Department of Pharmaceutics, School of Pharmacy, Southwest Medical University, No. 319, Zhongshan Rd Sanduan, Luzhou, Sichuan, 646000, PR China.
Department of Pharmaceutics, School of Pharmacy, Southwest Medical University, No. 319, Zhongshan Rd Sanduan, Luzhou, Sichuan, 646000, PR China; Department of Pharmacy, The Affiliated Hospital, Southwest Medical University, No.25, Taiping Street, Luzhou, Sichuan, 646000, China.
Eur J Med Chem. 2019 Oct 15;180:524-535. doi: 10.1016/j.ejmech.2019.07.034. Epub 2019 Jul 10.
Curcumin (CU), an edible natural pigment from Curcuma Longa, has demonstrated extensive anti-tumor effect in vivo and in vitro. With the property of reversing drug resistance and low toxicity, CU has been considered to develop a new adjuvant chemotherapy protocol of cancer. However, the poor stability, solubility, in vivo bioavailability and weak activity of CU greatly limit its clinical application. Therefore, CU analogues have been extensively studied. Starting from the study of natural CU analogues, multiple approaches are being sought to obtain more stable, soluble and effective analogues of CU. This review focuses on the progress of these approaches to more potent CU analogues.
姜黄素(CU)是从姜黄中提取的一种可食用天然色素,已在体内和体外显示出广泛的抗肿瘤作用。CU 具有逆转耐药性和低毒性的特性,已被认为是开发癌症新辅助化疗方案的药物。然而,CU 的稳定性差、溶解度低、体内生物利用度低和活性弱极大地限制了其临床应用。因此,CU 类似物已被广泛研究。从天然 CU 类似物的研究入手,正在寻求多种方法来获得更稳定、更有效和更有效的 CU 类似物。本综述重点介绍了这些方法在获得更有效的 CU 类似物方面的进展。