ArticlePloS one2014
Pterostilbene-isothiocyanate conjugate suppresses growth of prostate cancer cells irrespective of androgen receptor status.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.
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Who cites it
19 citing papers in PubMed, 1 synthesis or guideline pooled it, 35 citations in OpenAlex.
- Dietary polyphenols in prevention and treatment of prostate cancer.International journal of molecular sciences · 2015Pooled it
- Isothiocyanates in Cancer Therapeutics - A Molecular Perspective.Chemistry & biodiversity · 2026Review
- Targeting Prostate Cancer Metabolism Through Transcriptional and Epigenetic Modulation: A Multi-Target Approach to Therapeutic Innovation.International journal of molecular sciences · 2025Review
- Gnetin C in Cancer and Other Diseases: What Do We Know So Far?Nutrients · 2025Review
- Advances in antitumor effects of pterostilbene and its derivatives.Future medicinal chemistry · 2025Review
- Phytochemical and Biological Investigations of Crude Extracts ofPharmaceuticals (Basel, Switzerland) · 2024Article
- Inflammation in Prostate Cancer: Exploring the Promising Role of Phenolic Compounds as an Innovative Therapeutic Approach.Biomedicines · 2023Review
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- Involvement of Cdkal1 in the etiology of type 2 diabetes mellitus and microvascular diabetic complications: a review.Journal of diabetes and metabolic disorders · 2022Review
- Metastasis-associated protein 1-mediated antitumor and anticancer activity of dietary stilbenes for prostate cancer chemoprevention and therapy.Seminars in cancer biology · 2022Review
- Suppressive Effect and Molecular Mechanism ofCancers · 2021Article
- Transepithelial Anti-Neuroblastoma Response to Kale among Four Vegetable Juices Using In Vitro Model Co-Culture System.Nutrients · 2021Article
- Targeted bioimaging and sensing of folate receptor-positive cancer cells using folic acid-conjugated sulfur-doped graphene quantum dots.Mikrochimica acta · 2020Article
- Pterostilbene, An Active Constituent of Blueberries, Suppresses Proliferation Potential of Human CholangiocarcinomaFrontiers in pharmacology · 2019Article
- Pterostilbene Suppresses Ovarian Cancer Growth via Induction of Apoptosis and Blockade of Cell Cycle Progression Involving Inhibition of the STAT3 Pathway.International journal of molecular sciences · 2018Article
- Pterostilbene modulates the suppression of multidrug resistance protein 1 and triggers autophagic and apoptotic mechanisms in cisplatin-resistant human oral cancer CAR cells via AKT signaling.International journal of oncology · 2018Article
- Apoptotic and Nonapoptotic Activities of Pterostilbene against Cancer.International journal of molecular sciences · 2018Review
- Anticancer activities of pterostilbene-isothiocyanate conjugate in breast cancer cells: involvement of PPARγ.PloS one · 2014Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Chemotherapy and anti-hormonal therapies are the most common treatments for non-organ-confined prostate cancer (PCa). However, the effectiveness of these therapies is limited, thus necessitating the development of alternative approaches. The present study focused on analyzing the role of pterostilbene (PTER)-isothiocyanate (ITC) conjugate--a novel class of hybrid compound synthesized by appending an ITC moiety on PTER backbone--in regulating the functions of androgen receptor (AR), thereby causing apoptosis of PCa cells. The conjugate molecule caused 50% growth inhibition (IC50) at 40 ± 1.12 and 45 ± 1.50 μM in AR positive (LNCaP) and negative (PC-3) cells, respectively. The reduced proliferation of PC-3 as well as LNCaP cells by conjugate correlated with accumulation of cells in G2/M phase and induction of caspase dependent apoptosis. Both PI3K/Akt and MAPK/ERK pathways played an important and differential role in conjugate-induced apoptosis of these PCa cells. While the inhibitor of Akt (A6730) or Akt-specific small interference RNA (siRNA) greatly sensitized PC-3 cells to conjugate-induced apoptosis, on the contrary, apoptosis was accelerated by inhibition of ERK (by PD98059 or ERK siRNA) in case of LNCaP cells, both ultimately culminating in the expression of cleaved caspase-3 protein. Moreover, anti-androgenic activity of the conjugate was mediated by decreased expression of AR and its co-activators (SRC-1, GRIP-1), thus interfering in their interactions with AR. All these data suggests that conjugate-induced inhibition of cell proliferation and induction of apoptosis are partly mediated by the down regulation of AR, Akt, and ERK signaling. These observations provide a rationale for devising novel therapeutic approaches for treating PCa by using conjugate alone or in combination with other therapeutics.
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Registered trials
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