ArticleOncotarget2016
Hop derived flavonoid xanthohumol inhibits endothelial cell functions via AMPK activation.
Article in Oncotarget, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 36 citations in OpenAlex.
- Humulus lupus extract rich in xanthohumol improves the clinical course in critically ill COVID-19 patients.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2023Trial
- Xanthohumol: Mechanistic Actions and Emerging Evidence as a Multi-Target Natural Nutraceutical.Nutrients · 2026Review
- Review
- Multiple myeloma inhibitory effects of natural compounds: enhancement through nanoparticle carriers.Frontiers in pharmacology · 2025Review
- Flavonoids with Anti-Angiogenesis Function in Cancer.Molecules (Basel, Switzerland) · 2024Review
- The Hepatic Antisteatosis Effect of Xanthohumol in High-Fat Diet-Fed Rats Entails Activation of AMPK as a Possible Protective Mechanism.Foods (Basel, Switzerland) · 2023Article
- An Overview of Bioactive Phenolic Molecules and Antioxidant Properties of Beer: Emerging Trends.Molecules (Basel, Switzerland) · 2023Review
- Microbiota-Derived Natural Products Targeting Cancer Stem Cells: Inside the Gut Pharma Factory.International journal of molecular sciences · 2023Review
- Orchestrated Action of AMPK Activation and Combined VEGF/PD-1 Blockade with Lipid Metabolic Tunning as Multi-Target Therapeutics against Ovarian Cancers.International journal of molecular sciences · 2022Review
- Review
- Anti-Remodeling Effects of Xanthohumol-Fortified Beer in Pulmonary Arterial Hypertension Mediated by ERK and AKT Inhibition.Nutrients · 2019Article
- The Multiple Biological Targets of Hops and Bioactive Compounds.Chemical research in toxicology · 2019Review
- Non-estrogenic Xanthohumol Derivatives Mitigate Insulin Resistance and Cognitive Impairment in High-Fat Diet-induced Obese Mice.Scientific reports · 2018Article
- Antiangiogenic Effect of Flavonoids and Chalcones: An Update.International journal of molecular sciences · 2017Review
- AMPK activation-dependent autophagy compromises oleanolic acid-induced cytotoxicity in human bladder cancer cells.Oncotarget · 2017Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Angiogenesis, a process characterized by the formation of new blood vessels from pre-existing ones, is a crucial step in tumor growth and dissemination. Recently, increased attention has been addressed to the ability of flavonoids to prevent cancer by suppressing angiogenesis, strategy that we named "angioprevention". Several natural compounds exert their anti-tumor properties by activating 5' adenosine monophosphate-activated protein kinase (AMPK), a key regulator of metabolism in cancer cells. Drugs with angiopreventive activities, in particular metformin, regulate AMPK in endothelial cells. Here we investigated the involvement of AMPK in the anti-angiogenic effects of xanthohumol (XN), the major prenylated flavonoid of the hop plant, and mechanisms of action. The anti-angiogenic activity of XN was more potent than epigallocatechin-3-gallate (EGCG). Treatment of endothelial cells with XN led to increased AMPK phosphorylation and activity. Functional studies using biochemical approaches confirmed that AMPK mediates XN anti-angiogenic activity. AMPK activation by XN was mediated by CAMMKβ, but not LKB1. Analysis of the downstream mechanisms showed that XN-induced AMPK activation reduced nitric oxide (NO) levels in endothelial cells by decreasing eNOS phosphorylation. Finally, AKT pathway was inactivated by XN as part of its anti-angiogenic activity, but independently from AMPK, suggesting that these two signaling pathways proceed autonomously. Our study dissects the molecular mechanism by which XN exerts its potent anti-angiogenic activity, pointing out AMPK as a crucial signal transducer.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.