Binding and Anticancer Properties of Plumbagin with Human Serum Albumin
Binding and Anticancer Properties of Plumbagin with Human Serum Albumin
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DOI：
10.1111/cbdd.12501
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发表时间：
2015-09
影响因子：
3
通讯作者：
Y. Gou;Yao Zhang;J. Qi;Linlin Kong;Zuping Zhou;Shichu Liang;Feng Yang;Hong Liang
中科院分区：
文献类型：
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作者：
Y. Gou;Yao Zhang;J. Qi;Linlin Kong;Zuping Zhou;Shichu Liang;Feng Yang;Hong Liang
白花丹因作为一种很有前途的抗癌药物受到了广泛的关注。因此，我们研究了白藜芦素与人血清白蛋白的结合及抗癌作用。荧光结果表明，尽管不同的化合物对白蛋白的结合亲和力有不同程度的影响，但白花蛇毒与人血清白蛋白相互作用。人血清白蛋白-白蛋白-白蛋白复合体结构表明，白蛋白通过氢键和疏水相互作用与人血清白蛋白IIA亚区的疏水空腔结合。白花蛇舌草素-人血清白蛋白复合体将细胞毒性提高2-3倍，特别是在癌细胞中，但在体外对正常细胞没有影响。与未结合药物相比，人血清白蛋白-白蛋白复合体促进HeLa细胞凋亡，并具有更强的细胞周期阻滞能力。综上所述，本研究有助于合理设计和开发基于白蛋白的药物和药物-人血清白蛋白给药系统。
Plumbagin has received extensive attention as a promising anticancer drug. Therefore, we investigated the binding and anticancer properties of plumbagin with human serum albumin. Fluorescence results demonstrated that plumbagin interacts with human serum albumin, although its binding affinity may be affected to various extents by different compounds. The human serum albumin–plumbagin complex structure revealed that plumbagin binds to the hydrophobic cavity in the IIA subdomain of human serum albumin through hydrogen bonding and hydrophobic interactions. The plumbagin–human serum albumin complex enhances cytotoxicity by 2‐ to 3‐fold particularly in cancer cells but has no effect on normal cells in vitro. Compared with the unbound drug, the human serum albumin–plumbagin complex promotes HeLa cell apoptosis and has a stronger capacity for cell cycle arrest at the G2/M phase of HeLa cells. In conclusion, this study contributes to the rational design and development of plumbagin‐based drugs and a drug–human serum albumin delivery system.