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Host-Guest Complexation of Oxaliplatin and Para-Sulfonatocalix[n]Arenes for Potential Use in Cancer Therapy
| Content Provider | MDPI |
|---|---|
| Author | Fahmy, Sherif Ashraf Ponte, Fortuna Fawzy, Iten M. Sicilia, Emilia Bakowsky, Udo Azzazy, Hassan Mohamed El-Said |
| Copyright Year | 2020 |
| Description | P-sulfonatocalix[n]arenes have demonstrated a great potential for encapsulation of therapeutic drugs via host-guest complexation to improve solubility, stability, and bioavailability of encapsulated drugs. In this work, guest-host complexes of a third-generation anticancer drug (oxaliplatin) and p-4-sulfocalix[n]arenes (n = 4 and 6; p-SC4 and p-SC6, respectively) were prepared and investigated, using 1H NMR, UV, Job’s plot analysis, and DFT calculations, for use as cancer therapeutics. The peak amplitude of the prepared host-guest complexes was linearly proportional to the concentration of oxaliplatin in the range of 1.0 × 10−5 M−1 to 2.1 × 10−4 M−1. The reaction stoichiometry between either p-SC4 or p-SC6 and oxaliplatin in the formed complexes was 1:1. The stability constants for the complexes were 5.07 × 104 M−1 and 6.3 × 104 M−1. These correspond to complexation free energy of −6.39 and −6.52 kcal/mol for p-SC4 and p-SC6, respectively. Complexation between oxaliplatin and p-SC4 or p-SC6 was found to involve hydrogen bonds. Both complexes exhibited enhanced biological and high cytotoxic activities against HT-29 colorectal cells and MCF-7 breast adenocarcinoma compared to free oxaliplatin, which warrants further investigation for cancer therapy. |
| Starting Page | 5926 |
| e-ISSN | 14203049 |
| DOI | 10.3390/molecules25245926 |
| Journal | Molecules |
| Issue Number | 24 |
| Volume Number | 25 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2020-12-14 |
| Access Restriction | Open |
| Subject Keyword | Molecules Organic Chemistry Oxaliplatin 4-sulfonatocalix[4]arenes 4-sulfonatocalix[6]arenes Host-guest Complex Cancer Therapy |
| Content Type | Text |
| Resource Type | Article |
