ArticleFrontiers in pharmacology2020
Rhein Derivative 4F Inhibits the Malignant Phenotype of Breast Cancer by Downregulating Rac1 Protein.
Article in Frontiers in pharmacology, 2020. 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, 27 citations in OpenAlex.
- Rhein and its derivatives: potential anti-tumor drugs and corresponding targeted mechanism.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2026Review
- Emodin and the Anthraquinone Scaffold: Therapeutic Promise and Strategies to Overcome Translational Barriers.Molecules (Basel, Switzerland) · 2026Review
- The effects of mechanical stimulation on the morphology and function of spinal ligament cells.BMC musculoskeletal disorders · 2025Article
- The Construction of ceRNA Regulatory Network Unraveled Prognostic Biomarkers and Repositioned Drug Candidates for the Management of Pancreatic Ductal Adenocarcinoma.Current issues in molecular biology · 2025Article
- From Nature to Nanomedicine: Enhancing the Antitumor Efficacy of Rhein, Curcumin, and Resveratrol.Medicina (Kaunas, Lithuania) · 2025Review
- Structural Dynamics of Rho GTPases.Journal of molecular biology · 2025Review
- Palindrome-mediated DNA nanotubes with cell-specific aptamers to improve targeted antitumor effects and reduce toxicity on non-small cell lung cancer.Science China. Life sciences · 2025Article
- Bibliometric analysis of rhein in the treatment of tumors.Frontiers in oncology · 2025Article
- Rhein: An Updated Review Concerning Its Biological Activity, Pharmacokinetics, Structure Optimization, and Future Pharmaceutical Applications.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Cellular Traction Force Holds the Potential as a Drug Testing Readout for In Vitro Cancer Metastasis.Cellular and molecular bioengineering · 2024Article
- Molecular dynamic simulation reveals the inhibiting impact of Rhein on wild-type and P29S-mutated Rac1.Frontiers in molecular biosciences · 2024Article
- Molecular docking analysis of breast cancer target RAC1B with ligands.Bioinformation · 2024Article
- Therapeutic Potential of 1,8-Dihydroanthraquinone Derivatives for Breast Cancer.International journal of molecular sciences · 2023Review
- Molecular Targets for Nonhormonal Treatment Based on a Multistep Process of Adenomyosis Development.Reproductive sciences (Thousand Oaks, Calif.) · 2023Review
- Dahuang-Taoren, a botanical drug combination, ameliorates adenomyosisFrontiers in pharmacology · 2023Article
- Rhein promotes the proliferation of keratinocytes by targeting oestrogen receptors for skin ulcer treatment.BMC complementary medicine and therapies · 2022Article
- Article
- Drug Discovery of Plausible Lead Natural Compounds That Target the Insulin Signaling Pathway: Bioinformatics Approaches.Evidence-based complementary and alternative medicine : eCAM · 2022Review
- Immune Effect of Active Components of Traditional Chinese Medicine on Triple-Negative Breast Cancer.Frontiers in pharmacology · 2021Review
- Functional Metabolomics Analysis Elucidating the Metabolic Biomarker and Key Pathway Change Associated With the Chronic Glomerulonephritis and Revealing Action Mechanism of Rhein.Frontiers in pharmacology · 2020Article
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundTriple-negative breast cancer is a common malignant tumor with unfavorable prognosis affecting women worldwide; thus, there is an urgent need for novel therapeutic drugs with improved anti-tumor activity. Rac family small GTPase 1 (Rac1) plays an important role in malignant behavior and is a promising therapeutic target. We reported an anthraquinone compound, Rhein, and its derivative, 4F, and investigated their downregulation effects on Rac1 in breast cancer cells
methodsThe inhibition of cell proliferation by derivative 4F was investigated in two breast cancer (MDA-MB-231 and MCF-7) and normal breast (MCF-10A) cell lines by cell counting kit-8 assay and growth curves. The role of 4F in cell migration and invasion and cytoskeletal change were assessed by Transwell chamber assay and F-actin staining, respectively. The affinity of Rhein and its derivative for Rac1 protein and the regulation of Rac1 promoter activity were evaluated by molecular docking software and luciferase reporter gene assay, respectively. Rac1 protein expression was determined by western blot assay.
resultsCompared to Rhein, derivative 4F more strongly inhibited breast cancer cell proliferation, migration, and invasion and also cause cytoskeletal changes like those in paclitaxel. Derivative 4F not only bound more stably to Rac1 but also inhibited Rac1 promoter activity in cells and downregulated Rac1 protein expression.
conclusionsRhein derivative 4F is a new anthraquinone compound with better anti-tumor activity than that of the lead compound Rhein in breast cancer. It down-regulated Rac1 expression and may be a small molecule inhibitor of Rac1.
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