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“功效理论”或许有助于解释中药的特色优势。

["Efficacy Theory" may help to explain characteristic advantages of traditional Chinese medicines].

作者信息

Cai Shao-qing, Wang Xuan, Shang Ming-ying, Xu Feng, Liu Guang-xue

出版信息

Zhongguo Zhong Yao Za Zhi. 2015 Sep;40(17):3435-43.

Abstract

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 confirm are as follows: What are the TCMs' pharmacodynamic substance basis and mechanism made up of Why are toxicities of most TCMs' smaller How is the TCMs' "Efficacy Theory" which reflects characteristic advantage of TCMs applied in the research and development of new drugs.

摘要

本文提出了中药“功效理论”假说:中药通过众多有效形式(包括其成分或/和代谢产物)对同一靶点的加和作用、基于对各个靶点加和作用的整体作用的协同作用以及毒性分散作用来发挥药效并减弱毒性。一味中药可能含有约1000种成分,每种成分口服后在体内可能产生约100种代谢产物。无数难以计数的成分及其代谢产物的有效形式可像“集团军”一样协同作用。当特定靶点分子数量多于药物分子时,不同种类有效形式的分子可依次与靶点分子结合,发挥加和作用。当靶点分子大多被占据(“靶点空间大多被占据”)时,该中药开始起效。加和作用不仅可按浓度发挥,还可按时间顺序发挥,这赋予了中药持续的药效。加和作用和毒性分散作用源于不同有效形式分子中相同的有效基团而非相同的毒性基团。“毒性分散作用”可用于解释无毒中药,但不适用于有毒中药。功效理论表明,成分和代谢产物的多样性可能参与药效作用过程,包括加和作用、协同作用和毒性分散作用,这可能有助于解释和发挥中药的特色优势。我们需要研究或确认的问题如下:中药的药效物质基础和作用机制由什么构成?为何大多数中药的毒性较小?体现中药特色优势的中药“功效理论”如何应用于新药研发。

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