ArticleMolecules (Basel, Switzerland)2021
Acacetin Inhibits the Growth of STAT3-Activated DU145 Prostate Cancer Cells by Directly Binding to Signal Transducer and Activator of Transcription 3 (STAT3).
Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 29 citations in OpenAlex.
- Recent Progress on Polyphenols of Malaysian Honey and Their Molecular Mechanism Pathways in Cancer-A Comprehensive Review.International journal of molecular sciences · 2026Review
- Prostate Cancer, JAK/STAT3 Dysregulation, and Flavonoids: Is There a Possible Link?International journal of molecular sciences · 2026Review
- Acacetin Attenuates Lysophosphatidylcholine-Induced Vascular Smooth Muscle Cell Injury via Sirt1-Nrf2/p62 Signaling Axis.Biomedicines · 2026Article
- Molecular Mechanism Discovery of Acacetin Against Cancers: Insights from Network Pharmacology and Molecular Docking.International journal of molecular sciences · 2025Review
- Exploring the molecular mechanism of Xiao Ji (Asian biomedicine : research, reviews and news · 2025Article
- Identification of Flavonoid-based Hypoxia-inducible Factor-2 Alpha Inhibitors for the Treatment of Breast Cancer-Anti-cancer agents in medicinal chemistry · 2025Article
- Acacetin, a Natural Flavone with Potential in Improving Liver Disease Based on Its Anti-Inflammation, Anti-Cancer, Anti-Infection and Other Effects.Molecules (Basel, Switzerland) · 2024Review
- Effect of acacetin on inhibition of apoptosis inWorld journal of gastrointestinal oncology · 2024Article
- Review
- Flavonoids fromADMET & DMPK · 2024Review
- Targeting PI3K/Akt signaling in prostate cancer therapy.Journal of cell communication and signaling · 2023Review
- [Therapeutic mechanism of Shenbing Decoction Ⅲ for renal fibrosis in chronic kidney disease: a study with network pharmacology, molecular docking and validation in rats].Nan fang yi ke da xue xue bao = Journal of Southern Medical University · 2023Article
- Flavones: The Apoptosis in Prostate Cancer of Three Flavones Selected as Therapeutic Candidate Models.International journal of molecular sciences · 2023Review
- Acacetin exerts antitumor effects on gastric cancer by targeting EGFR.Frontiers in pharmacology · 2023Article
- Nitidine chloride induces caspase 3/GSDME-dependent pyroptosis by inhibting PI3K/Akt pathway in lung cancer.Chinese medicine · 2022Article
- Review
- Flavones: Six Selected Flavones and Their Related Signaling Pathways That Induce Apoptosis in Cancer.International journal of molecular sciences · 2022Review
- From Therapy Resistance to Targeted Therapies in Prostate Cancer.Frontiers in oncology · 2022Review
- Targeting Oxidative Stress and Inflammation in Intervertebral Disc Degeneration: Therapeutic Perspectives of Phytochemicals.Frontiers in pharmacology · 2022Review
- Effects of Acacetin on the Pharmacokinetics of Diazepam in vivo and in vitro.Iranian journal of pharmaceutical research : IJPRArticle
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Signal transducer and activator of transcription 3 (STAT3) plays a critical role in the formation and growth of human cancer. Therefore, STAT3 is a therapeutic target for cancer drug discovery. Acacetin, a flavone present in various plants, inhibits constitutive and inducible STAT3 activation in STAT3-activated DU145 prostate cancer cells. Acacetin inhibits STAT3 activity by directly binding to STAT3, which we confirmed by a pull-down assay with a biotinylated compound and two level-free methods, namely, a drug affinity responsive target stability (DARTS) experiment and a cellular thermal shift assay (CETSA). Acacetin inhibits STAT3 phosphorylation at the tyrosine 705 residue and nuclear translocation in DU145 cells, which leads to the downregulation of STAT3 target genes. Acacetin then induces apoptosis in a time-dependent manner. Interestingly, acacetin induces the production of reactive oxygen species (ROS) that are not involved in the acacetin-induced inhibition of STAT3 activation because the suppressed p-STAT3 level is not rescued by treatment with GSH or NAC, which are general ROS inhibitors. We also found that acacetin inhibits tumor growth in xenografted nude mice. These results suggest that acacetin, as a STAT3 inhibitor, could be a possible drug candidate for targeting STAT3 for the treatment of cancer in humans.
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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.