The "tonify" means that it can enrich and regulate the blood, replenish the body and improve the health. However, the crude drugs and the cooked ones in the clinic use and market circulation were undifferentiated, which might bring the unstable curative effects or even adverse reactions. Since the efficacy differences between the crude Notoginseng Radix and cooked materials were difficult to be represented by current quality control (QC) indices, an individualized QC method was proposed and developed to differentiate the effects between the crude and the cooked ones. According to the basic understanding that there were differences in the efficacies, related constituents and targets for treating different diseases between the crude and the cooked drugs, we applied the chemical detection, biological evaluation and spectrum-effect analysis methods to study the constituents difference correlated to the efficacies. The reverse docking and target prediction techniques were applied to investigate the possible mechanisms related to the efficacies of the crude drugs and the cooked ones. On the basis of clarifying the authenticity of “the crude hitting and the cooked tonifying”, as well as the constituents difference, the Effect-constituent Index (ECI) of Notoginseng Radix was established to guide the individualized quality control and efficacy representation of the crude drugs and cooked ones. We hope to provide some references for the rational drug use of Notoginseng Radix, and the strategy for the QC and evaluation of other Chinese materia medica (CMM) with difference in the use between the crude and cooked, as well as the promotion of accurate quality standard of CMM.

三七在数百年的用药历史中具有“生打熟补”之说，所谓“打”指三七能止血活血、消肿定痛，“补”指其能补血理血，补益强身。但是，当前临床使用及市场流通时未将生、熟三七明显区分，生、熟制品常作为同一药材或饮片使用，易造成使用时疗效的不稳定性甚至不良反应。针对现行质控方法难以合理有效表征生、熟三七效用差异这一问题，本项目根据生、熟药材功用不同、发挥药效物质不同、对不同疾病作用靶标不同的基本认识，采用化学检测、生物评价及谱效相关技术分析三七功效关联的物质差异，通过活性成分的反向对接及靶点预测探讨三七发挥不同药效的可能机制，在初步阐明其“生打熟补”效用的客观真实性和物质差异的基础上，构建生、熟三七效应成分指数（Effect-constituent Index，ECI）个体化质控方法及标准，为指导生、熟三七合理用药，以及其它生熟异用中药质量的科学评控，和精准化中药标准的提升提供研究思路及技术参考。

三七在数百年的用药历史中具有“生打熟补”之说，所谓“打”指三七能止血活血、消肿定痛，“补”指其能补血理血，补益强身。但是，当前临床使用及市场流通时未将生、熟三七明显区分，生、熟制品常作为同一药材或饮片使用，易造成使用时疗效的不稳定性甚至不良反应。针对现行质控方法难以合理有效表征生、熟三七效用差异这一问题，本项目根据生、熟药材功用不同、发挥药效物质不同、对不同疾病作用靶标不同的基本认识，采用化学检测、生物评价及谱效相关技术分析三七功效关联的物质差异，通过网络药理学预测分析结合药理模型验证，对三七相关药效作用机制进行了探讨，在初步阐明其“生打熟补”效用的客观真实性和物质差异的基础上，对关联生、熟三七不同功效的指标性成分给出了建议，并针对不同效应构建了三七效应成分指数（Effect-constituent Index，ECI），对其在个体化评价三七不同效用及质控方面的应用进行了探讨，以期为指导生、熟三七合理用药，以及其它生熟异用中药质量的科学评控，和精准化中药标准的提升提供研究思路及技术参考。