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A Carrier-Free Nanostructure Based on Platinum(IV) Prodrug Enhances Cellular Uptake and Cytotoxicity.

ABSTRACT: Flurbiprofen, a hydrophobic COX inhibitor, was coordinated axially with oxoplatin to form a new conjugate, cis, cis, trans-[Pt(IV)(NH3)2Cl2(flurbiprofen)2]. The successful synthesis of this new conjugate was confirmed by 1H, 13C, and 195Pt NMR. The potential of this conjugate being reduced to cisplatin and subsequently exerting its DNA cross-linking ability was verified using cyclic voltammetry (CV), HPLC, and mass spectrometry (MS). This conjugate showed markedly higher cytotoxicity on many cancer cell lines than cisplatin, flurbiprofen, and their physical mixture (mole ratio, cisplatin:flurbiprofen = 1:2). This is consistent with the result of an apoptosis-inducing assay. This conjugate spontaneously assembles carrier-free nanoparticles in aqueous solution, which is confirmed by DLS, TEM, SEM, and AFM, and thus facilitates cellular uptake and markedly improves its cytotoxicity and apoptosis-inducing ability in vitro.

SUBMITTER: Tan J 

PROVIDER: S-EPMC7057395 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature

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A Carrier-Free Nanostructure Based on Platinum(IV) Prodrug Enhances Cellular Uptake and Cytotoxicity.

Tan Jingjie J   Li Chan C   Wang Qian Q   Li Shuyi S   Chen Shizhu S   Zhang Jinchao J   Wang Paul C PC   Ren Lei L   Liang Xing-Jie XJ  

Molecular pharmaceutics 20180314 4

Flurbiprofen, a hydrophobic COX inhibitor, was coordinated axially with oxoplatin to form a new conjugate, cis, cis, trans-[Pt(IV)(NH<sub>3</sub>)<sub>2</sub>Cl<sub>2</sub>(flurbiprofen)<sub>2</sub>]. The successful synthesis of this new conjugate was confirmed by <sup>1</sup>H, <sup>13</sup>C, and <sup>195</sup>Pt NMR. The potential of this conjugate being reduced to cisplatin and subsequently exerting its DNA cross-linking ability was verified using cyclic voltammetry (CV), HPLC, and mass spec  ...[more]

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