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Updated: Jul 6, 2025

Ex Vivo Treatment Response of Primary Tumors and/or Associated Metastases for Preclinical and Clinical Development of Therapeutics
Published on: October 2, 2014
Apigenin exerts anti-cancer effects in colon cancer by targeting HSP90AA1
Arindam Sain1, Dipshikha Khamrai1, Thirukumaran Kandasamy2
1Department of Biotechnology, Maulana Abul Kalam Azad University of Technology, West Bengal, Nadia, West Bengal, India.
Abstract:
Apigenin, a flavonoid, has shown early promise in colon cancer (CC); thus, exploring potential mechanisms of Apigenin is obligatory. In this study, shared targets of Apigenin and CC were identified through online tools, which were then subjected to functional enrichment analyses, Gene Ontology and KEGG. Further, the protein-protein interaction network of the shared targets was developed (via STRING). The top targets of Apigenin in CC were identified by molecular docking; further investigated for differential gene and protein expression in CC and their influence on CC patient survival (using TCGA data). Out of 13 hub genes, the top 3 targets (HSP90AA1, MMP9, PTGS2) were selected based on docking score. Their expression was significantly elevated and related to poor overall survival in CC (except PTGS2). Molecular dynamics simulation further validated protein-ligand interactions and divulged HSP90AA1 as the best target of Apigenin in CC. Finally, the anti-cancer effects of Apigenin and its major metabolite, luteolin, were investigated in CC, which is involved in the cytotoxicity of CC cells (COLO-205) by reducing HSP90AA1 expression revealed by real-time PCR. Thus, HSP90AA1 was identified as one of the prime targets of Apigenin in CC, and Apigenin could be effective against CC.
Insights
Apigenin shows promise for colon cancer (CC). This study identifies HSP90AA1 as a key target, demonstrating Apigenin
Area of Science:
- Oncology
- Pharmacology
- Bioinformatics
Background:
- Colon cancer (CC) remains a significant health concern.
- Flavonoids, like Apigenin, are being investigated for their anti-cancer properties.
- Understanding Apigenin's mechanisms in CC is crucial for therapeutic development.
Purpose of the Study:
- To identify and validate molecular targets of Apigenin in colon cancer.
- To explore the therapeutic potential of Apigenin and its metabolite, luteolin, against CC.
- To elucidate the role of HSP90AA1 in Apigenin's anti-cancer effects.
Main Methods:
- Bioinformatic analysis to identify shared targets between Apigenin and CC.
- Functional enrichment analysis (Gene Ontology, KEGG) and protein-protein interaction network construction.
- Molecular docking, molecular dynamics simulation, differential gene/protein expression analysis (TCGA data), and real-time PCR.
Main Results:
- HSP90AA1, MMP9, and PTGS2 were identified as top potential targets.
- HSP90AA1 and MMP9 expression were elevated in CC and linked to poor survival.
- HSP90AA1 was confirmed as a primary target, with Apigenin reducing its expression and inducing cytotoxicity in CC cells.
Conclusions:
- HSP90AA1 is a key molecular target for Apigenin's anti-colon cancer activity.
- Apigenin and its metabolite luteolin exhibit anti-cancer effects against CC cells.
- Apigenin holds potential as a therapeutic agent for colon cancer treatment.
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