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Published on: December 1, 2016
Exploration of quinolone and quinoline derivatives as potential anticancer agents
Jamshed Iqbal1, Syeda Abida Ejaz2, Imtiaz Khan3
1Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan. drjamshed@ciit.net.pk.
Background:
Among the different types of cancers, breast cancer, bone cancer and cervical cancer are the most common gender specific cancer types that are affecting the women worldwide. Currently, many enzymatic and cellular pathways are known as drug targets for the treatment of cancer. Even though many improvements have been made in the therapy of various types of cancer, but the major disadvantage of available anti-cancer drugs is their non-selective behavior towards cancer cells as well as normal cells.
Objectives:
In the light of this fact, the searching of new compounds with selective behavior only towards cancer cells is critically important. Previously, we have identified several series of compounds as the potential inhibitors of these families.
Methods:
Herein, we investigate quinolones and quinolines for their anti-cancer activity against breast cancer cells (MCF-7), bone marrow cancer cells (K-562) and cervical cancer cells (HeLa) by MTT assay. The most effective derivatives were further subjected to flow cytometry analysis followed by fluorescence microscopic analysis by using 4´,6-diamidine-2´-phenylindole (DAPI) and propidium staining (PI) staining.
Results:
All the tested compounds were found selective only towards cancer cells. The identified compounds also induced either G2 or S-phase cell cycle arrest within the respective cancer cell line, chromatin condensation and the nuclear fragmentation, as well as maximum interaction with DNA.
Conclusions:
These results provide evidence that the characteristic chemical features of attached groups are the key factors for their anticancer effects and play a useful role in revealing the mechanisms of action in relation to the known compounds in future research programs. Graphical abstract Flow cytometric analysis of cell cycle using propidium iodide staining. Cell apoptosis observed under fluorescence microscope using DAPI and PI staining.
Insights
New quinolone and quinoline compounds show selective anti-cancer activity against breast, bone, and cervical cancer cells. These compounds induce cell cycle arrest and DNA interaction, offering a promising avenue for targeted cancer therapies.
Area of Science:
- Medicinal Chemistry
- Oncology
- Molecular Biology
Background:
- Breast, bone, and cervical cancers are prevalent women's cancers with limited targeted therapies.
- Current anti-cancer drugs often lack selectivity, affecting both cancerous and normal cells.
- Developing novel, selective anti-cancer agents is crucial for improved treatment outcomes.
Purpose of the Study:
- To investigate the anti-cancer potential of quinolone and quinoline derivatives.
- To evaluate the selectivity of these compounds against specific cancer cell lines.
- To elucidate the mechanism of action of effective anti-cancer compounds.
Main Methods:
- MTT assay was used to assess anti-cancer activity against MCF-7, K-562, and HeLa cancer cells.
- Flow cytometry and fluorescence microscopy (DAPI/PI staining) were employed for cell cycle and apoptosis analysis.
- Investigated interaction with DNA and induction of chromatin condensation/nuclear fragmentation.
Main Results:
- All tested quinolone and quinoline compounds demonstrated selectivity towards cancer cells.
- Compounds induced G2 or S-phase cell cycle arrest in treated cancer cell lines.
- Evidence of chromatin condensation, nuclear fragmentation, and significant DNA interaction was observed.
Conclusions:
- The chemical structure of substituents on quinolone and quinoline derivatives dictates their anti-cancer efficacy.
- These findings provide insights into the mechanism of action for future drug development.
- The study highlights the potential of these compounds for targeted cancer therapy research.
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