ArticlePloS one2011
Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings.
Article in PloS one, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 81 citations in OpenAlex.
- Gut microbial metabolites targeting JUN in renal cell carcinoma via IL-17 signaling pathway: network pharmacology approach.Molecular diversity · 2026Article
- Icaritin ameliorates mitochondrial dysfunction and autophagy impairment in cellular models of Alzheimer's disease.Frontiers in aging neuroscience · 2026Article
- Genome-wide identification of the phenylalanine ammonia-lyase gene from Epimedium Pubescens Maxim. (Berberidaceae): novel insight into the evolution of the PAL gene family.BMC plant biology · 2024Article
- Icaritin greatly attenuates β-amyloid-induced toxicity in vivo.CNS neuroscience & therapeutics · 2024Article
- Transplant oncology and anti-cancer immunosuppressants.Frontiers in immunology · 2024Review
- N-Ethyl-N-Nitrosourea Induced Leukaemia in a Mouse Model: Protective Effect of Icaritin via Inhibition of IL-6/JAK2/STAT3 Pathway Causes Apoptosis.Journal of inflammation research · 2024Article
- Advancements in the Biotransformation and Biosynthesis of the Primary Active Flavonoids Derived fromMolecules (Basel, Switzerland) · 2023Review
- Time-series transcriptome provides insights into the gene regulation network involved in the icariin-flavonoid metabolism during the leaf development ofFrontiers in plant science · 2023Article
- Icaritin inhibits PLK1 to activate DNA damage response in NK/T cell lymphoma and increases sensitivity to GELOX regime.Molecular therapy oncolytics · 2022Article
- Cabozantinib promotes erythroid differentiation in K562 erythroleukemia cells through global changes in gene expression and JNK activation.Cancer gene therapy · 2022Article
- Research Progress of Natural Small-Molecule Compounds Related to Tumor Differentiation.Molecules (Basel, Switzerland) · 2022Review
- Flavonoids against non-physiologic inflammation attributed to cancer initiation, development, and progression-3PM pathways.The EPMA journal · 2021Review
- Folic Acid Deficiency Enhances the Tyr705 and Ser727 Phosphorylation of Mitochondrial STAT3 in In Vivo and In Vitro Models of Ischemic Stroke.Translational stroke research · 2021Article
- Analysis of Clinical Trials of New Drugs for Liver Diseases in China.Drug design, development and therapy · 2021Review
- Icaritin induces cellular senescence by accumulating the ROS production and regulation of the Jak2/Stat3/p21 pathway in imatinib-resistant, chronic myeloid leukemia cells.American journal of translational research · 2021Article
- A comparative study on theDrug delivery · 2020Article
- Icaritin-induced immunomodulatory efficacy in advanced hepatitis B virus-related hepatocellular carcinoma: Immunodynamic biomarkers and overall survival.Cancer science · 2020Article
- Icaritin enhances the efficacy of cetuximab against triple-negative breast cancer cells.Oncology letters · 2020Article
- Human BCR/ABL1 induces chronic myeloid leukemia-like disease in zebrafish.Haematologica · 2020Article
- Induction of ROS and DNA damage-dependent senescence by icaritin contributes to its antitumor activity in hepatocellular carcinoma cells.Pharmaceutical biology · 2019Article
Corrections and comments
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Authors and funding
14 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo explore the effects of Icaritin on chronic myeloid leukemia (CML) cells and underlying mechanisms.
methodCML cells were incubated with various concentration of Icaritin for 48 hours, the cell proliferation was analyzed by MTT and the apoptosis was assessed with Annexin V and Hoechst 33258 staining. Cell hemoglobinization was determined. Western blotting was used to evaluate the expressions of MAPK/ERK/JNK signal pathway and Jak-2/Phorpho-Stat3/Phorsph-Akt network-related protein. NOD-SCID nude mice were applied to demonstrate the anti-leukemia effect of Icaritin in vivo.
resultsIcaritin potently inhibited proliferation of K562 cells (IC50 was 8 µM) and primary CML cells (IC50 was 13.4 µM for CML-CP and 18 µM for CML-BC), induced CML cells apoptosis and promoted the erythroid differentiation of K562 cells with time-dependent manner. Furthermore, Icaritin was able to suppress the growth of primary CD34+ leukemia cells (CML) and Imatinib-resistant cells, and to induce apoptosis. In mouse leukemia model, Icaritin could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells as effective as Imatinib without suppression of bone marrow. Icaritin could up-regulate phospho-JNK or phospho-C-Jun and down-regulate phospho-ERK, phospho-P-38, Jak-2, phospho-Stat3 and phospho-Akt expression with dose- or time-dependent manner. Icaritin had no influence both on c-Abl and phospho-c-Abl protein expression and mRNA levels of Bcr/Abl.
conclusionIcaritin from Chinese herb medicine may be a potential anti-CML agent with low adverse effect. The mechanism of anti-leukemia for Icaritin is involved in the regulation of Bcr/Abl downstream signaling. Icaritin may be useful for an alternative therapeutic choice of Imatinib-resistant forms of CML.
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