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Published on: March 18, 2015
DNA-Binding, Photocleavage, and Photodynamic Anti-cancer Activities of Pyridyl Corroles
Zhen-Hua Liang1, Hai-Yang Liu2, Rong Zhou1,3
1School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou, 510641, People's Republic of China.
Abstract:
The DNA-binding, photocleavage, and antitumor activity of three free base pyridyl corroles 1, 2, and 3 have been investigated. The binding affinity toward CT-DNA decreases with increasing number of pentafluorophenyl, whereas the photocleavage activity toward pBR322 DNA becomes more efficient. Singlet oxygen was demonstrated as active species responsible for DNA cleavage. These corroles exhibited high cytotoxicity against three tested cancer cells (Hela, HapG2, and A549) and the cytotoxicity could be further enhanced under irradiation. Intracellular reactive oxygen species level was also monitored using HeLa Cells upon the combined treatment of corroles and light. These corroles could be absorbed by HeLa cells at low concentration. They can induce the decrease of mitochondrial membrane potential and apoptosis of tumor cells under irradiation.
Insights
Three pyridyl corroles show potent antitumor activity, effectively cleaving DNA and inducing cancer cell death, especially when activated by light. These compounds generate singlet oxygen, a key factor in their DNA-damaging and cytotoxic effects.
Area of Science:
- Supramolecular Chemistry
- Photodynamic Therapy
- Medicinal Chemistry
Background:
- Pyridyl corroles are macrocyclic compounds with potential applications in medicine.
- Understanding their interaction with DNA and their photophysical properties is crucial for developing new cancer therapies.
Purpose of the Study:
- To investigate the DNA-binding, photocleavage, and antitumor activities of three free base pyridyl corroles.
- To elucidate the mechanism of DNA cleavage and the role of reactive oxygen species.
- To evaluate the photodynamic effects on cancer cell lines.
Main Methods:
- Synthesis and characterization of three pyridyl corroles.
- DNA binding affinity studies using UV-Vis titration and fluorescence spectroscopy.
- DNA photocleavage assays using pBR322 DNA.
- Cytotoxicity assays against Hela, HepG2, and A549 cancer cell lines.
- Intracellular reactive oxygen species (ROS) detection and mitochondrial membrane potential assessment.
Main Results:
- DNA binding affinity decreased with increasing pentafluorophenyl substitution.
- Photocleavage activity against pBR322 DNA increased with substitution.
- Singlet oxygen was identified as the primary species responsible for DNA cleavage.
- Corroles exhibited high cytotoxicity against tested cancer cells, enhanced by light irradiation.
- Irradiation of corrole-treated HeLa cells led to decreased mitochondrial membrane potential and induced apoptosis.
Conclusions:
- Pyridyl corroles demonstrate promising DNA photocleavage and photodynamic antitumor activities.
- The observed cytotoxicity is mediated by light-induced generation of reactive oxygen species.
- These corroles represent potential candidates for photodynamic cancer therapy.
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