TCMs＇ efficacy theory effective forms additive effects on a

  本文关键词：中药“显效理论”或有助于阐释并弘扬中药特色优势，由笔耕文化传播整理发布。

中药“显效理论”或有助于阐释并弘扬中药特色优势

“Efficacy Theory”may help to explain characteristic advantages of traditional Chinese medicines

[1] [2] [3] [4] [5]

CAI Shao-qing,WANG Xuan,SHANG Ming-ying,XU Feng,LIU Guang-xue （ 1. Division of Pharmacognosy, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China; 2. Depar

[1]北京大学药学院生物学研究室,北京100191; [2]北京大学药学院化学生物学系,北京100191

文章摘要：该文归纳出中药＂显效理论＂,即中药通过＂众多显效形式（显效型）的单靶点叠加作用、多靶点协同作用及毒性分散效应＂发挥药效并削弱自身毒性。一味中药可含有约1 000种成分,一种成分口服进入体内后又可产生约100种代谢产物。无数化学成分及其无数体内代谢产物中的众多显效形式可共同发挥＂集团军式作用＂。在药物分子少、靶点分子多的情况下,中药不同种的显效型分子可相继与靶点分子结合,发生叠加作用,当＂靶点充分占位＂时药效始启动。既有浓度上的叠加作用又有时间段先后的叠加作用,这使得药效得以持久。显效型呈现药效叠加和毒性分散,源于不同显效形式分子结构之间药效基团相同而毒性基团不完全相同。＂毒性分散效应＂适于对无毒中药而不适于对有毒中药的解释。显效理论揭示中药可以众多化学成分及众多代谢产物参与发挥药效过程,包括叠加作用、协同作用及毒性分散效应,可有助于阐释和弘扬中药特色优势。今后需研究/确证的问题：中药药效物质基础及其作用机制是怎样构成的？多数中药为什么毒性小？体现中药特色优势的中药＂显效理论＂如何在新药研发中应用？

Abstr：This article proposes the ″Efficacy Theory″ hypothesis of the traditional Chinese medicines（ TCMs） ： TCMs take effects and weaken toxicities through the additive effects of numerous effective forms（ including their constituents or / and metabolites） on a same target,the synergistic effects based on the overall action of the additive effects on individual targets and their toxicities scattering effects. A TCM may include approximately 1000 constituents and each constituent may produce about 100 metabolites in vivo after oral administration. Numerous effective forms of incalculable constituents and their metabolites could work like a ″army group″ together. When the quantity of a specific target molecule is larger than the pharmaceutical molecules,the molecules of different kinds of effective forms could combine with the target molecules successively,to exert the additive effects. When the target molecules are mostly occupied（ ″target most spaces occupied″）,this TCM begins to work. The additive effects maybe exert not only in concentration but also in a time order way,which gives a sustained efficacy of TCM. The additive effects and the toxicities scattering effects are resulted from the same effective groups and not identical toxic groups among different effective form molecules. The ″toxicities scattering effect″ can be used to explain the non-toxic TCMs,but not fit for toxic TCMs. The efficacy theory showed that the variety of constituents and metabolites may participate in the process of pharmacodynamic actions,including the additive effects,synergy effects and toxicities scattering effects,which may be useful for explaining and developing the characteristic advantage of the TCMs. The questions we need to study or con

文章关键词：

Keyword：:TCMs＇ efficacy theory effective forms additive effects on a same target synergistic effects among individual targets toxicities scattering effects army group actions target molecule target most spaces

课题项目：国家九五攀登计划项目（1998）; 国家973项目（G1999054406）; 国家自然科学基金杰出青年基金项目（30425018）;国家自然科学基金重点项目（30830120）;国家自然科学基金面上项目（81274073,81274074）; 国家“重大新药创制”科技重大专项（2013ZX09103002006,2013ZX09508104）

作者信息：会员可见

  本文关键词：中药“显效理论”或有助于阐释并弘扬中药特色优势，，由笔耕文化传播整理发布。