Potent Antineoplastic Activity against Breast Cancer in Vitro and in Vivo of a Chloro-Substituted Polyaromatic Platinum(II) Complex and Its Platinum(IV) Prodrug
5 affiliations
- 1School of Arts and Sciences, Department of Biological Sciences, Lebanese American University, P.O. Box 13-5053, Chouran, Beirut, 1102 2801 Lebanon.
- 2School of Science, Western Sydney University, Locked Bag 1797 Penrith South, 2751 New South Wales, Australia.
- 3Gilbert and Rose-Marie Chagoury School of Medicine, Lebanese American University, P.O. Box 13-5053, Chouran, Beirut, 1102 2801 Lebanon.
- 4Alice Ramez Chagoury School of Nursing, Lebanese American University, P.O. Box 13-5053, Chouran, Beirut, 1102 2801 Lebanon.
- 5School of Arts and Sciences, Department of Physical Sciences, Lebanese American University, P.O. Box 13-5053, Chouran, Beirut, 1102 2801 Lebanon.
Abstract
This study investigates the chemotherapeutic potential of PtII5CLSS and PtIV5CLSS against breast cancer in vivo. Cell viability was assessed 72 h post-treatment, revealing potent cytotoxic activity with IC50 values of 0.447 μM for PtII5CLSS and 0.922 μM for PtIV5CLSS. Cellular uptake studies used ICP-MS to confirm active transport of both complexes into cells, showing significant accumulation in the nuclear/cytoskeletal fractions. A 28-day toxicity study in female Sprague-Dawley rats demonstrated that escalating doses up to 15 mg/kg (PtII5CLSS) and 30 mg/kg (PtIV5CLSS) caused no mortality nor adverse effects on liver and kidney function. In a chemically induced breast cancer rat model, both complexes significantly reduced tumor weight by 93–100% at doses of 1 and 5 mg/kg, with no observable nephrotoxicity or hepatotoxicity. Histopathological analysis confirmed the reduction or absence of tumors in the majority of the treated animals with PtIV5CLSS (1 mg/kg bw) being the most effective. Toxicity evaluation in sus scrofa pigs showed that PtIV5CLSS was well tolerated at both 1- and 2.5 mg/kg bw, with no mortality, behavioral changes, or signs of acute toxicity. Overall, both PtII5CLSS and PtIV5CLSS demonstrate strong antineoplastic activity against breast cancer with a favorable safety profile, supporting their potential as alternative platinum-based chemotherapeutic agents.
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BibTeX
@article{hammoud2026potent,
title = {{Potent Antineoplastic Activity against Breast Cancer in Vitro and in Vivo of a Chloro-Substituted Polyaromatic Platinum(II) Complex and Its Platinum(IV) Prodrug}},
author = {Omar Hammoud and Maria George Elias and Amjad Slika and Aleen Khoury and Stephanie Mehanna and Joelle Abou Chacra and Selim Nasser and Janice R Aldrich-Wright and Costantine F Daher and Robin I Taleb},
journal = {ACS Omega},
year = {2026},
month = oct,
doi = {10.1021/acsomega.5c11584},
url = {https://pubs.acs.org/acsodf/article/11/41/62402/5445926/Potent-Antineoplastic-Activity-against-Breast},
note = {CC BY-NC-ND 4.0},
}
RIS
TY - JOUR
TI - Potent Antineoplastic Activity against Breast Cancer in Vitro and in Vivo of a Chloro-Substituted Polyaromatic Platinum(II) Complex and Its Platinum(IV) Prodrug
AU - Omar Hammoud
AU - Maria George Elias
AU - Amjad Slika
AU - Aleen Khoury
AU - Stephanie Mehanna
AU - Joelle Abou Chacra
AU - Selim Nasser
AU - Janice R Aldrich-Wright
AU - Costantine F Daher
AU - Robin I Taleb
PY - 2026
DA - 2026/10/07
JO - ACS Omega
DO - 10.1021/acsomega.5c11584
UR - https://pubs.acs.org/acsodf/article/11/41/62402/5445926/Potent-Antineoplastic-Activity-against-Breast
AB - This study investigates the chemotherapeutic potential of PtII5CLSS and PtIV5CLSS against breast cancer in vivo. Cell viability was assessed 72 h post-treatment, revealing potent cytotoxic activity with IC50 values of 0.447 μM for PtII5CLSS and 0.922 μM for PtIV5CLSS. Cellular uptake studies used ICP-MS to confirm active transport of both complexes into cells, showing significant accumulation in the nuclear/cytoskeletal fractions. A 28-day toxicity study in female Sprague-Dawley rats demonstrated that escalating doses up to 15 mg/kg (PtII5CLSS) and 30 mg/kg (PtIV5CLSS) caused no mortality nor adverse effects on liver and kidney function. In a chemically induced breast cancer rat model, both complexes significantly reduced tumor weight by 93–100% at doses of 1 and 5 mg/kg, with no observable nephrotoxicity or hepatotoxicity. Histopathological analysis confirmed the reduction or absence of tumors in the majority of the treated animals with PtIV5CLSS (1 mg/kg bw) being the most effective. Toxicity evaluation in sus scrofa pigs showed that PtIV5CLSS was well tolerated at both 1- and 2.5 mg/kg bw, with no mortality, behavioral changes, or signs of acute toxicity. Overall, both PtII5CLSS and PtIV5CLSS demonstrate strong antineoplastic activity against breast cancer with a favorable safety profile, supporting their potential as alternative platinum-based chemotherapeutic agents.
SN - 2470-1343
ER -