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Published on: April 6, 2016
Systematic understanding of anti-tumor mechanisms of Tamarixetin through network and experimental analyses
Sanu K Shaji1, G Drishya1, Damu Sunilkumar1
1School of Biotechnology, Amrita Vishwa Vidyapeetham, Amritapuri, Clappana P.O, Kollam, Kerala, 690525, India.
Abstract:
Tamarixetin, a flavonoid derived from Quercetin, was shown to possess anti-cancer properties in various types of cancer. However, the mechanism of action of this compound is not well understood. Observations from reverse docking and network pharmacology analysis, were validated by cell based studies to analyse the chemotherapeutic potential and elucidate the molecular mechanism of action of Tamarixetin in breast cancer. In silico analysis using reverse docking and PPI analysis clearly indicated that out of 35 proteins targeted by Tamarixetin, the top 3 hub genes, namely, AKT1, ESR1 and HSP90AA1, were upregulated in breast tumor tissues and more importantly showed strong negative correlation to breast cancer patient survival. Furthermore, the KEGG pathway analysis showed enrichment of target proteins of Tamarixetin in 33 pathways which are mainly involved in neoplastic signalling. In vitro cell-based studies demonstrated that Tamarixetin could inhibit cell proliferation, induce ROS and reduce mitochondrial membrane potential, leading to cell death. Tamarixetin induced cell cycle arrest at G2/M phase and inhibited the migration as well as the invasion of breast cancer cells. Taken together, the combination of in silico and in vitro approaches used in the present study clearly provides evidence for the chemotherapeutic potential of Tamarixetin in breast cancer.
Insights
Tamarixetin, a flavonoid, shows promise as a breast cancer treatment by inhibiting cancer cell growth and survival. This study elucidates its anticancer mechanisms through computational and cell-based analyses.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Tamarixetin, a quercetin-derived flavonoid, exhibits anticancer properties.
- The precise molecular mechanisms underlying Tamarixetin's efficacy remain largely unelucidated.
Purpose of the Study:
- To investigate the chemotherapeutic potential of Tamarixetin in breast cancer.
- To elucidate the molecular mechanisms of action of Tamarixetin in breast cancer using integrated in silico and in vitro approaches.
Main Methods:
- In silico analyses including reverse docking and network pharmacology.
- Protein-protein interaction (PPI) and KEGG pathway analyses.
- In vitro cell-based assays to assess proliferation, cell death, cell cycle, migration, and invasion.
Main Results:
- In silico analysis identified AKT1, ESR1, and HSP90AA1 as key targets of Tamarixetin, negatively correlated with breast cancer patient survival.
- KEGG pathway analysis revealed Tamarixetin targets are enriched in neoplastic signaling pathways.
- In vitro studies confirmed Tamarixetin inhibits breast cancer cell proliferation, induces reactive oxygen species (ROS), reduces mitochondrial membrane potential, causes G2/M cell cycle arrest, and inhibits migration and invasion.
Conclusions:
- Tamarixetin demonstrates significant chemotherapeutic potential against breast cancer.
- The study provides comprehensive evidence for Tamarixetin's anticancer effects and molecular mechanisms in breast cancer.
