Department of Biomedical Engineering, Manipal Institute of Technology, Manipal Academy of Higher Education, Manipal, 576 104, India.
Department of Chemistry, Manipal Institute of Technology, Manipal Academy of Higher Education, Manipal, 576 104, India.
Eur J Med Chem. 2019 Sep 1;177:76-104. doi: 10.1016/j.ejmech.2019.04.058. Epub 2019 May 14.
Curcumin is a pharmacologically active polyphenol derived from the popular spice element-Turmeric. The therapeutic activity of curcumin has been extensively investigated over the last few decades and reports suggest the role of curcumin in a large number of biological activities, particularly its prominent anticancer activity. Curcumin, being a pleiotropic molecule, is a regulator of multiple molecular targets which play crucial roles in various cell signaling pathways. It is known to suppress transformation, inhibit proliferation as well as induce apoptosis. However, despite all these benefits, the efficacy of curcumin remains limited due to its poor bioavailability, poor absorption within the systemic circulation and rapid elimination from the body. To overcome these limiting factors, researchers all around the world are working towards designing a synthetic and superior curcuminoid by making suitable structural modifications to the parent skeleton. These curcuminoids, mainly analogues and derivatives, will not only improve the physicochemical properties but also enhance the efficacy simultaneously. The present review will provide a comprehensive account of the analogues and derivatives of curcumin that have been reported since 2014 which have indicated a better anticancer activity than curcumin.
姜黄素是一种从常用香料姜黄中提取的具有药理活性的多酚。在过去几十年中,人们对姜黄素的治疗活性进行了广泛的研究,报告表明姜黄素在许多生物活性中发挥作用,特别是其突出的抗癌活性。姜黄素作为一种多效分子,是多种分子靶点的调节剂,这些靶点在各种细胞信号通路中发挥着关键作用。它被认为能抑制转化、抑制增殖并诱导细胞凋亡。然而,尽管有这些益处,由于其生物利用度低、在全身循环中的吸收不良以及在体内迅速消除,姜黄素的疗效仍然有限。为了克服这些限制因素,全世界的研究人员都致力于通过对母体骨架进行适当的结构修饰来设计出一种合成的、更优越的姜黄素类似物。这些姜黄素类似物主要是类似物和衍生物,不仅可以改善物理化学性质,还可以同时提高疗效。本综述将全面介绍自 2014 年以来报道的姜黄素类似物和衍生物,它们显示出比姜黄素更好的抗癌活性。