Details

Autor(en) / Beteiligte

• Spector, Daniil V.
• Erofeev, Alexander S.
• Gorelkin, Petr V.
• Vaneev, Alexander N.
• Akasov, Roman A.
• Ul’yanovskiy, Nikolay V.
• Nikitina, Vita N.
• Semkina, Alevtina S.
• Vlasova, Kseniya Yu
• Soldatov, Mikhail A.
• Trigub, Alexander L.
• Skvortsov, Dmitry A.
• Finko, Alexander V.
• Zyk, Nikolay V.
• Sakharov, Dmitry A.
• Majouga, Alexander G.
• Beloglazkina, Elena K.
• Krasnovskaya, Olga O.

Titel

Electrochemical Detection of a Novel Pt(IV) Prodrug with the Metronidazole Axial Ligand in the Hypoxic Area

Ist Teil von

• Inorganic chemistry, 2022-09, Vol.61 (37), p.14705-14717

Ort / Verlag

American Chemical Society

Erscheinungsjahr

2022

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• We report herein a Pt­(IV) prodrug with metronidazole in axial positions Pt-Mnz. The nitroaromatic axial ligand was conjugated with a cisplatin scaffold to irreversibly reduce under hypoxic conditions, thereby retaining the Pt­(IV) prodrug in the area of hypoxia. X-ray near-edge adsorption spectroscopy (XANES) on dried drug-preincubated tumor cell samples revealed a gradual release of cisplatin from the Pt-Mnz prodrug instead of rapid intracellular degradation. The ability of the prodrug to penetrate into three-dimensional (3D) spheroid cellular cultures was evaluated by a novel electrochemical assay via a platinum-coated carbon nanoelectrode, capable of single-cell measurements. Using a unique technique of electrochemical measurements in single tumor spheroids, we were able to both detect the real-time response of the axial ligand to hypoxia and establish the depth of penetration of the drug into the tumor model.