Department of Chemistry, University of Adelaide, Adelaide, South Australia, 5005, Australia.
Curr Pharm Des. 2013;19(11):2070-83. doi: 10.2174/138161213805289237.
Curcumin, a yellow pigment extracted from the rhizome of Curcuma longa, commonly known as turmeric, is the most active agent of this herbal medicine. The therapeutic activities of curcumin are exemplified not only by its enhancement in wound healing but also in the treatment of inflammation, cystic fibrosis, Alzheimer's disease and cancer. There are two critical issues involving low aqueous stability and solubility that limit the bioavailability and application of curcumin as a therapeutic agent. To address these issues, delivery systems of curcumin including surfactant micelles, liposomes, polymer nanoparticles, casein micelles, plasma proteins and cyclodextrins have been developed and characterized. From a biochemical perspective, the medicinal activities of curcumin are proposed to be related to an elevated level of transition metals including copper, zinc and iron in many disease sites, especially those in cancer and Alzheimer's disease. Previous studies have demonstrated the importance of copper(II)-curcumin complexes in DNA damage owing to the strong interaction between curcumin and copper(II). Curcumin, as an anti-oxidant, possesses the abilities to scavenge radicals and maintain the levels of anti-oxidant enzymes in the presence of copper. On the other hand, copper(II)-curcumin complexes show pro-oxidant effects by generating reactive oxygen species at a high free copper level in a reducing environment. This condition results in DNA damage and inhibition of vital signaling pathways in cancer cells, leading to apoptosis. In short, curcumin has dual roles as an anti-oxidant and a prooxidant in the presence of copper and these fascinating phenomena contribute greatly to its multiple medicinal effects.
姜黄素是从姜黄根茎中提取的一种黄色色素,通常被称为 turmeric,是这种草药中最活跃的成分。姜黄素的治疗活性不仅体现在其对伤口愈合的增强作用上,还体现在对炎症、囊性纤维化、阿尔茨海默病和癌症的治疗作用上。有两个关键问题涉及低水稳定性和溶解度,限制了姜黄素作为治疗剂的生物利用度和应用。为了解决这些问题,已经开发和表征了包括表面活性剂胶束、脂质体、聚合物纳米粒子、酪蛋白胶束、血浆蛋白和环糊精在内的姜黄素传递系统。从生化角度来看,姜黄素的药用活性被认为与许多疾病部位(特别是癌症和阿尔茨海默病)中过渡金属(包括铜、锌和铁)水平升高有关。先前的研究表明,铜(II)-姜黄素配合物在 DNA 损伤中的重要性,这是由于姜黄素与铜(II)之间的强相互作用。作为一种抗氧化剂,姜黄素有清除自由基和在存在铜的情况下维持抗氧化酶水平的能力。另一方面,铜(II)-姜黄素配合物在还原环境中具有高游离铜水平时会产生活性氧,表现出促氧化剂效应。这种情况会导致 DNA 损伤,并抑制癌细胞中重要的信号通路,导致细胞凋亡。简而言之,姜黄素在铜存在下具有抗氧化剂和促氧化剂的双重作用,这些迷人的现象极大地促进了其多种药用效果。