Antineoplastic activity of idazoxan hydrochloride

Purpose Idazoxan hydrochloride (IDA) is a 241 molecular weight imidazoline and adrenoreceptor ligand. It binds to mitochondrial membranes and promotes apoptosis of pancreatic beta cells. Since IDA has not been tested against tumor cells, the purpose of our study was to determine if IDA has antineopl...

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Bibliographic Details
Published in:Cancer chemotherapy and pharmacology 2009-11, Vol.64 (6), p.1157-1163
Main Authors: Eilon, G. F., Weisenthal, L., Stupecky, M., Landucci, G., Slater, L. M.
Format: Article
Language:English
Subjects:
Animals
Annexin A5 - metabolism
Antineoplastic agents
Antineoplastic Agents - pharmacology
Apoptosis - drug effects
Biological and medical sciences
Calreticulin - metabolism
Cancer Research
Carcinoma, Lewis Lung - pathology
Cell Line, Tumor
Cell Survival - drug effects
Dose-Response Relationship, Drug
Humans
Idazoxan - pharmacology
Male
Medical sciences
Medicine
Medicine & Public Health
Mice
Neoplasms - pathology
Oncology
Original
Original Article
Pharmacology. Drug treatments
Pharmacology/Toxicology
Prostatic Neoplasms - pathology
Tumor Cells, Cultured
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Summary:Purpose Idazoxan hydrochloride (IDA) is a 241 molecular weight imidazoline and adrenoreceptor ligand. It binds to mitochondrial membranes and promotes apoptosis of pancreatic beta cells. Since IDA has not been tested against tumor cells, the purpose of our study was to determine if IDA has antineoplastic activity. Methods We used the conversion of a soluble tetrazolium salt to an insoluble formazan precipitate and differential staining cytotoxicity assays to determine if IDA was cytotoxic to cell lines of murine lung cancer and human prostate cancer, as well as to a variety of fresh human tumor samples. We used flow cytometry to analyze cell death and calreticulin expression. Results IDA is cytotoxic to both cell lines and against aliquots of specimens of breast, gastric, lung, ovarian and prostate cancers as well as non-Hodgkin’s lymphoma. It produces apoptotic cell death and promotes calreticulin expression, suggesting that IDA might be immunomodulatory in vivo. Conclusion We anticipate that IDA will be clinically useful in cancer treatment.
ISSN:0344-5704
1432-0843
DOI:10.1007/s00280-009-0978-9