ArticleScientific reports2018
Shikonin Inhibits Tumor Growth in Mice by Suppressing Pyruvate Kinase M2-mediated Aerobic Glycolysis.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 84 papers, 1 of them a synthesis that pooled it.
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Who cites it
84 citing papers in PubMed, 1 synthesis or guideline pooled it, 149 citations in OpenAlex.
- Natural products targeting glycolysis in cancer.Frontiers in pharmacology · 2022Pooled it
- Shikonin Promotes Apoptosis in Multiple Myeloma Cells Through the PKM2-AMPK-PGC1α Metabolic Axis.Journal of clinical laboratory analysis · 2026Article
- Targeting Pyruvate Kinase M2: Signal Transduction Pathways and Exploration of Cancer Therapeutic Strategies.The AAPS journal · 2026Review
- PKM2-Mediated Glycolytic Reprogramming in Thyroid Cancer: Mechanistic Insights and Therapeutic Potential.Molecules (Basel, Switzerland) · 2026Review
- Review
- Benzyl-Naphthoquinones as Selective Anticancer Agents for Oral Squamous Cell Carcinoma via Apoptosis Induction.Biomedicines · 2026Article
- Glycolysis and glycolytic enzymes in acute myeloid leukemia: Warburg and beyond.Frontiers in pharmacology · 2026Review
- HPV-driven metabolic reprogramming promotes T cell exhaustion: targeting immunometabolic barriers with natural products.Frontiers in immunology · 2026Review
- Pyruvate kinase M2 in Alzheimer's disease: from dysregulation to therapeutic inhibition.Brain communications · 2026Review
- PKM2 is the Metabolic Checkpoint for Stemness Features in Head and Neck Cancer.Journal of Cancer · 2026Article
- Role of elevation of glycolysis in tumor-associated macrophages in glioblastoma immune evasion and therapeutic implications.PNAS nexus · 2026Review
- Nanotechnology-based shikonin delivery strategies for modulating the tumor immune microenvironment efficacy.Drug delivery and translational research · 2026Review
- Co-delivery of shikonin and JQ1 inhibits triple-negative breast tumor progression and lung metastasis through inhibition of epithelial-mesenchymal transition and vasculogenic mimicry.Acta pharmacologica Sinica · 2025Article
- The expression of establishment of cohesion 1 homolog 2 (ESCO2) in tumor cells and its research progress as a therapeutic target.European journal of medical research · 2025Review
- Mechanistic Insights into the Anticancer Action of Novel 2‑Hydroxy-1,4-naphthoquinone Thiol Derivatives.ACS omega · 2025Article
- Research Progress of Natural Compounds from Chinese Herbal Medicine in the Treatment of Melanoma.Current treatment options in oncology · 2025Review
- The glycolytic reaction PGAM restrains Th17 pathogenicity and Th17-dependent autoimmunity.Cell reports · 2025Article
- Evolutionary Transcriptomics of Cancer Development.International journal of molecular sciences · 2025Article
- Herbal Medicine: Enhancing the Anticancer Potential of Natural Products in Hepatocellular Carcinoma Therapy Through Advanced Drug Delivery Systems.Pharmaceutics · 2025Review
- Oxidized LDL stimulates PKM2-mediated mtROS production and phagocytosis.Journal of lipid research · 2025Article
24 more citing papers are in PubMed but not listed here.
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Shift metabolism profile from mitochondrial oxidative phosphorylation to aerobic glycolysis (Warburg effect) is a key for tumor cell growth and metastasis. Therefore, suppressing the tumor aerobic glycolysis shows a great promise in anti-tumor therapy. In the present study, we study the role of shikonin, a naphthoquinone isolated from the traditional Chinese medicine Lithospermum, in inhibiting tumor aerobic glycolysis and thus tumor growth. We found that shikonin dose-dependently inhibited glucose uptake and lactate production in Lewis lung carcinoma (LLC) and B16 melanoma cells, confirming the inhibitory effect of shikonin on tumor aerobic glycolysis. Treatment of shikonin also decreased tumor cell ATP production. Furthermore, pyruvate kinase M2 (PKM2) inhibitor or activator respectively altered the effect of shikonin on tumor cell aerobic glycolysis, suggesting that suppression of cell aerobic glycolysis by shikonin is through decreasing PKM2 activity. Western blot analysis confirmed that shikonin treatment reduced tumor cell PKM2 phosphorylation though did not reduce total cellular PKM2 level. In vitro assay also showed that shikonin treatment significantly promoted tumor cell apoptosis compared to untreated control cells. Finally, when mice implanted with B16 cells were administered with shikonin or control vehicle, only shikonin treatment significantly decreased B16 tumor cell growth. In conclusion, this study demonstrates that shikonin inhibits tumor growth in mice by suppressing PKM2-mediated aerobic glycolysis.
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