China-Japan Union Hospital of Jilin University, Changchun, P R China.
Macromol Biosci. 2013 Jul;13(7):954-65. doi: 10.1002/mabi.201300057. Epub 2013 Jun 6.
A core cross-linked polymeric micellar cisplatin(IV) conjugate prodrug is prepared by attaching the cisplatin(IV) to mPEG-b-PLL biodegradable copolymers to form micellar nanoparticles that can disintegrate to release the active anticancer agent cisplatin(II) in a mild reducing environment. Moreover, in vitro studies show that this cisplatin(IV) conjugate prodrug displays enhanced cytotoxicity against HepG2 cancer cells compared with cisplatin(II). Further studies demonstrate that the high cellular uptake and platinum-DNA adduct of this cisplatin(IV) conjugate prodrug can induce more cancer-cell apoptosis than cisplatin(II), which is responsible for its enhanced anticancer activity.
一种核心交联聚合物胶束顺铂（IV）偶联前药是通过将顺铂（IV）连接到 mPEG-b-PLL 可生物降解共聚物上制备的，形成胶束纳米颗粒，在温和的还原环境中可以分解释放出活性抗癌剂顺铂（II）。此外，体外研究表明，与顺铂（II）相比，这种顺铂（IV）偶联前药对 HepG2 癌细胞具有增强的细胞毒性。进一步的研究表明，这种顺铂（IV）偶联前药的高细胞摄取率和铂-DNA 加合物可以诱导比顺铂（II）更多的癌细胞凋亡，这是其增强抗癌活性的原因。
