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Gold(III)-dithiocarbamato anticancer agents: activity, toxicology and histopathological studies in rodents
Cristina Marzano1, Luca Ronconi, Federica Chiara
1Department of Pharmaceutical Sciences, University of Padova, Padova, Italy.
Abstract:
Gold(III)-dithiocarbamato complexes have recently gained increasing attention as potential anticancer agents because of their strong tumor cell growth--inhibitory effects, generally achieved by exploiting non-cisplatin-like mechanisms of action. The rationale of our research work is to combine the antitumor properties of the gold(III) metal center with the potential chemoprotective function of coordinated dithiocarbamates in order to reduce toxic side effects (in particular nephrotoxicity) induced by clinically established platinum-based drugs. In this context, [Au(III) Br(2) (ESDT)] (AUL12) was proved to exert promising and outstanding antitumor activity in vitro and to overcome both acquired and intrinsic resistance showed by some types of tumors toward cisplatin. As a subsequent extension of our previous work, we here report on detailed in vivo studies in rodents, including antitumor activity toward three transplantable murine tumor models, toxicity, nephrotoxicity and histopathological investigations. Remarkably, the gold(III) complex AUL12 stands out for higher anticancer activity than cisplatin toward all the murine tumor models examined, inducing up to 80% inhibition of tumor growth. In addition, it shows low acute toxicity levels (lethal dose, LD(50) = 30 mg kg(-1) ) and reduced nephrotoxicity. Altogether, these results confirm the reliability of our drug design strategy and support the validation of this gold(III)-dithiocarbamato derivative as a suitable candidate for clinical trials.
Insights
A novel gold(III) complex, AUL12, demonstrates superior anticancer activity compared to cisplatin in preclinical rodent models. This dithiocarbamato derivative shows reduced toxicity and nephrotoxicity, supporting its potential for clinical trials.
Area of Science:
- Inorganic Chemistry
- Medicinal Chemistry
- Oncology
Background:
- Gold(III)-dithiocarbamato complexes are explored as anticancer agents due to non-cisplatin-like mechanisms.
- Platinum-based drugs cause significant toxic side effects, particularly nephrotoxicity.
- There is a need for novel anticancer agents with improved efficacy and reduced toxicity.
Purpose of the Study:
- To evaluate the in vivo antitumor activity, toxicity, and nephrotoxicity of the gold(III) complex [Au(III) Br(2) (ESDT)] (AUL12).
- To compare the efficacy and safety profile of AUL12 with cisplatin in preclinical cancer models.
- To validate a drug design strategy combining gold(III) properties with dithiocarbamate chemoprotection.
Main Methods:
- In vivo studies in rodents using three transplantable murine tumor models.
- Assessment of antitumor activity, acute toxicity (LD50), and nephrotoxicity.
- Histopathological investigations to evaluate tissue damage.
Main Results:
- AUL12 exhibited higher anticancer activity than cisplatin across all tested murine tumor models, achieving up to 80% tumor growth inhibition.
- The complex demonstrated low acute toxicity with an LD50 of 30 mg kg(-1).
- AUL12 showed significantly reduced nephrotoxicity compared to established platinum-based drugs.
Conclusions:
- The gold(III)-dithiocarbamato complex AUL12 is a promising anticancer candidate with superior efficacy and a favorable safety profile.
- The study validates the drug design strategy for developing novel gold-based anticancer agents.
- AUL12 warrants further investigation in clinical trials for cancer treatment.
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