Department of Inorganic and Physical Chemistry, Indian Institute of Science, Bangalore 560012, Karnataka (India).
Department of Molecular Reproduction, Development and Genetics, Indian Institute of Science, Bangalore 560012, Karnataka (India).
Angew Chem Int Ed Engl. 2015 Nov 16;54(47):13989-93. doi: 10.1002/anie.201507281. Epub 2015 Sep 30.
Pt(cur)(NH3)2 (1), a curcumin-bound cis-diammineplatinum(II) complex, nicknamed Platicur, as a novel photoactivated chemotherapeutic agent releases photoactive curcumin and an active platinum(II) species upon irradiation with visible light. The hydrolytic instability of free curcumin reduces upon binding to platinum(II). Interactions of 1 with 5'-GMP and ct-DNA indicated formation of platinum-bound DNA adducts upon exposure to visible light (λ=400-700 nm). It showed apoptotic photocytotoxicity in cancer cells (IC50 ≈ 15 μM), thus forming (⋅)OH, while remaining passive in the darkness (IC50 >200 μM). A comet assay and platinum estimation suggest Pt-DNA crosslink formation. The fluorescence microscopic images showed cytosolic localization of curcumin, thus implying possibility of dual action as a chemo- and phototherapeutic agent.
Pt(cur)(NH3)2 (1)，一种姜黄素结合的顺式二氨二氯铂(II)配合物，名为 Platicur，作为一种新型的光激活化疗药物，在可见光照射下释放光活性姜黄素和活性铂(II)物种。游离姜黄素的水解不稳定性在与铂(II)结合后降低。1 与 5'-GMP 和 ct-DNA 的相互作用表明，在可见光照射下（λ=400-700nm）形成铂结合的 DNA 加合物。它在癌细胞中表现出凋亡光细胞毒性（IC50≈15μM），因此形成（⋅）OH，而在黑暗中保持被动（IC50>200μM）。彗星试验和铂估计表明铂-DNA 交联形成。荧光显微镜图像显示姜黄素的细胞质定位，因此暗示其作为化疗和光疗药物的双重作用的可能性。
