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Astemizole inhibits cell proliferation in human prostate tumorigenic cells expressing ether à-go-go-1 potassium
Gloria Bernal-Ramos1, Elisabeth Hernández-Gallegos2, Eunice Vera2
1Department of Genetics and Molecular Biology, Centro de Investigación y de Estudios Avanzados del I.P.N., Avenida Instituto Politécnico Nacional 2508, Mexico City 07360, Mexico.
Abstract:
Prostate cancer (PC) is the main cause of cancer mortality in men worldwide. Therefore, novel treatments for PC are needed. Ether à-go-go-1 (Eag1) potassium channels display oncogenic properties, and have been suggested as early tumor markers and therapeutic targets for different cancers. These channels are overexpressed in many human tumors including PC. Astemizole targets several molecules involved in cancer including Eag1 channels, histamine receptors and ABC transporters. Here we studied Eag1 mRNA expression and protein levels in the non-tumorigenic and non-invasive human prostate RWPE-1 cell line, and in the tumorigenic and highly invasive human prostate WPE1-NB26 cell lines. The effect of astemizole on cell proliferation and apoptosis was also studied. The human prostate cell lines RWPE-1 and WPE1-NB26 were cultured following the provider´s instructions. Eag1 mRNA expression and protein levels were studied by real time RT-PCR and immunocytochemistry, respectively. Cell proliferation and apoptosis were studied by a fluorescence AlamarBlue® assay and flow cytometry, respectively. No difference in Eag1 mRNA expression was observed between the cell lines. However, high Eag1 protein levels were observed in the invasive WPE1-NB26 cells, in contrast to the weak protein expression in RWPE-1 cells. Accordingly, astemizole decreased cell proliferation at nanomolar concentrations only in the invasive WPE1-NB26 cells. Our results suggest that astemizole may have clinical relevance for prostate cancer treatment in patients with high Eag1 protein levels.
Insights
Novel prostate cancer (PC) treatments are needed. Astemizole effectively reduced proliferation in invasive PC cells with high Ether à-go-go-1 (Eag1) protein levels, suggesting therapeutic potential.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Prostate cancer (PC) is a leading cause of cancer mortality in men globally, necessitating novel therapeutic strategies.
- Ether à-go-go-1 (Eag1) potassium channels are implicated in oncogenesis and are overexpressed in various human tumors, including PC.
- Astemizole is a drug known to target molecules involved in cancer, such as Eag1 channels, histamine receptors, and ABC transporters.
Purpose of the Study:
- To investigate Eag1 mRNA and protein expression in non-tumorigenic (RWPE-1) and invasive (WPE1-NB26) human prostate cell lines.
- To evaluate the effect of astemizole on the proliferation and apoptosis of these prostate cancer cell lines.
- To determine the potential of astemizole as a therapeutic agent for prostate cancer based on Eag1 expression.
Main Methods:
- Real-time RT-PCR was used to quantify Eag1 mRNA levels.
- Immunocytochemistry was employed to assess Eag1 protein expression.
- Cell proliferation was measured using a fluorescence AlamarBlue® assay, and apoptosis was analyzed by flow cytometry.
Main Results:
- Eag1 mRNA expression showed no significant difference between RWPE-1 and WPE1-NB26 cell lines.
- Invasive WPE1-NB26 cells exhibited high Eag1 protein levels, whereas non-tumorigenic RWPE-1 cells showed weak expression.
- Astemizole significantly decreased cell proliferation in WPE1-NB26 cells at nanomolar concentrations, but not in RWPE-1 cells.
Conclusions:
- Eag1 protein levels are elevated in invasive prostate cancer cells.
- Astemizole demonstrates anti-proliferative effects specifically in prostate cancer cells with high Eag1 protein expression.
- These findings suggest astemizole holds clinical relevance for treating prostate cancer patients with elevated Eag1 protein levels.
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Ethers can be prepared from organic compounds by various methods. Some of them are discussed below,
Preparation of Ethers by Alcohol Dehydration
In this method, in the presence of protic acids, alcohol dehydrates to produce alkenes and ethers under different conditions. For example, in the presence of sulphuric acid, dehydration of ethanol at 413 K yields ethoxyethane, whereas it yields ethene at 443 K.