姜黃素類化合物具有明確而廣泛的藥理作用,但因其溶解度差、結(jié)構(gòu)不穩(wěn)定,生物利用度極低。主要通過(guò)對(duì)姜黃素類化合物體內(nèi)代謝途徑及其相關(guān)代謝產(chǎn)物進(jìn)行綜述,以明確姜黃素生物利用度低的原因,并提出姜黃素發(fā)揮藥理活性的物質(zhì)基礎(chǔ)可能與其通過(guò)自身氧化和催化氧化過(guò)程產(chǎn)生的雙環(huán)乙酰丙酮結(jié)構(gòu)有關(guān)。因此對(duì)姜黃素代謝產(chǎn)物進(jìn)行藥動(dòng)學(xué)及相關(guān)藥效研究,能夠?yàn)榕R床應(yīng)用提供更為關(guān)鍵的基礎(chǔ)性數(shù)據(jù),也具有更為重要的研究?jī)r(jià)值。

Curcuminoids have clear and extensive pharmacological effects. However, curcumin has very low bioavailability because of its poor solubility and unstable structure. The metabolic pathways in vivo and their metabolites of curcuminoids are mainly reviewed in this paper, in order to make clear the reason of low bioavailability. Besides, it is inferred that the structure of bicyclopentadiones by autoxidation and catalytic oxygenation plays an important role of the material basis for the pharmacological activities of curcumin. Therefore, the pharmacokinetics and pharmacodynamics research of curcumin metabolites can provide more key foundational data for clinical application, and has more important research value.

國(guó)家自然科學(xué)基金重點(diǎn)項(xiàng)目(81430096);重大新藥創(chuàng)制科技重大專項(xiàng)(2012ZX09303010)