Department of Chemistry, University of Fort Hare, Alice Campus, Alice 5700, Eastern Cape, South Africa.
Molecules. 2019 Nov 30;24(23):4386. doi: 10.3390/molecules24234386.
Cancer is a life-threatening disease and is the second leading cause of death around the world. The increasing threats of drug-resistant cancers indicate that there is an urgent need for the improvement or development of more effective anticancer agents. Curcumin, a phenolic compound originally derived from turmeric plant ( L. (Zingiberaceae family)) widely known as a spice and a coloring agent for food have been reported to possess notable anticancer activity by inhibiting the proliferation and metastasis, and enhancing cell cycle arrest or apoptosis in various cancer cells. In spite of all these benefits, the therapeutic application of curcumin in clinical medicine and its bioavailability are still limited due to its poor absorption and rapid metabolism. Structural modification of curcumin through the synthesis of curcumin-based derivatives is a potential approach to overcome the above limitations. Curcumin derivatives can overcome the disadvantages of curcumin while enhancing the overall efficacy and hindering drug resistance. This article reports a review of published curcumin derivatives and their enhanced anticancer activities.
癌症是一种危及生命的疾病,是全球第二大致死原因。癌症耐药性的威胁日益增加,表明迫切需要改进或开发更有效的抗癌药物。姜黄素是一种酚类化合物,最初来源于姜黄植物(姜科),作为一种香料和食品着色剂广为人知,据报道,它具有显著的抗癌活性,可抑制增殖和转移,并在各种癌细胞中增强细胞周期停滞或凋亡。尽管有这些好处,但由于其吸收不良和快速代谢,姜黄素在临床医学中的治疗应用及其生物利用度仍然受到限制。通过合成姜黄素类衍生物对姜黄素进行结构修饰是克服上述限制的一种潜在方法。姜黄素衍生物可以克服姜黄素的缺点,同时提高整体疗效,阻止耐药性的产生。本文综述了已发表的姜黄素衍生物及其增强的抗癌活性。