【作者】 徐晶晶； 尚明英； 徐风； 王璇； 蔡少青；

【Author】 Xu Jing-jing;Shang Ming-ying;Xu Feng;Wang Xuan;Cai Shao-qing;Division of Pharmacognosy,School of Pharmaceutical Sciences,Peking University;Department of Chemical Biology,School of Pharmaceutical Sciences,Peking University;

【机构】 北京大学药学院生物学研究室； 北京大学药学院化学生物学系；

【摘要】 目的:血药浓度可间接地反映药物在受体部位的浓度,一定程度上决定了药物效应的发挥。中药入血成分(包括中药化学成分原形及其代谢产物)的血药浓度很低。中药中单一的低浓度入血成分是否有发挥药效的可能性?中药中大量的低浓度入血成分与药效间有什么样的关系?为此本文调研了临床常用中药及化学药的血药浓度并对其进行了比较分析,以推测中药单一成分在相应血药浓度下发挥药效的可能性,在此基础上探讨中药的作用机制。方法:通过检索Scifinder、CNKI等中英文数据库,对2006～2016年间的72篇文献进行整理汇总,对常规剂量下中药化学成分的最大血药浓度和临床常用化学药的最小有效血药浓度进行了比较分析。结果:对总结得到的73种常用化学药最小有效血药浓度及42种中药(复方)中135个化学成分最大血药浓度比较后,发现最大血药浓度小于100ng/ml的中药化学成分(代谢产物)共88个(占总数的65%),化学药共15个(占总数的21%);33个(占总数的45%)化学药最小有效血药浓度分布在较高的浓度区间(1000-100000ng/ml),而中药化学成分只有8个(占总数的5%);即随着血药浓度由低到高,化学药数量呈由少到多的变化,中药化学成分(原形/代谢产物)数量则由多到少。结论:所列中药化学成分最大血药浓度总体分布低于化学药最小有效血药浓度,推知中药起效时体内各化学成分实际血药浓度可能比化学药最小有效血药浓度更低。中药体内(大多数)单一化学成分激动相关靶点并引起相应药理效应的可能性较小。推测作用于相同靶点的所有化学成分浓度的叠加可能是中药产生药理作用的机制之一。更多还原

【Abstract】 Objective: Blood concentration can indirectly reflect the target concentration and to a certain extent, can determine the drug effect. The blood concentration of components of Chinese medicine is very low. Can these constituents with low blood concentration exert pharmacological actions? And what is the relationship between these components and the efficiency? To answer these questions, we investigated the the blood concentration of the common pharmaceutical chemicals and Chinese medicine to infer whether single component of Chinese medicine can exert effect under the corresponding blood concentration and explore the mechanism. Method: After researching scifinder、CNKI, 72 papers during 2006-2016 were collected and analyzed. Result: It was found that the maximum blood concentration of the 88 components of Chinese medicine(65% of total) and the minimum effective blood concentration of 15 pharmaceutical chemicals(21% of total) were less than 100 ng/ml; the minimum effective blood concentration of 33 pharmaceutical chemicals(45% of total) and the maximum blood concentration of the 8 components of Chinese medicine(5% of total) distributed in 1000-100000 ng/ml. Therefore most Chinese medicine components were lower than the minimum effective blood concentration of pharmaceutical chemicals. Conclusion: The possibility that single component of Chinese medicine can affect target is very small. Additive Effect is likely to be one of the mechanism of Chinese medicine.更多还原