目前绝大多数中药的药效物质基础尚不清楚，这不利于中药疗效的提高，也不利于其作为现代药物获得国际普遍认可。中药多为复方，化学组成十分复杂，建立一套切实可行研究复方中药药效物质基础的方法是当前亟待解决的问题。本项申请拟以有效中药“复方丹参方”为研究选药，着重从三方面研究该中药在人体内的暴露物质与其抗心绞痛作用的关联性：（1）研究复方丹参方全方制剂给药后在人体内的物质暴露、药动学特征和能否达到靶标受体、以及影响暴露的药代因素；（2）多指标研究复方丹参方体内暴露物质的抗心绞痛药理活性和起效浓度、以及药代因素对其药理活性的影响；（3）研究复方丹参方体内暴露物质间会否发生药代机制相互作用，能否在“药效协同或叠加”的同时保持“药代和谐”并共同构成复方的药效物质基础。该项研究将探索出一套具有较好普适性的研究中药药效物质基础方法，揭示复方丹参方的药效物质基础。

For vast majority of Chinese herbal medicines, the chemical basis responsible for their therapeutic actions is not clear. This impedes the optimization of herbal therapies and their global acceptance as modern drug products. Chinese herbal medicines are often prepared from combination of multiple herbs with very complex chemical composition. It is important to establish a methodology for identification of chemical basis responsible for therapeutic actions of an herbal medicine. The current application is designed to investigate human exposure to compounds from dosed Fufang-Danshen formula, a three-herb combination medicine, and its correlation with the medicine’s antianginal properties from the following three aspects: (1) human systemic exposure to and pharmacokinetics of unchanged and metabolized herbal compounds after oral administration of Fufang-Danshen formulations and factors that can influence exposure to the herbal compounds after dosing, (2) antianginal activities of circulating herbal compounds from the dosed Fufang-Danshen formulations and the compounds’ effective concentrations and influences of pharmacokinetic factors on the compounds in exerting their antianginal activities, and (3) propensity for untoward pharmacokinetic interactions among circulating herbal compounds from dosed Fufang-Danshen formulations. The proposed study will explore an efficient methodology for identification of chemical basis responsible for therapeutic actions of an herbal medicine and will identify the chemical basis responsible for antianginal actions of Fufang-Danshen formula.