A Smart Europium–Ruthenium Complex as Anticancer Prodrug: Controllable Drug Release and Real-Time Monitoring under Different Light Excitations,Journal of Medicinal Chemistry

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A Smart Europium–Ruthenium Complex as Anticancer Prodrug: Controllable Drug Release and Real-Time Monitoring under Different Light Excitations
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-10-19 00:00:00 , DOI: 10.1021/acs.jmedchem.7b01162
Hongguang Li ₁ , Chen Xie ₁ , Rongfeng Lan _{1,

2} , Shuai Zha ₁ , Chi-Fai Chan ₁ , Wing-Yan Wong ₃ , Ka-Lok Ho ₁ , Brandon Dow Chan ₃ , Yuxia Luo ₁ , Jing-Xiang Zhang _{1,

4} , Ga-Lai Law ₃ , William C. S. Tai ₃ , Jean-Claude G. Bünzli _{1,

5} , Ka-Leung Wong ₁

Affiliation

A unique, dual-function, photoactivatable anticancer prodrug, RuEuL, has been tailored that features a ruthenium(II) complex linked to a cyclen–europium chelate via a π-conjugated bridge. Under irradiation at 488 nm, the dark-inactive prodrug undergoes photodissociation, releasing the DNA-damaging ruthenium species. Under evaluation-window irradiation (λ_irr = one-photon 350 nm or two-photon 700 nm), the drug delivery process can be quantitatively monitored in real-time because of the long-lived red europium emission. Linear relationships between released drug concentration and ESI-MS or luminescence responses are established. Finally, the efficiency of the new prodrug is demonstrated both in vitro RuEuL anticancer prodrug over some existing ones and open the way for decisive improvements in multipurpose prodrugs.

中文翻译：

作为抗癌前药的智能Euro-钌配合物：可控药物释放和不同光激发下的实时监测

量身定制的独特的双重功能，可光活化的抗癌药物RuEuL具有钌（II）配合物，其通过π共轭桥与周期素-che螯合物连接。在488 nm的辐射下，对黑暗无活性的前药进行光解离，释放出破坏DNA的钌物种。在评估窗口辐照下（_λirr =一光子350 nm或两光子700 nm），由于红red的寿命长，可以实时定量监测药物输送过程。建立了释放的药物浓度与ESI-MS或发光响应之间的线性关系。最后，在体外RuEuL上都证明了新前药的有效性 抗癌药物前身，为多用途前药的决定性改进开辟了道路。

更新日期：2017-10-19

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