ArticleCancer prevention research (Philadelphia, Pa.)2010
Disruption of androgen and estrogen receptor activity in prostate cancer by a novel dietary diterpene carnosol: implications for chemoprevention.
Article in Cancer prevention research (Philadelphia, Pa.), 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed, 86 citations in OpenAlex.
- Article
- Exploring the therapeutic role of carnosol in cancer: from molecular insights to clinical promise.Medical oncology (Northwood, London, England) · 2025Review
- Phytochemical Analysis and In Vivo Anticancer Effect ofNutrients · 2025Article
- Pharmacological assessment ofBioinformatics advances · 2025Article
- Cellular mechanisms mediating the anti-cancer effects of carnosol on gingiva carcinoma.Scientific reports · 2024Article
- Targeting Triple-Negative Breast Cancer by the Phytopolyphenol Carnosol: ROS-Dependent Mechanisms.Antioxidants (Basel, Switzerland) · 2023Review
- Carnosol induces the osteogenic differentiation of bone marrow-derived mesenchymal stem cellsThe Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2021Article
- Carnosic Acid Induces Antiproliferation and Anti-Metastatic Property of Esophageal Cancer Cells via MAPK Signaling Pathways.Journal of oncology · 2021Article
- Anticancer Properties of Carnosol: A Summary of in Vitro and In Vivo Evidence.Antioxidants (Basel, Switzerland) · 2020Review
- Anticancer Activity ofNutrients · 2020Review
- Mechanism of protective effect of carnosol on pig intestinal epithelial cells.International journal of clinical and experimental pathology · 2020Article
- Metabolomics Study Reveals Inhibition and Metabolic Dysregulation inFrontiers in microbiology · 2020Article
- Carnosol, a Natural Polyphenol, Inhibits Migration, Metastasis, and Tumor Growth of Breast Cancer via a ROS-Dependent Proteasome Degradation of STAT3.Frontiers in oncology · 2019Article
- Article
- Carnosol, a dietary diterpene from rosemary (Integrative molecular medicine · 2018Article
- Carnosol Increases Skeletal Muscle Cell Glucose Uptake via AMPK-Dependent GLUT4 Glucose Transporter Translocation.International journal of molecular sciences · 2018Article
- The Mechanisms of Carnosol in Chemoprevention of Ultraviolet B-Light-Induced Non-Melanoma Skin Cancer Formation.Scientific reports · 2018Article
- Bioassay-Guided Isolation of Anti-Candida Biofilm Compounds From Methanol Extracts of the Aerial Parts ofFrontiers in pharmacology · 2018Article
- Rosmarinic acid prevents fibrillization and diminishes vibrational modes associated to β sheet in tau protein linked to Alzheimer's disease.Journal of enzyme inhibition and medicinal chemistry · 2017Article
- Hypersensitivity of BRCA2 deficient cells to rosemary extract explained by weak PARP inhibitory activity.Scientific reports · 2017Article
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Emerging data are suggesting that estrogens, in addition to androgens, may also be contributing to the development of prostate cancer (PCa). In view of this notion, agents that target estrogens, in addition to androgens, may be a novel approach for PCa chemoprevention and treatment. Thus, the identification and development of nontoxic dietary agents capable of disrupting androgen receptor (AR) in addition to estrogen receptor (ER) could be extremely useful in the management of PCa. Through molecular modeling, we found that carnosol, a dietary diterpene, fits within the ligand-binding domain of both AR and ER-alpha. Using a time-resolved fluorescence resonance energy transfer assay, we found that carnosol interacts with both AR and ER-alpha and additional experiments confirmed that it functions as a receptor antagonist with no agonist effects. LNCaP, 22Rv1, and MCF7 cells treated with carnosol (20-40 mumol/L) showed decreased protein expression of AR and ER-alpha. Oral administration of carnosol at 30 mg/kg 5 days weekly for 28 days to 22Rv1 PCa xenografted mice suppressed tumor growth by 36% (P = 0.028) and was associated with a decrease in serum prostate-specific antigen by 26% (P = 0.0042). These properties make carnosol unique to any known antiandrogen or antiestrogen investigated thus far for the simultaneous disruption of AR and ER-alpha. We suggest that carnosol may be developed or chemically modified through more rigorous structure-activity relationship studies for a new class of investigational agents-a dual AR/ER modulator.
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Registered trials
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.