Peptide‐Coated Platinum Nanoparticles with Selective Toxicity against Liver Cancer Cells

Peptide‐stabilized platinum nanoparticles (PtNPs) were developed that have significantly greater toxicity against hepatic cancer cells (HepG2) than against other cancer cells and non‐cancerous liver cells. The peptide H‐Lys‐Pro‐Gly‐d Lys‐NH₂ was identified by a combinatorial screening and further optimized to enable the formation of water‐soluble, monodisperse PtNPs with average diameters of 2.5 nm that are stable for years. In comparison to cisplatin, the peptide‐coated PtNPs are not only more toxic against hepatic cancer cells but have a significantly higher tumor cell selectivity. Cell viability and uptake studies revealed that high cellular uptake and an oxidative environment are key for the selective cytotoxicity of the peptide‐coated PtNPs.     

Cover Picture: Angew. Chem. Int. Ed. 15/2002

The cover picture shows the interior of a red‐figure kylix (440–430 BC, British Museum London) which shows the brilliant exploits of Theseus, the Greek mythology hero. In the center, Theseus is shown defeating the infamous Minataur within the labyrinth. On the right, the hero raises his hand against Sciron, below whom the turtle is visible. Next clockwise, are shown the bull of Marathon, the punishment of Sinis, the slaying of the sow Phaea, the battle of Cercyon, and finally the punishment of Procrustes. The labors of Theseus are no different from the accomplishments of today's synthetic chemists working in total synthesis. One such endeavor, the total synthesis of the CP molecules with its challenges, twists and turns, and dead‐ends, but also its rewards, is compared to the conquest of the Minotaur by Theseus in the Review by K. C. Nicolaou and P. S. Baran on p. 2678 ff.