Antitumor activity of pyrvinium pamoate, 6‐(dimethylamino)‐2‐[2‐(2,5‐dimethyl‐1‐phenyl‐1 H‐pyrrol‐3‐yl)ethenyl]‐1‐methyl‐quinolinium pamoate salt, showing preferential cytotoxicity during glucose starvation
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An anthelminthic, pyrvinium pamoate (PP), 6‐(dimethylamino)‐2‐[2‐(2,5‐dimethyl‐1‐phenyl‐1 H‐pyrrol‐3‐yl)ethenyl]‐1‐methyl‐quino‐linium pamoate salt, has been found to be extremely toxic to PANC‐1 cells in glucose‐free medium, but not to be toxic to the same cells cultured in ordinary medium, Dulbecco's modified Eagle's medium (DMEM). It showed the same preferential toxicity for various cancer cell lines during glucose starvation. When 0.1 μg/ml PP was added to the medium, spheroid growth of human colon cancer cell line WiDr was strongly inhibited to a diameter of 750 μm, and this finding is consistent with the concept of anti‐austerity. PP was also found to exert antitumor activity against human pancreatic cancer cell line PANC‐1 in nude mice and SCID mice when it was administered subcutaneously or orally. Regarding the mechanism of PP action, inhibition of Akt phosphoryla‐tion, which has been found to be essential for the austerity mechanism, was observed in vitro and in vivo. These findings indicate that PP may be useful for anticancer therapy and that anti‐austerity therapy could be a novel strategy for anticancer therapy.
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Esumi et al. showed that pyrvinium pamoate is highly toxic to serum-starved PANC-1 cells and can clear PANC-1 xenografts in vivo.
“Esumi et al. [10] showed that PP is highly toxic to serum‐starved PANC‐1 cells and can clear PANC‐1 xenografts in vivo.”
From Pyrvinium Pamoate Alone and With Gemcitabine Exhibits Anti‐Pancreatic Cancer Activity in <scp>2D</scp> and <scp>3D</scp> Cell Culture Models (2024) · cites this paper as [10]
The Results (page unavailable) say PP was toxic to PANC-1 cells when glucose was depleted, regardless of serum, but had little effect when glucose was present; serum starvation alone was not the reported condition for strong toxicity. The SCID-mouse results (page unavailable) report suppressed tumor growth and describe residual tumors, not clearance of xenografts. (LLM, conf=0.90)
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Experimental — accuracy not yet measuredPP was previously shown to be effective under conditions that mimic the PDAC TME.
“PP was previously shown to be effective under conditions that mimic the PDAC TME [10, 11, 12]”
From Pyrvinium Pamoate Alone and With Gemcitabine Exhibits Anti‐Pancreatic Cancer Activity in <scp>2D</scp> and <scp>3D</scp> Cell Culture Models (2024) · cites this paper as [10]
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- Authors
- Esumi, H., Lu, J., Kurashima, Y., & Hanaoka, T.
- Affiliations
- National Cancer Center Hospital East (JP)
- Corresponding author
- Esumi, Hiroyasu
- Venue
- Cancer Science
- Publisher
- Wiley
- Published
- 2004-08
- Volume
- 95
- Issue
- 8
- Pages
- 685-690
- ISSN
- 1347-9032 (ISSN-L)
- 1349-7006
- PMC
- PMC11159109
- OpenAlex
- W1968162861
- Cited by
- 127
- References
- 2
- Citations by year
- 2025: 3 · 2024: 6 · 2023: 1 · 2022: 8 · 2021: 7 · 2020: 9 · 2019: 10 · 2018: 7 · 2017: 8 · 2016: 3 · 2015: 12 · 2014: 5 · 2013: 11 · 2012: 10
- FWCI
- 0.56
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Cancer Science (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Hypoxia, and Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Toxicology › Bioactive Compounds and Antitumor Agents
- Keywords
- pyrvinium pamoate, anthelmintic repurposing, glucose deprivation, pancreatic cancer, colon cancer, PANC-1 cells, WiDr cells, anticancer activity, anticancer drug discovery
- MeSH terms
- Animals, Cell Division, Colonic Neoplasms, Glucose, Humans, Immunohistochemistry, Mice, Nude, Pancreatic Neoplasms, Phosphorylation, Proto-Oncogene Proteins, Pyrvinium Compounds, Tumor Cells, Cultured, Protein Serine-Threonine Kinases, Cell Culture Techniques, Cell Size, Proto-Oncogene Proteins c-akt, Mice
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