ArticleCancer medicine2022
Ursolic acid silences CYP19A1/aromatase to suppress gastric cancer growth.
Article in Cancer medicine, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13 citing papers in PubMed, 33 citations in OpenAlex.
- Identification of the CYP19A1-GPER1 axis as a critical oncogenic driver in hepatocellular carcinoma via AKT activation.Journal of translational medicine · 2026Article
- Immune and Tumor Microenvironment Mechanisms ofCancers · 2026Review
- Nutritional Impact on Breast Cancer in Menopausal and Post-Menopausal Patients Treated with Aromatase Inhibitors.Cancers · 2025Review
- Ursolic acid suppresses gastric cancer by targeting the miR-27a-3p/Wnt/β-catenin signaling axis.European journal of medical research · 2025Article
- Review
- Farrerol inhibits proliferation and migration of colorectal cancer via the VEGF signaling pathway: evidence from network pharmacology, molecular docking, molecular dynamics simulation, andFrontiers in pharmacology · 2025Article
- Ursolic Acid induces ferroptosis by affecting redox balance and FADS2-mediated unsaturated fatty acid synthesis in Non-Small Cell Lung Cancer.Journal of Cancer · 2025Article
- CYP19A1 Silencing Inhibits Cell Proliferation and Endoplasmic Reticulum Stress in Stomach Adenocarcinoma.Oncology research · 2025Article
- CYP19A1 regulates chemoresistance in colorectal cancer through modulation of estrogen biosynthesis and mitochondrial function.Cancer & metabolism · 2024Article
- Integrated analysis of single-cell and bulk RNA-sequencing reveals a novel signature based on NK cell marker genes to predict prognosis and immunotherapy response in gastric cancer.Scientific reports · 2024Article
- Article
- A Novel 3D Culture Scaffold to Shorten Development Time for Multicellular Tumor Spheroids.International journal of molecular sciences · 2022Article
- Ursolic acid silences CYP19A1/aromatase to suppress gastric cancer growth.Cancer medicine · 2022Article
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
introductionGastric cancer (GCa) is a malignancy with few effective treatments. Ursolic acid (UA), a bioactive triterpenoid enriched in Hedyotis diffusa Willd, known to suppress GCa without identified target. CYP19A1 (cytochrome P450 family 19A1; also known as aromatase, Ar) was correlated to GCa prognosis. Relatedly, Ar silencers, which halt the expression of Ar exhibited anti-GCa effects in experimental models, are currently being investigated.
methodThe docking simulation score of UA was compared with Ar inhibitors, e.g., letrozole, exemestane, in Ar protein crystallization. Hedyotis diffusa Willd ethanol extract, UA, or 5-fluracil were applied onto AGS, SC-M1, MKN45 GCa cells for cancer inhibition tests. Immunoblot for measuring gene expressions upon drug treatments, or gene knockdown/overexpression. Treatments were also applied in a MKN45 implantation tumor model. A web-based GCa cohort for Ar expression association with prognosis was performed.
resultThe ethanol extracts of Hedyotis diffusa Willd, enrich with UA, exhibited cytotoxic activity against GCa cells. Molecular docking simulations with the 3D Ar structure revealed an excellent fitting score for UA. UA increase cytotoxic, and suppressed colony, in addition to its Ar silencing capacity. Moreover, UA synergistically facilitated 5-FU, (a standard GCa treatment) regimen in vitro. Consistent with those results, adding estradiol did not reverse the cancer-suppressing effects of UA, which confirmed UA acts as an Ar silencer. Furthermore, UA exhibited tumor-suppressing index (TSI) score of 90% over a 6-week treatment term when used for single dosing in xenograft tumor model. In the clinical setting, Ar expression was found to be higher in GCa tumors than normal parental tissue from the TCGA (The Cancer Genome Atlas) cohort, while high Ar expression associated with poor prognosis. Together, the results indicate UA could be used to treat GCa by silencing Ar expression in GCa. Hedyotis diffusa Willd ethanol extract could be an functional food supplements.
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