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Itraconazole Inhibits Intracellular Cholesterol Trafficking and Decreases Phosphatidylserine Level in Cervical Cancer Cells
Abstract
BACKGROUND/AIM: Itraconazole shows anticancer activity in various types of cancer but its underlying mechanism is unclear. We investigated the effect of itraconazole on membrane-associated lipids. MATERIALS AND METHODS: To investigate the influences of itraconazole on cholesterol trafficking, cervical cancer CaSki cells were cultured with itraconazole and analyzed by Filipin staining followed by confocal microscopy. Effect on the glycerophospholipid profiles was analyzed by liquid chromatography/mass spectrometry (LC/MS). RESULTS: After itraconazole treatment, Filipin staining revealed cholesterol accumulation in the intracellular compartments, which was similar to the distribution after treatment of U18666A (cholesterol transport inhibitor). LC/MS analysis showed a significant decrease in phosphatidylserine levels and an increase in lysophosphatidylcholine levels in CaSki cells. CONCLUSION: Itraconazole inhibited cholesterol trafficking and altered the phospholipid composition. Alterations in the cell membrane can potentiate the anticancer activity of itraconazole.
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ITZ changed the phospholipid makeup and prevented cholesterol from moving.
“ITZ changed the phospholipid makeup and prevented cholesterol from moving.”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [75]
Phosphatidylserine levels in CaSki cells significantly decreased, but lysophosphatidylcholine levels increased after ITZ.
“Phosphatidylserine levels in CaSki cells significantly decreased, but lysophosphatidylcholine levels increased, according to liquid chromatography/mass spectrometry (LC/MS) research.”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [75]
ITZ's anticancer action may be enhanced by modifications to the cell membrane.
“ITZ's anticancer action may be enhanced by modifications to the cell membrane.”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [75]
The distribution of cholesterol in intracellular compartments following ITZ treatment was comparable to that observed following treatment with U18666A.
“The distribution of cholesterol in the intracellular compartments following ITZ treatment was comparable to that observed following treatment with U18666A (cholesterol transport inhibitor), according to filipin staining.”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [75]
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Use of cholesterol metabolism for anti-cancer strategies
Ediriweera, M. K. (2022) · Drug Discovery Today · doi:10.1016/j.drudis.2022.103347 · Cited by 16
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Kulkarni, A. M., Gayam, P. K. R., Baby, B. T., & Aranjani, J. M. (2025) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2025.189279 · Cited by 9
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Wang, X., Cheng, Y., Tian, Y., Song, Z., He, Z., Shen, P., Wang, H., Luo, L., & Cui, R. (2022) · Research Square · doi:10.21203/rs.3.rs-1189067/v1 · Cited by 1
Marzi, M., Ghasemian, A., Ghanbariasad, A., Nournia, E., & Zarenezhad, E. (2026) · RSC Advances · doi:10.1039/d5ra09799a
Cimato, A. N., Degrossi, J., Facorro, G. B., & Sarrasague, M. M. M. (2025) · Respiratory Physiology & Neurobiology · doi:10.1016/j.resp.2025.104503
Metadata
- Authors
- ISONO, R., TSUBAMOTO, H., UEDA, T., TAKIMOTO, Y., INOUE, K., SAKATA, K., SHIBAHARA, H., & NISHIUMI, S.
- Affiliations
- Hyogo Medical University (JP)
- Venue
- Anticancer Research
- Published
- 2021-11
- Volume
- 41
- Issue
- 11
- Pages
- 5477-5480
- ISSN
- 0250-7005 (ISSN-L)
- 1791-7530
- OpenAlex
- W3210615253
- Cited by
- 5
- References
- 0
- Citations by year
- 2026: 1 · 2025: 2 · 2022: 2
- FWCI
- 0.20
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Anticancer Research (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Lipids, and Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Lipid Membrane Structure and Behavior
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Cholesterol and Lipid Metabolism
- Keywords
- itraconazole, cholesterol transport, phosphatidylserine, lysophosphatidylcholine, cervical cancer, CaSki cells, membrane lipids, anticancer mechanism, cholesterol accumulation, U18666A
- MeSH terms
- Antineoplastic Agents, Biological Transport, Uterine Cervical Neoplasms, Cholesterol, Female, Humans, Lysophosphatidylcholines, Phosphatidylserines, Itraconazole, Cell Line, Tumor
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