Discovery of a new function of curcumin which enhances its anticancer therapeutic potency.
Discovery of a new function of curcumin which enhances its anticancer therapeutic potency.
复制标题
DOI：
10.1038/srep30962
复制
发表时间：
2016-08-01
影响因子：
4.6
通讯作者：
Kawakami J
中科院分区：
文献类型：
--
作者：
Nagahama K;Utsumi T;Kumano T;Maekawa S;Oyama N;Kawakami J
姜黄素因其丰富的生物活性，被认为是治疗多种疾病的有前途的候选药物，在过去的几十年里受到了广泛的关注。然而，由于其极低的水溶性、化学稳定性和细胞摄取，其临床应用一直受到阻碍。在这项研究中，我们发现了姜黄素的一种新的功能，即ph响应性内体破坏活性，源于姜黄素的自组装。以姜黄素的抗癌活性为例，探讨了ph响应特性对其抗癌活性的影响。结果表明，姜黄素的ph响应特性显著增强了姜黄素的抗癌活性。此外，我们证明了姜黄素作为阿霉素纳米载体用于联合癌症治疗的ph响应特性的效用。这些结果清楚地表明，智能姜黄素组装体作为开发基于姜黄素的治疗药物的有前途的纳米平台。
Curcumin has received immense attention over the past decades because of its diverse biological activities and recognized as a promising drug candidate in a large number of diseases. However, its clinical application has been hindered due to extremely low aqueous solubility, chemical stability, and cellular uptake. In this study, we discovered quite a new function of curcumin, i.e. pH-responsive endosomal disrupting activity, derived from curcumin’s self-assembly. We selected anticancer activity as an example of biological activities of curcumin, and investigated the contribution of pH-responsive property to its anticancer activity. As a result, we demonstrated that the pH-responsive property significantly enhances the anticancer activity of curcumin. Furthermore, we demonstrated a utility of the pH-responsive property of curcumin as delivery nanocarriers for doxorubicin toward combination cancer therapy. These results clearly indicate that the smart curcumin assemblies act as promising nanoplatform for development of curcumin-based therapeutics.