ArticleEuropean journal of medical research2023
Luteolin inhibits A549 cells proliferation and migration by down-regulating androgen receptors.
Article in European journal of medical research, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 13 citations in OpenAlex.
- Protective Effects of Luteolin Against Cisplatin-Induced Hepatic and Renal Toxicity: Biochemical and Cellular Evidence.Journal of biochemical and molecular toxicology · 2026Article
- Luteolin as a Cancer Therapeutic: From Preclinical Evidence to Translational Potential.Chemistry & biodiversity · 2026Review
- Potential Efficacy of Luteolin in Cutaneous Squamous Cell Carcinoma: A Combined In Vitro and In Vivo Study.Biomolecules · 2026Article
- Testosterone and Androgen Receptor in Cancers with Significant Sex Dimorphism in Incidence Rates and Survival.Cancers · 2025Review
- Transcription factors and hormone receptors: Sex‑specific targets for cancer therapy (Review).Oncology letters · 2025Review
- Luteolin: exploring its therapeutic potential and molecular mechanisms in pulmonary diseases.Frontiers in pharmacology · 2025Review
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Authors and funding
7 authors at 5 institutions in 1 country.
Funding
Abstract
backgroundYi Fei Qing Hua Granules (YQG) is a traditional Chinese herbal medicine with the effects of inhibiting the proliferation of lung cancer cells. Luteolin is one of the active compounds of YQG. Luteolin is a common flavonoid extracted from natural herbs and it can promote cancer cells apoptosis has been reported. However, the underlying molecular mechanism and effects of luteolin on human lung cancer needs to be validated.
methodsMolecular docking, network pharmacology methods and quantitative structure-activity relationship (QSAR) model were used to identify the active components of YQG and their possible mechanisms of action. Western blot analysis was used to measure AR expression in A549 cells. Cell migration assays were used to detect A549 cells proliferation transfected by AR plasmid and AR mutation plasmid, respectively.
resultsTCMSP search results revealed that there are 182 active compounds in YQG, which correspond to 232 target genes. Sixty-one genes were overlapping genes in the 2 datasets of TCMSP and GeneCards. Through bioinformatics tagging of these overlapping genes, a total of 1,951 GO functional tagging analysis and 133 KEGG pathways were obtained. Through molecular docking technology and QSAR model verification, the multi-target active compound luteolin was screened out as one of the active components of YQG for in vitro verification. Androgen receptor (AR) was the hub protein with the highest docking score of luteolin. Western blot showed that luteolin could inhibit AR protein expression in lung cancer cell line A549. After the phosphorylation site of AR protein 877 was inactivated, the ability of luteolin to inhibit the proliferation of lung cancer cells was weakened. Luteolin significantly inhibited the growth of A549 xenogeneic tumors at day 25 and 28 and inhibited the expression of AR.
conclusionIn this study, we have explored luteolin as one of the active components of YQG, and may inhibit the proliferation and migration of A549 cells by decreasing the expression of AR and the regulation of phosphorylation at AR-binding sites.
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