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.

中文翻译：

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基于Platinum（IV）前药的无载体纳米结构可增强细胞摄取和细胞毒性。

疏水性COX抑制剂氟比洛芬与氧铂轴向配位形成新的结合物，顺式，顺式，反式-[Pt（IV）（NH3）2Cl2（氟比洛芬）2]。1H，13C和195Pt NMR证实了这种新偶联物的成功合成。使用循环伏安法（CV），HPLC和质谱（MS）验证了该缀合物被还原为顺铂并随后发挥其DNA交联能力的潜力。该缀合物在许多癌细胞系中显示出比顺铂，氟比洛芬及其物理混合物明显更高的细胞毒性（摩尔比，顺铂：氟比洛芬= 1：2）。这与细胞凋亡诱导测定的结果一致。这种缀合物可在水溶液中自发组装无载体的纳米颗粒，这经DLS，TEM，SEM和AFM证实，