ArticlePloS one2011
Guggulsterone targets smokeless tobacco induced PI3K/Akt pathway in head and neck cancer cells.
Article in PloS one, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 34 citations in OpenAlex.
- Phytochemicals Modulating Redox Homeostasis in Head and Neck Cancer.Cell biochemistry and biophysics · 2026Review
- Article
- Molecular pathways modulated by phytochemicals in head and neck cancer.Journal of cell communication and signaling · 2023Review
- Potential of guggulsterone, a farnesoid X receptor antagonist, in the prevention and treatment of cancer.Exploration of targeted anti-tumor therapy · 2020Review
- Googling the Guggul (Commiphora and Boswellia) for Prevention of Chronic Diseases.Frontiers in pharmacology · 2018Review
- Potential therapeutic targets of Guggulsterone in cancer.Nutrition & metabolism · 2017Review
- Anticancer activity of pyrithione zinc in oral cancer cells identified in small molecule screens and xenograft model: Implications for oral cancer therapy.Molecular oncology · 2015Article
- Proteomic analysis of rosiglitazone and guggulsterone treated 3T3-L1 preadipocytes.Molecular and cellular biochemistry · 2013Article
- Article
- Guggulsterone enhances antitumor activity of gemcitabine in gallbladder cancer cells through suppression of NF-κB.Journal of cancer research and clinical oncology · 2012Article
- siRNA-mediated downregulation of TC21 sensitizes esophageal cancer cells to cisplatin.World journal of gastroenterology · 2012Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundEpidemiological association of head and neck cancer with smokeless tobacco (ST) emphasizes the need to unravel the molecular mechanisms implicated in cancer development, and identify pharmacologically safe agents for early intervention and prevention of disease recurrence. Guggulsterone (GS), a biosafe nutraceutical, inhibits the PI3K/Akt pathway that plays a critical role in HNSCC development. However, the potential of GS to suppress ST and nicotine (major component of ST) induced HNSCC remains unexplored. We hypothesized GS can abrogate the effects of ST and nicotine on apoptosis in HNSCC cells, in part by activation of PI3K/Akt pathway and its downstream targets, Bax and Bad. METHODS AND
resultsOur results showed ST and nicotine treatment resulted in activation of PI3K, PDK1, Akt, and its downstream proteins--Raf, GSK3β and pS6 while GS induced a time dependent decrease in activation of PI3K/Akt pathway. ST and nicotine treatment also resulted in induction of Bad and Bax phosphorylation, increased the association of Bad with 14-3-3ζresulting in its sequestration in the cytoplasm of head and neck cancer cells, thus blocking its pro-apoptotic function. Notably, GS pre-treatment inhibited ST/nicotine induced activation of PI3K/Akt pathway, and inhibited the Akt mediated phosphorylation of Bax and Bad.
conclusionsIn conclusion, GS treatment not only inhibited proliferation, but also induced apoptosis by abrogating the effects of ST/nicotine on PI3K/Akt pathway in head and neck cancer cells. These findings provide a rationale for designing future studies to evaluate the chemopreventive potential of GS in ST/nicotine associated head and neck cancer.
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