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Organotin(IV) Azo Hydrazonates as Lysosome-Targeted Imaging and Anticancer Agents
Sanchita Das1, Pratikshya Das Pattanayak1, Takahiro Sasamori2
1Department of Chemistry, National Institute of Technology, Rourkela, Odisha, India.
Abstract:
Metallodrugs with organotin(IV) compounds emerging as a potential alternative to platinum-based drugs have revolutionized the field of both diagnosis and therapy, offering enhanced anticancer efficacy and bio-imaging capabilities for targeting intracellular organelles. In this regard, we embarked on an effort to explore the theranostic potential of a new class of azo hydrazone-based organotin(IV) complexes [SnIVL1-4(Ph)2] (1-4). The speciation studies suggested the complexes possess exceptional hydrolytic stability. Moreover, the hydrophobic nature of complexes, as determined through partition coefficient measurements, allows their efficient cellular penetration. The cytotoxic potential of 1-4 was evaluated against A549, HT-29, and NIH-3T3 cell lines, revealing that 3 was the most toxic among the series, with an IC50 of 7.8 ± 0.2 µM against A549. Further in-depth mechanistic studies revealed that they preferentially accumulate in the lysosome, damage lysosomal membrane potential, and upregulate intracellular reactive oxygen species (ROS), leading to apoptotic-mediated cancer cell death.
Insights
New organotin(IV) complexes show promise as anticancer agents. These metallodrugs effectively target cancer cells, leading to cell death via lysosomal damage and reactive oxygen species (ROS) production.
Area of Science:
- Organometallic Chemistry
- Medicinal Chemistry
- Cancer Therapeutics
Background:
- Organotin(IV) compounds are emerging as alternatives to platinum-based drugs in cancer therapy.
- These metallodrugs offer potential for enhanced anticancer efficacy and bio-imaging.
- Azo hydrazone-based ligands are being explored for novel metallodrug development.
Purpose of the Study:
- To explore the theranostic potential of novel azo hydrazone-based organotin(IV) complexes.
- To evaluate the anticancer efficacy and cellular mechanisms of these new metallodrugs.
- To assess the hydrolytic stability and cellular penetration of the synthesized complexes.
Main Methods:
- Synthesis and characterization of four organotin(IV) complexes: [SnIVL1-4(Ph)2] (1-4).
- Speciation studies to determine hydrolytic stability.
- Partition coefficient measurements to assess hydrophobicity and cellular penetration.
- In vitro cytotoxicity assays against A549, HT-29, and NIH-3T3 cell lines.
- Mechanistic studies involving lysosomal localization, membrane potential assessment, and ROS level determination.
Main Results:
- The synthesized organotin(IV) complexes exhibited excellent hydrolytic stability.
- Their hydrophobic nature facilitated efficient cellular penetration.
- Complex 3 demonstrated significant cytotoxicity against A549 cells with an IC50 of 7.8 ± 0.2 µM.
- Mechanistic studies indicated lysosomal accumulation, lysosomal membrane potential damage, and ROS upregulation.
Conclusions:
- The novel azo hydrazone-based organotin(IV) complexes possess significant theranostic potential.
- Complex 3 is a potent anticancer agent inducing apoptosis through lysosomal disruption and ROS generation.
- These findings support the development of organotin(IV) compounds as a new class of metallodrugs for cancer treatment.
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