靛玉红是当归龙回湾和清代的重要成分,用于治疗慢性粒细胞白血病的中药方剂在中国已有数百年的历史。尽管在中国已将单体靛玉红用于治疗人类慢性粒细胞白血病。然而,由于水溶性低,不良的药代动力学特性和低的治疗效果是主要障碍,严重限制了其临床应用。因此,靛玉红的有吸引力的抗癌概况使许多研究人员发现了具有改善的药效学活性以及良好的药代动力学性质的新型靛玉红衍生物。在本文中,我们全面回顾了靛蓝抗癌潜力的最新进展,结构修饰和构效关系,这可能为进一步开发具有用于治疗各种类型的癌症的改善的药理学谱的新型靛蓝素类提供有用的方向。
Indirubin is the crucial ingredient of Danggui Longhui Wan and Qing-Dai, traditional Chinese medicine herbal formulas used for the therapy of chronic myelocytic leukemia in China for hundreds of years. Although the monomeric indirubin has been used in China for the treatment human chronic myelocytic leukemia. However, due to low water solubility, poor pharmacokinetic properties and low therapeutic effects are the major obstacle, and had significantly limited its clinical application. Consequently, the attractive anticancer profile of indirubin has enthused numerous researchers to discover novel indirubin derivatives with improved pharmacodynamic activity as well as good pharmacokinetic property. In this paper, we comprehensively review the recent progress of anticancer potential of indirubins, structural modification and structure-activity relationship, which may provide useful direction for the further development of novel indirubins with improved pharmacological profiles for the treatment of various types of cancer.