ArticleInternational journal of molecular sciences2019
Vanillic Acid Suppresses HIF-1α Expression via Inhibition of mTOR/p70S6K/4E-BP1 and Raf/MEK/ERK Pathways in Human Colon Cancer HCT116 Cells.
Article in International journal of molecular sciences, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 papers.
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Who cites it
64 citing papers in PubMed, 120 citations in OpenAlex.
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- Therapeutic Potential of Plant Phenolic Acids Combating Cancer Drug Resistance.Recent advances in food, nutrition & agriculture · 2026Review
- ERBB2 mutations promote recurrence and metastasis in non-muscle-invasive bladder cancer via HIF-1 phosphorylation: Insights from whole exome sequencing.Journal of pharmaceutical analysis · 2026Article
- Evaluation of Anticancer Potential ofAntioxidants (Basel, Switzerland) · 2025Article
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- The Protective Effects of Vanillic Acid on LPS-induced Acute Lung Injury by Inhibiting STIM1-mediated NLRP3 Inflammasome Activation.Inflammation · 2025Article
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- Metabolomics Revealed the Differential Metabolites of Different Broomcorn Millet Varieties in Shanxi.Food science & nutrition · 2025Article
- Spectroscopic, antioxidant and cytotoxicity studies of vanillic acids.Scientific reports · 2025Article
- Liensinine reshapes the immune microenvironment and enhances immunotherapy by reprogramming metabolism through the AMPK-HIF-1α axis in hepatocellular carcinoma.Journal of experimental & clinical cancer research : CR · 2025Article
- Mushroom-derived bioactive compounds pharmacological properties and cancer targeting: a holistic assessment.Discover oncology · 2025Review
- Phillygenin regulates the colorectal cancer tumor microenvironment by inhibiting hypoxia-inducible factor 1 alpha.Cytotechnology · 2025Article
- Anti-tumor role and molecular mechanism of vanillic acid.Discover oncology · 2025Review
- The Role of Zuo Jin Wan in Modulating the Tumor Microenvironment of Colorectal Cancer.Combinatorial chemistry & high throughput screening · 2025Article
- Recent Update of Natural Compounds as HIF-1α Inhibitors in Colorectal Carcinoma.Drug design, development and therapy · 2025Review
- Phenolic Characterization and Quality Evaluation of Herbal Coffee from Roasted Juniper Berry Fruits (Foods (Basel, Switzerland) · 2024Article
- Correlation Analysis Among the Chemical Composition and Cytotoxic and Antioxidative Activities of aPlants (Basel, Switzerland) · 2024Article
4 more citing papers are in PubMed but not listed here.
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
Abstract
Hypoxia-inducible factor 1 (HIF-1) plays a pivotal role in tumor adaptation to microenvironmental hypoxia, and it also exerts important roles in angiogenesis and tumor development. Vanillic acid is a dietary phenolic compound reported to exhibit anticancer properties. However, the mechanisms by which vanillic acid inhibits tumor growth are not fully understood. Here, we investigated the effect of vanillic acid on HIF-1α activation. Vanillic acid significantly inhibits HIF-1α expression induced by hypoxia in various human cancer cell lines. Further analysis revealed that vanillic acid inhibited HIF-1α protein synthesis. Neither the HIF-1α protein degradation rate nor the steady-state HIF-1α mRNA levels were affected by vanillic acid. Moreover, vanillic acid inhibited HIF-1α expression by suppressing mammalian target of rapamycin/p70 ribosomal protein S6 kinase/eukaryotic initiation factor 4E-binding protein-1 and Raf/extracellular signal-regulated kinase (ERK) kinase (MEK)/ERK pathways. We found that vanillic acid dose-dependently inhibited VEGF and EPO protein expressions and disrupted tube formation. The results suggest that vanillic acid effectively inhibits angiogenesis. Flow cytometry analysis demonstrated that vanillic acid significantly induced G1 phase arrest and inhibited the proliferation of human colon cancer HCT116 cells. In vivo experiments confirmed that vanillic acid treatment caused significant inhibition of tumor growth in a xenografted tumor model. These studies reveal that vanillic acid is an effective inhibitor of HIF-1α and provides new perspectives into the mechanism of its antitumor activity.
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