本项目是已结题国家自然基金项目延续和深入。民族药滇白珠在多个民族中用于治疗风湿疾病，但是其活性成分颇有争议。基于滇白珠大极性部位有显著抗风湿活性，其所含多类成分均有很好的抗炎镇痛活性，申请者提出“滇白珠是多成分整体发挥抗炎镇痛作用”的工作思路。由于药物发挥药效是体内具有适宜动力学特征多种原形成分组及活性代谢物组的整体作用，本项目拟以前期化学成分、药理活性和分析方法为基础，以滇白珠抗风湿活性部位为对象，以体外化学成分、正常和病理状态下体内成分及药代动力学与药效动力学（PK/PD）相结合的方法，开展胃肠道生物转化吸收和成分分离鉴定，正常和病理机体体内成分确认分析及其体内发挥药效时间-浓度-效应三者关系建立的研究，阐明滇白珠抗炎镇痛体内代谢成分和体外原型有效成分及其变化规律，推测其抗风湿作用机制；建立活性部位指纹谱、量效指纹谱以及药物代谢指纹谱的多维抗风湿组分谱从而有效科学的质量控制和指导用药。

This project is the continuation and further study of the finished 81001697 NSFC. Compared with monomer salicylic acid methyl glucoside which has good anti-inflammatory activity, the active parts of Dianbaizhu, form the plant Gaultheria leucocarpa var. yunnanensis (Franch.) T. Z. Hsu & R. C. Fang, process better activity. Not only the salicylic acid methyl glucoside, the active parts also contain some anti-inflammatory and analgesic activity compounds like flavones and organic acid. In view of the effective substances of Chinese/folk medicine should being various prototype group and active metabolites group that process suitable dynamic characteristics in vivo, using the active part of Dianbaizhu as the object, and chemical components in vitro, in normal and pathological body combined pharmacokinetics and pharmacodynamics (PK/PD) as the research method, basing on the technology platform of analytical test, cell experiment and animal experiment, this project carries out the study of gastrointestinal bioconversion and absorption, constituent isolation and identification, the analysis and identification of the constituent in normal and pathological body, and the establishment of their relationship of the time-concentration-efficiency. This project aimed at clarifying anti-inflammatory and analgesic metabolites in vivo and prototype in vitro and their change law, and further speculate the mechanism of action. Otherwise, establishing the multidimensional spectrum of active part fingerprint, dose-effect fingerprint and drug metabolism fingerprint, in order to control quality of Dianbaizhu and guide rational use of drugs.