ArticleActa pharmacologica Sinica2022
Helichrysetin inhibits gastric cancer growth by targeting c-Myc/PDHK1 axis-mediated energy metabolism reprogramming.
Article in Acta pharmacologica Sinica, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 27 citations in OpenAlex.
- Targeting the remodeled peritoneal ecosystem: a paradigm shift from tumor cells to the microenvironment in gastric cancer peritoneal metastasis.Frontiers in immunology · 2026Review
- Potential roles of plant metabolites and Traditional Chinese Medicine formulas in regulating glycolysis-OXPHOS plasticity in gastric precancerous lesions and gastric cancer: a critical appraisal of the evidence.Frontiers in pharmacology · 2026Review
- Role and Molecular Mechanisms of Aerobic Glycolysis in Gastrointestinal Tumors.Journal of Cancer · 2026Review
- Immunometabolism: crosstalk with tumor metabolism and implications for cancer immunotherapy.Molecular cancer · 2025Review
- Living Biotherapeutics Using Nanoparticles-Armed Cyanobacteria for Boosting Photodynamic-Immunotherapy of Cancer.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Histone deacetylases facilitate Th17-cell differentiation and pathogenicity in autoimmune uveitis via CDK6/ID2 axis.Journal of advanced research · 2025Article
- In Silico and In Vitro Analyses of Strawberry-Derived Extracts in Relation to Key Compounds' Metabolic and Anti-Tumor Effects.International journal of molecular sciences · 2025Article
- Oxidative Stress and Redox Signaling in Gastric Cancer: From Mechanisms to Therapeutic Implications.Antioxidants (Basel, Switzerland) · 2025Review
- Medicinally Privileged Natural Chalcones: Abundance, Mechanisms of Action, and Clinical Trials.International journal of molecular sciences · 2024Review
- The Induction of G2/M Phase Cell Cycle Arrest and Apoptosis by the Chalcone Derivative 1C in Sensitive and Resistant Ovarian Cancer Cells Is Associated with ROS Generation.International journal of molecular sciences · 2024Article
- The role of reactive oxygen species in gastric cancer.Cancer biology & medicine · 2024Review
- MCM8 promotes gastric cancer progression through RPS15A and predicts poor prognosis.Cancer medicine · 2024Article
- A novel peptide PDHK1-241aa encoded by circPDHK1 promotes ccRCC progression via interacting with PPP1CA to inhibit AKT dephosphorylation and activate the AKT-mTOR signaling pathway.Molecular cancer · 2024Article
- Natural Product-Based Glycolysis Inhibitors as a Therapeutic Strategy for Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitor-Resistant Non-Small Cell Lung Cancer.International journal of molecular sciences · 2024Review
- Mechanistic insights into the role of traditional Chinese medicine in treating gastric cancer.Frontiers in oncology · 2024Review
- A Novel Tri-Hydroxy-Methylated Chalcone Isolated fromInternational journal of molecular sciences · 2023Article
- Anticancer Potential of Natural Chalcones: In Vitro and In Vivo Evidence.International journal of molecular sciences · 2023Review
- AAZ2 induces mitochondrial-dependent apoptosis by targeting PDK1 in gastric cancer.Journal of Zhejiang University. Science. B · 2023Article
- Traditional Chinese medicine for transformation of gastric precancerous lesions to gastric cancer: A critical review.World journal of gastrointestinal oncology · 2023Review
- The identification and validation of hub genes associated with advanced IPF by weighted gene co-expression network analysis.Functional & integrative genomics · 2022Article
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Authors and funding
13 authors at 4 institutions in 2 countries.
Funding
Abstract
Helichrysetin (HEL), a chalcone isolated from Alpinia katsumadai Hayata, has an antitumor activity in human lung and cervical cancers. However, the inhibitory effect and underlying mechanism of HEL in gastric cancer have not been elucidated. Here, HEL significantly inhibited the growth of gastric cancer MGC803 cells in vitro and in vivo. HEL decreased expression and transcriptional regulatory activity of c-Myc and mRNA expression of c-Myc target genes. HEL enhanced mitochondrial oxidative phosphorylation (OXPHOS) and reduced glycolysis as evidenced by increased mitochondrial adenosine triphosphate (ATP) production and excessive reactive oxygen species (ROS) accumulation, and decreased the pPDHA1/PDHA1 ratio and Glyco-ATP production. Pyruvate enhanced OXPHOS after HEL treatment. c-Myc overexpression abolished HEL-induced inhibition of cell viability, glycolysis, and protein expression of PDHK1 and LDHA. PDHK1 overexpression also counteracted inhibitory effect of HEL on cell viability. Conversely, c-Myc siRNA decreased cell viability, glycolysis, and PDHK1 expression. NAC rescued the decrease in viability of HEL-treated cells. Additionally, HEL inhibited the overactivated mTOR/p70S6K pathway in vitro and in vivo. HEL-induced cell viability inhibition was counteracted by an mTOR agonist. mTOR inhibitor also decreased cell viability. Similar results were obtained in SGC7901 cells. HEL repressed lactate production and efflux in MGC803 cells. These results revealed that HEL inhibits gastric cancer growth by targeting mTOR/p70S6K/c-Myc/PDHK1-mediated energy metabolism reprogramming in cancer cells. Therefore, HEL may be a potential agent for gastric cancer treatment by modulating cancer energy metabolism reprogramming.
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