ArticleClinical cancer research : an official journal of the American Association for Cancer Research2011
Lupeol, a novel androgen receptor inhibitor: implications in prostate cancer therapy.
Article in Clinical cancer research : an official journal of the American Association for Cancer Research, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
30 citing papers in PubMed, 96 citations in OpenAlex.
- Exploring the therapeutic potential of Lupeol isolated from Ochrosia elliptica Labill. leaves in polycystic ovarian syndrome.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Nano-phytochemical-based formulations as promising opportunities for prostate cancer therapy and management: a comprehensive narrative review.Medical oncology (Northwood, London, England) · 2025Review
- Function-Oriented Synthesis of Pentacyclic Triterpenoids and Discovery of anOrganic letters · 2024Article
- Effects of lupeol and flutamide on experimentally-induced polycystic ovary syndrome in mice.Iranian journal of basic medical sciences · 2024Article
- Molecular Insight into Prostate Cancer: Preventive Role of Selective Bioactive Molecules.Life (Basel, Switzerland) · 2023Review
- Neolamarckia cadamba (Roxb.) Bosser (Rubiaceae) extracts: promising prospects for anticancer and antibacterial potential through in vitro and in silico studies.Medical oncology (Northwood, London, England) · 2023Article
- Acetyl-CoA Counteracts the Inhibitory Effect of Antiandrogens on Androgen Receptor Signaling in Prostate Cancer Cells.Cancers · 2022Article
- Lupeol synergizes with doxorubicin to induce anti-proliferative and apoptotic effects on breast cancer cells.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2022Article
- Technologies for Solubility, Dissolution and Permeation Enhancement of Natural Compounds.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Isolation and HPLC Quantitative Determination of 5α-Reductase Inhibitors fromMolecules (Basel, Switzerland) · 2022Article
- AR imposes different effects on ZFHX3 transcription depending on androgen status in prostate cancer cells.Journal of cellular and molecular medicine · 2022Article
- Role of lupeol in chemosensitizing therapy-resistant prostate cancer cells by targeting MYC, β-catenin and c-FLIP: in silico and in vitro studies.In silico pharmacology · 2022Article
- Phytochemicals With Anti 5-alpha-reductase Activity: A Prospective For Prostate Cancer Treatment.F1000Research · 2021Review
- New Tailored RNA-Targeted Organometallic Drug Candidates against Huh7 (Liver) and Du145 (Prostate) Cancer Cell Lines.ACS omega · 2020Article
- Natural Compounds in Sex Hormone-Dependent Cancers: The Role of Triterpenes as Therapeutic Agents.Frontiers in endocrinology · 2020Review
- Deep insights into the response of human cervical carcinoma cells to a new cyano enone-bearing triterpenoid soloxolone methyl: a transcriptome analysis.Oncotarget · 2019Article
- Groove Binding of Vanillin and Ethyl Vanillin to Calf Thymus DNA.Journal of fluorescence · 2017Article
- Protective Effect of Lupeol Against Lipopolysaccharide-Induced Neuroinflammation via the p38/c-Jun N-Terminal Kinase Pathway in the Adult Mouse Brain.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2016Article
- In vitro evaluation of anticancer potentials of lupeol isolated from Elephantopus scaber L. on MCF-7 cell line.Journal of advanced pharmaceutical technology & research · 2014Article
- Negative regulation of signal transducer and activator of transcription-3 signalling cascade by lupeol inhibits growth and induces apoptosis in hepatocellular carcinoma cells.British journal of cancer · 2014Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
purposeConventional therapies to treat prostate cancer (CaP) of androgen-dependent phenotype (ADPC) and castration-resistant phenotype (CRPC) are deficient in outcome which has necessitated a need to identify those agents that could target AR for both disease types. We provide mechanism-based evidence that lupeol (Lup-20(29)-en-3b-ol) is a potent inhibitor of androgen receptor (AR) in vitro and in vivo. EXPERIMENTAL
designNormal prostate epithelial cell (RWPE-1), LAPC4 (wild functional AR/ADPC), LNCaP (mutant functional/AR/ADPC), and C4-2b (mutant functional/AR/CRPC) cells were used to test the anti-AR activity of lupeol. Cells grown under androgen-rich environment and treated with lupeol were tested for proliferation, AR transcriptional activity, AR competitive ligand binding, AR-DNA binding, and AR-ARE/target gene binding. Furthermore, in silico molecular modeling for lupeol-AR binding was done. Athymic mice bearing C4-2b and LNCaP cell-originated tumors were treated intraperitoneally with lupeol (40 mg/kg; 3 times/wk) and tumor growth and surrogate biomarkers were evaluated. To assess bioavailability, lupeol serum levels were measured.
resultsLupeol significantly inhibited R1881 (androgen analogue) induced (i) transcriptional activity of AR and (ii) expression of PSA. Lupeol (i) competed antagonistically with androgen for AR, (ii) blocked the binding of AR to AR-responsive genes including PSA, TIPARP, SGK, and IL-6, and (iii) inhibited the recruitment of RNA Pol II to target genes. Lupeol sensitized CRPC cells to antihormone therapy. High-performance liquid chromatography analysis showed that lupeol is bioavailable to mice. Lupeol inhibited the tumorigenicity of both ADPC and CRPC cells in animals. Serum and tumor tissues exhibited reduced PSA levels.
conclusionLupeol, an effective AR inhibitor, could be developed as a potential agent to treat human CaP.
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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.