ArticleBMC pharmacology & toxicology2020
Inhibition of PI3K/AKT molecular pathway mediated by membrane estrogen receptor GPER accounts for cryptotanshinone induced antiproliferative effect on breast cancer SKBR-3 cells.
Article in BMC pharmacology & toxicology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 25 citations in OpenAlex.
- Cryptotanshinone Directly Targets MEK1 to Inhibit Migration and Invasion of Breast Cancer Cells Through Down-Regulating ERK/EMT Axis.Phytotherapy research : PTR · 2026Article
- Preclinical approach of two novel tetrahydroquinoline derivatives targeting GPER and Bcl-2 for anti-glioblastoma therapy.Scientific reports · 2025Article
- A Review of Cryptotanshinone and its Nanoformulation in Cancer Therapy.Anti-cancer agents in medicinal chemistry · 2025Review
- Clinically proven natural products against breast cancer, with mechanistic insights.Oncology research · 2025Review
- Pharmacological Mechanisms of Cryptotanshinone: Recent Advances in Cardiovascular, Cancer, and Neurological Disease Applications.Drug design, development and therapy · 2024Review
- Tanshinone IIA Inhibits Triple-Negative Breast Cancer Cells MDA-MB-231 via G Protein-Coupled Estrogen Receptor- (GPER-) Dependent Signaling Pathway.Disease markers · 2023Article
- Tanshinone IIA and hepatocellular carcinoma: A potential therapeutic drug.Frontiers in oncology · 2023Review
- Heart Failure in Menopause: Treatment and New Approaches.International journal of molecular sciences · 2022Review
- Molecular Mechanism of Tanshinone against Prostate Cancer.Molecules (Basel, Switzerland) · 2022Review
- Assessment of G Protein-Coupled Oestrogen Receptor Expression in Normal and Neoplastic Human Tissues Using a Novel Rabbit Monoclonal Antibody.International journal of molecular sciences · 2022Article
- Article
- Anticancer potential of cryptotanshinone on breast cancer treatment; A narrative review.Frontiers in pharmacology · 2022Review
- Electro-Acupuncture Regulates Metabolic Disorders of the Liver and Kidney in Premature Ovarian Failure Mice.Frontiers in endocrinology · 2022Article
- Review
- From Menopause to Neurodegeneration-Molecular Basis and Potential Therapy.International journal of molecular sciences · 2021Review
- Therapeutic Perspectives on the Modulation of G-Protein Coupled Estrogen Receptor, GPER, Function.Frontiers in endocrinology · 2020Review
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
backgroundBreast cancer is the most frequently diagnosed malignancy among women and the second leading cause of cancer death worldwide. Among which nuclear estrogen receptor (nER) negative breast cancer is always with much poor prognosis. Recently, membrane G protein coupled estrogen receptor (GPER), a newly recognized estrogen receptor has been documented to take essential part in the development and treatment of breast cancer. The present study was designed to investigate the anti nER negative breast cancer effect of cryptotanshinone (CPT), an important active compound of traditional Chinese medicine Danshen and its possible molecular pathway.
methodsThe following in vitro tests were performed in nER negative but GPER positive breast cancer SKBR-3 cells. The effect of CPT on cell proliferation rate and cell cycle distribution was evaluated by MTT cell viability test and flow cytometry assay respectively. The role of PI3K/AKT pathway and the mediated function of GPER were tested by western blot and immunofluorescence. Technique of gene silence and the specific GPER agonist G-1 and antagonist G-15 were employed in the experiments to further verify the function of GPER in mediating the anticancer role of CPT.
resultsThe results showed that proliferation of SKBR-3 cells could be blocked by CPT in a time and dose dependent manner. CPT could also exert antiproliferative activities by arresting cell cycle progression in G1 phase and down regulating the expression level of cyclin A, cyclin B, cyclin D and cyclin-dependent kinase 2 (CDK2). The antiproliferative effect of CPT was further enhanced by G-1 and attenuated by G-15. Results of western blot and immunofluorescence showed that expression of PI3K and p-AKT could be downregulated by CPT and such effects were mediated by GPER which were further demonstrated by gene silence test.
conclusionThe current study showed that the antiproliferative action of CPT on SKBR-3 cells was realized by inhibition of GPER mediated PI3K/AKT pathway. These findings provide further validation of GPER serving as useful therapeutic target.
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