Abstract
Epigenetic regulation involves reversible changes in histones and DNA modifications that can be inherited without any changes in the DNA sequence. Dysregulation of normal epigenetic processes can lead to aberrant gene expression as observed in many diseases, notably cancer. Recent insights into the mechanisms of DNA methylation, histone modifications, and non-coding RNAs involved in altered gene expression profiles of tumor cells have caused a paradigm shift in the diagnostic and therapeutic approaches towards cancer. There has been a surge in search for compounds that could modulate the altered epigenetic landscape of tumor cells, and to exploit their therapeutic potential against cancers. Flavonoids are naturally occurring phenol compounds which are abundantly found among phytochemicals and have potentials to modulate epigenetic processes. Knowledge of the precise flavonoid-mediated epigenetic alterations is needed for the development of epigenetics drugs and combinatorial therapeutic approaches against cancers. This review is aimed to comprehensively explore the epigenetic modulations of flavonoids and their anti-tumor activities.
Highlights
Epigenetics can be defined as the study of heritable changes in gene expression without involving any changes in the DNA sequence (Weinhold, 2006)
LncRNAs like MALAT1 and HOTAIR which are associated with metastasis are over expressed in cancer and MEG3 and PTENP1 which inhibit cell proliferation and migration are downregulated in cancer (Huarte, 2015)
There are recent reports indicating that flavonoids may reinstate the standard epigenetic marks which are changed during carcinogenesis (Carlos-Reyes et al, 2019; Jiang et al, 2021; Khan et al, 2021)
Summary
Nishat Fatima 1, Syed Shabihe Raza Baqri 2, Atrayee Bhattacharya 3, Nii Koney-Kwaku Koney 4, Kazim Husain 5, Ata Abbas 6,7 and Rais A. Dysregulation of normal epigenetic processes can lead to aberrant gene expression as observed in many diseases, notably cancer. Recent insights into the mechanisms of DNA methylation, histone modifications, and non-coding RNAs involved in altered gene expression profiles of tumor cells have caused a paradigm shift in the diagnostic and therapeutic approaches towards cancer. There has been a surge in search for compounds that could modulate the altered epigenetic landscape of tumor cells, and to exploit their therapeutic potential against cancers. Flavonoids are naturally occurring phenol compounds which are abundantly found among phytochemicals and have potentials to modulate epigenetic processes. Knowledge of the precise flavonoid-mediated epigenetic alterations is needed for the development of epigenetics drugs and combinatorial therapeutic approaches against cancers. This review is aimed to comprehensively explore the epigenetic modulations of flavonoids and their anti-tumor activities
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