Photoinduced Reduction of Novel Dual-Action Riboplatin Pt(IV) Prodrug.

Controlled photoreduction of Pt(IV) prodrugs is a challenging task due to the possibility of targeted light-controlled activation of anticancer agents without affecting healthy tissues. Also, a conjugation of photosensitizers and clinically used platinum drugs into one Pt(IV) prodrug allows combining photodynamic therapy and chemotherapy approaches into one molecule. Herein, we designed the cisplatin-based Pt(IV) prodrug Riboplatin with tetraacetylriboflavin in the axial position.

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

We report herein a Pt(IV) prodrug with metronidazole in axial positions -. 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 prodrug instead of rapid intracellular degradation.

Pt(IV) Prodrugs with Non-Steroidal Anti-inflammatory Drugs in the Axial Position.

We report herein the design, synthesis, and biological investigation of a series of novel Pt(IV) prodrugs with non-steroidal anti-inflammatory drugs naproxen, diclofenac, and flurbiprofen, as well as these with stearic acid in the axial position. Six Pt(IV) prodrugs were designed, which showed superior antiproliferative activity compared to cisplatin as well as an ability to overcome tumor cell line resistance to cisplatin. By tuning the drug lipophilicity via variation of the axial ligands, the most potent Pt(IV) prodrug was obtained, with an enhanced cellular accumulation of up to 153-fold that of cisplatin and nanomolar cytotoxicity both in 2D and 3D cell cultures.

Linking stages of non-rapid eye movement sleep to the spectral EEG markers of the drives for sleep and wake.

The conventional staging classification reduces all patterns of sleep polysomnogram signals to a small number of yes-or-no variables labeled wake or a stage of sleep (e.g., W, N1, N2, N3, and R for wake, the first, second, and third stages of non-rapid eye movement sleep and rapid eye movement sleep, respectively).

[Effects of weak low-frequency electromagnetic field on sleep structure during daytime sleep].

Objective: To test the hypothesis that weak electromagnetic fields of low frequencies (0.5-26 Hz) could affect daytime sleep features and structure.

Material And Methods: Parameters of daytime sleep continuity were compared in the study with counterbalanced control/exposition (40 min exposure to electromagnetic field at 1 Hz/0.