Bisht Savita, Maitra Anirban
Department of Pathology, The Sol Goldman Pancreatic Cancer Research Center, Johns Hopkins University School of Medicine, Baltimore, MD 21231, USA.
Curr Drug Discov Technol. 2009 Sep;6(3):192-9. doi: 10.2174/157016309789054933. Epub 2009 Sep 1.
Curcumin, a polyphenolic compound derived from the dietary spice turmeric, possesses diverse pharmacologic effects including anti-inflammatory, anti-oxidant, anti-proliferative and anti-angiogenic activities. Accumulating experimental evidence suggests that curcumin interferes with a variety of molecular targets and processes involved in cancer. Further, data obtained in multiple preclinical models, as well as in preliminary clinical trials, have documented minimal toxicity of curcumin, even at relatively high doses. However, the clinical advancement of this promising molecule has been hindered by its poor water solubility, short biological half-life, and low bioavailability after oral administration. A variety of approaches are being pursued to overcome these limitations, which include synthesis of curcumin analogues, the use of adjuvants (e.g. piperine), and the development of improved delivery platforms for the parental compound, including liposomal, nanoparticulated and phospholipid complex formulations of curcumin. This review is intended to provide the reader an update on the bioavailability and pharmacokinetic pitfalls of free curcumin, and a comprehensive cataloging of ongoing approaches that have been undertaken to resolve these issues, with the goal of harnessing the true potential of this anti-cancer agent in the clinical arena.
姜黄素是一种从食用香料姜黄中提取的多酚类化合物，具有多种药理作用，包括抗炎、抗氧化、抗增殖和抗血管生成活性。越来越多的实验证据表明，姜黄素会干扰癌症相关的多种分子靶点和过程。此外，在多个临床前模型以及初步临床试验中获得的数据表明，即使在相对高剂量下，姜黄素的毒性也极小。然而，这种有前景的分子的临床进展受到其水溶性差、生物半衰期短以及口服给药后生物利用度低的阻碍。人们正在采用多种方法来克服这些限制，包括合成姜黄素类似物、使用佐剂（如胡椒碱）以及开发改进的母体化合物递送平台，包括姜黄素的脂质体、纳米颗粒和磷脂复合物制剂。这篇综述旨在向读者提供关于游离姜黄素生物利用度和药代动力学缺陷的最新信息，以及为解决这些问题而正在采取的现有方法的全面编目，目标是在临床领域发挥这种抗癌药物的真正潜力。
