基于血药协同作用研究抗风湿民族药荨麻的质量评价指标

Multi-component synergetic effect is the characteristic and advantage of ethnomedicines and traditional Chinese medicines (TCMs). The quality evaluation standard of ethnomedicines and TCMs should include the mainly active and synergetic ingredients. How to study the quality evaluation index is the tough problem in the modern research of ethnomedicines and TCMs. So, a novel research method for the quality evaluation index based on the synergetic effect of the constituents absorbed into blood is put forward in the present application. Taken the widely-used ethnomedicine Uritcae Fissae Herba as an example: firstly, the mainly active and synergetic constituents absorbed into blood will be screened as the effective constituents by cell experiments in vitro; and then, the effective constituents will be adversely traced to the materia medica, and the influences of the other ingredients on the anti-rheumatic activities and pharmacokinetics parameters of the effective constituents will be further investigated to elaborate the synergetic constituents in the materia medica. Finally, the quality evaluation criteria consist of the effective and synergetic constituents will be established. The accomplishment of this project will not only provide the scientific proof to the modern quality evaluation of Uritcae Fissae Herba for rheumatism, but also supply a novel exploratory method to establish the quality evaluation criteria of ethnomedicines and TCMs.

多成分协同作用是民族药/中药的特色和优势，其质量评价标准不应局限于主要活性成分，还应包括协同成分。如何确定质量评价指标是民族药/中药现代研究中亟待解决的难题之一。鉴于此，本申请提出基于血药成分协同作用研究民族药/中药质量评价指标的思路。以多个民族广泛应用的荨麻为例：首先研究血药成分及其协同作用，发现体内功效成分；然后通过逆向追踪，确定药材中的主要活性成分；进而考察药材其他成分对主要活性成分抗风湿作用及药代动力学参数的影响，发现药材中的主要协同成分；最终建立包括主要活性成分及协同成分在内的、反映荨麻抗风湿作用的质量评价指标。本申请的完成不仅将为荨麻的质量评价提供科学依据，同时也将为如何建立民族药/中药的现代质量评价标准提供一种研究思路。

民族药/中药化学成分复杂，其作用又往往是多成分协同作用的结果，如何确定质量评价指标是民族药/中药现代化研究中的瓶颈问题。针对这一研究难题，本课题提出基于协同作用研究民族药/中药质量评价指标的思路。以多个民族广泛应用的荨麻为例：首先系统研究了荨麻的化学成分，从中分离鉴定了113个成分（其中：新化合物11个、新的天然产物2个、首次从荨麻中分得化合物86个）；筛选了荨麻抗风湿的活性组分，发现荨麻抗风湿是多组分协同作用的结果，进而确定了协同组分及初步协同机制；在此基础上，采用UPLC-DAD/-Q-TOF-MS技术分析了荨麻入血成分，从中鉴定了24个药源性成分；进一步对入血成分进行了活性测试，确定了体内活性成分及协同成分；最终建立了包括主要活性成分及协同成分在内的、反映荨麻抗风湿作用的7个质量评价指标。本课题不仅为荨麻的质量评价提供了科学依据，同时也为民族药/中药的质量评价标准提供了研究思路。