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Statins Do Not Directly Inhibit the Activity of Major Epigenetic Modifying Enzymes
Stephanie Bridgeman1, Wendy Northrop2, Gaewyn Ellison3
1School of Pharmacy and Biomedical Sciences, and Curtin Health Innovation Research Institute, Curtin University, Bentley, WA 6102, Australia. stephanie.allen@postgrad.curtin.edu.au.
Cancers
|April 13, 2019
Summary
Statins, cholesterol-lowering drugs, did not directly alter major epigenetic enzyme activities like HDAC or HAT. However, statins showed a tendency to increase DNA methyltransferase (DNMT) activity, suggesting this is not the mechanism behind potential anticancer effects.
Area of Science:
- Epigenetics
- Pharmacology
- Oncology
Background:
- Statins are widely used cholesterol-lowering drugs with potential anticancer effects.
- Epigenetic modifying drugs, such as HDAC and DNMT inhibitors, are also of interest in cancer therapy.
- The direct impact of statins on epigenetic modifications remains to be fully elucidated.
Purpose of the Study:
- To investigate the effect of statin drugs on epigenetic modifications.
- To quantify the activity of histone deacetylase (HDAC), histone acetyltransferase (HAT), and DNA methyltransferase (DNMT) enzymes.
- To examine global histone acetylation levels in response to statin treatment.
Main Methods:
- Treatment of multiple cancer cell lines (hepatocellular carcinoma, breast carcinoma, leukemic macrophages, cervical adenocarcinoma) and mouse liver extracts with statins.
- Quantification of HDAC, HAT, and DNMT activities.
- Analysis of histone H3 and H4 acetylation via immunoblotting.
Main Results:
- Statins did not alter HDAC or HAT activity.
- Histone H3 and H4 acetylation levels remained unchanged following statin treatment.
- Statins exhibited a trend towards increasing DNMT activity.
Conclusions:
- The direct inhibition of major epigenetic modifying enzymes is unlikely to mediate the potential anticancer effects of statins.
- Statins may influence epigenetic modifications through mechanisms other than direct enzyme inhibition.
- Further investigation is needed to explore statin effects on specific genomic regions and epigenetic modifications.
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