Synthesis and Characterization of Nitric Oxide-Releasing Platinum(IV) Prodrug and Polymeric Micelle Triggered by Light,Bioconjugate Chemistry

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Synthesis and Characterization of Nitric Oxide-Releasing Platinum(IV) Prodrug and Polymeric Micelle Triggered by Light
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2017-12-27 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00749
Swapan Pramanick ₁ , Jihoon Kim ₂ , Jinhwan Kim ₂ , Gurusamy Saravanakumar ₂ , Dongsik Park ₁ , Won Jong Kim ₁

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Herein, we report the proof of concept of photoresponsive chemotherapeutics comprising nitric oxide-releasing platinum prodrugs and polymeric micelles. Photoactivatable nitric oxide-releasing donors were integrated into the axial positions of a platinum(IV) prodrug, and the photolabile hydrophobic groups were grafted in the block copolymers. The hydrophobic interaction between nitric oxide donors and the photolabile groups allowed for the loading of platinum drugs and nitric oxide-releasing donors in the photolabile polymeric micelles. After cellular uptake of micelles, light irradiation induced the release of nitric oxide, which sensitized the cancer cells. Simultaneously, photolabile hydrophobic groups were cleaved from micelles, and the nitric oxide-releasing donor was altered to be more hydrophilic, resulting in the rapid release of platinum(IV) prodrugs. The strategy of using platinum(IV) prodrugs and nitric oxide led to enhanced anticancer effects.

中文翻译：

一氧化氮释放铂（IV）前药和高分子胶束的合成与表征

在本文中，我们报告了包含释放一氧化氮的铂前药和聚合物胶束的光响应化学治疗概念的证明。将可光活化的释放一氧化氮的供体整合到铂（IV）前药的轴向位置，并将对光不稳定的疏水基团接枝在嵌段共聚物中。一氧化氮供体与光不稳定基团之间的疏水相互作用使铂化合物和一氧化氮释放性供体负载在光不稳定的聚合物胶束中。细胞摄取胶束后，光照射诱导释放一氧化氮，使癌细胞敏感。同时，将光不稳定的疏水基团从胶束上裂解下来，并将释放一氧化氮的供体改变为更具亲水性，导致铂（IV）前药的快速释放。使用铂（IV）前药和一氧化氮的策略导致增强的抗癌作用。

更新日期：2017-12-27

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