AI Article Synopsis
- Glycosylated platinum(IV) complexes were developed as new cancer treatment substrates and demonstrated significant cytotoxicity against cancer cells in both lab and live models.
- These complexes, specifically galactoside, glucoside, and mannoside variants, were shown to possess nearly 166 times greater antitumor activity compared to traditional platinum-based drugs like cisplatin.
- The addition of a hexadecanoic chain improved drug delivery through binding with human serum albumin, enhancing stability and reducing unwanted interactions in the bloodstream, indicating potential safety for clinical use.
Article Abstract
Glycosylated platinum(IV) complexes were synthesized as substrates for GLUTs and OCTs for the first time, and the cytotoxicity and detailed mechanism were determined in vitro and in vivo. Galactoside Pt(IV), glucoside Pt(IV), and mannoside Pt(IV) were highly cytotoxic and showed specific cancer-targeting properties in vitro and in vivo. Glycosylated platinum(IV) complexes 5, 6, 7, and 8 (IC 0.24-3.97 μM) had better antitumor activity of nearly 166-fold higher than the positive controls cisplatin (1a), oxaliplatin (3a), and satraplatin (5a). The presence of a hexadecanoic chain allowed binding with human serum albumin (HSA) for drug delivery, which not only enhanced the stability of the inert platinum(IV) prodrugs but also decreased their reduction by reductants present in human whole blood. Their preferential accumulation in cancer cells compared to noncancerous cells (293T and 3T3 cells) suggested that they were potentially safe for clinical therapeutic use.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acs.jmedchem.7b00433 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!