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TCMs' efficacy theory effective forms additive effects on a

發(fā)布時間:2016-10-30 13:47

  本文關(guān)鍵詞:中藥“顯效理論”或有助于闡釋并弘揚(yáng)中藥特色優(yōu)勢,由筆耕文化傳播整理發(fā)布。


中藥“顯效理論”或有助于闡釋并弘揚(yáng)中藥特色優(yōu)勢

“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]北京大學(xué)藥學(xué)院生物學(xué)研究室,北京100191; [2]北京大學(xué)藥學(xué)院化學(xué)生物學(xué)系,北京100191

文章摘要該文歸納出中藥"顯效理論",即中藥通過"眾多顯效形式(顯效型)的單靶點(diǎn)疊加作用、多靶點(diǎn)協(xié)同作用及毒性分散效應(yīng)"發(fā)揮藥效并削弱自身毒性。一味中藥可含有約1 000種成分,一種成分口服進(jìn)入體內(nèi)后又可產(chǎn)生約100種代謝產(chǎn)物。無數(shù)化學(xué)成分及其無數(shù)體內(nèi)代謝產(chǎn)物中的眾多顯效形式可共同發(fā)揮"集團(tuán)軍式作用"。在藥物分子少、靶點(diǎn)分子多的情況下,中藥不同種的顯效型分子可相繼與靶點(diǎn)分子結(jié)合,發(fā)生疊加作用,當(dāng)"靶點(diǎn)充分占位"時藥效始啟動。既有濃度上的疊加作用又有時間段先后的疊加作用,這使得藥效得以持久。顯效型呈現(xiàn)藥效疊加和毒性分散,源于不同顯效形式分子結(jié)構(gòu)之間藥效基團(tuán)相同而毒性基團(tuán)不完全相同。"毒性分散效應(yīng)"適于對無毒中藥而不適于對有毒中藥的解釋。顯效理論揭示中藥可以眾多化學(xué)成分及眾多代謝產(chǎn)物參與發(fā)揮藥效過程,包括疊加作用、協(xié)同作用及毒性分散效應(yīng),可有助于闡釋和弘揚(yáng)中藥特色優(yōu)勢。今后需研究/確證的問題:中藥藥效物質(zhì)基礎(chǔ)及其作用機(jī)制是怎樣構(gòu)成的?多數(shù)中藥為什么毒性?體現(xiàn)中藥特色優(yōu)勢的中藥"顯效理論"如何在新藥研發(fā)中應(yīng)用?

AbstrThis 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

文章關(guān)鍵詞:

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

課題項(xiàng)目:國家九五攀登計劃項(xiàng)目(1998); 國家973項(xiàng)目(G1999054406); 國家自然科學(xué)基金杰出青年基金項(xiàng)目(30425018);國家自然科學(xué)基金重點(diǎn)項(xiàng)目(30830120);國家自然科學(xué)基金面上項(xiàng)目(81274073,81274074); 國家“重大新藥創(chuàng)制”科技重大專項(xiàng)(2013ZX09103002006,2013ZX09508104)

作者信息:會員可見

 

 


  本文關(guān)鍵詞:中藥“顯效理論”或有助于闡釋并弘揚(yáng)中藥特色優(yōu)勢,,由筆耕文化傳播整理發(fā)布。



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