The Essential Medicinal Chemistry of Curcumin.
The Essential Medicinal Chemistry of Curcumin.
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DOI：
10.1021/acs.jmedchem.6b00975
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发表时间：
2017-03-09
影响因子：
7.3
通讯作者：
Walters MA
中科院分区：
文献类型：
--
作者：
Nelson KM;Dahlin JL;Bisson J;Graham J;Pauli GF;Walters MA
姜黄素是传统药物姜黄的一种成分（高达约5%）。对姜黄的治疗用途和相对容易分离的姜黄素的兴趣导致了它们的广泛研究。姜黄素最近被列为泛分析干扰化合物（PAINS）和无效代谢万灵药（IMPS）候选药物。姜黄素在体内和体外可能存在的假活性导致了姜黄素治疗多种疾病的120多项临床试验。目前尚无双盲、安慰剂对照的姜黄素临床试验取得成功。这篇文章回顾了姜黄素的基本药物化学，并提供证据表明姜黄素是一种不稳定的，活性的，非生物利用的化合物，因此，一个非常不可能的线索。在此基础上，展望了姜黄素研究的新方向。
Curcumin is a constituent (up to ∼5%) of the traditional medicine known as turmeric. Interest in the therapeutic use of turmeric and the relative ease of isolation of curcuminoids has led to their extensive investigation. Curcumin has recently been classified as both a PAINS (pan-assay interference compounds) and an IMPS (invalid metabolic panaceas) candidate. The likely false activity of curcumin in vitro and in vivo has resulted in >120 clinical trials of curcuminoids against several diseases. No double-blinded, placebo controlled clinical trial of curcumin has been successful. This manuscript reviews the essential medicinal chemistry of curcumin and provides evidence that curcumin is an unstable, reactive, nonbioavailable compound and, therefore, a highly improbable lead. On the basis of this in-depth evaluation, potential new directions for research on curcuminoids are discussed.