Plant Phytochemicals as Epigenetic Modulators: Role in Cancer Chemoprevention
Journal Title: The AAPS Journal - Year 2014, Vol 16, Issue 1
Abstract
In recent years, “nutri-epigenetics,” which focuses on the influence of dietary agents on epigenetic mechanism(s), has emerged as an exciting novel area in epigenetics research. Targeting of aberrant epigenetic modifications has gained considerable attention in cancer chemoprevention research because, unlike genetic changes, epigenetic alterations are reversible and occur during early carcinogenesis. Aberrant epigenetic mechanisms, such as promoter DNA methylation, histone modifications, and miRNA-mediated post-transcriptional alterations, can silence critical tumor suppressor genes, such as transcription factors, cell cycle regulators, nuclear receptors, signal transducers, and apoptosis-inducing and DNA repair gene products, and ultimately contribute to carcinogenesis. In an effort to identify and develop anticancer agents which cause minimal harm to normal cells while effectively killing cancer cells, a number of naturally occurring phytochemicals in food and medicinal plants have been investigated. This review highlights the potential role of plant-derived phytochemicals in targeting epigenetic alterations that occur during carcinogenesis, by modulating the activity or expression of DNA methyltransferases, histone modifying enzymes, and miRNAs. We present in detail the epigenetic mode of action of various phytochemicals and discuss their potential as safe and clinically useful chemopreventive strategies.
Authors and Affiliations
Vijay S. Thakur, Gauri Deb, Melissa A. Babcook, Sanjay Gupta
Prodrug Approaches for CNS Delivery
Central nervous system (CNS) drug delivery remains a major challenge, despite extensive efforts that have been made to develop novel strategies to overcome obstacles. Prodrugs are bioreversible derivatives of drug molecu...
Current industrial practices of assessing permeability and P-glycoprotein interaction
Combination of the in vitro models that are high throughput but less predictive and the in vivo models that are low throughput but more predictive is used effectively to evaluate the intestinal permeability and transport...
Deorphanization of Novel Peptides and Their Receptors
Peptide hormones and neuropeptides play important roles in endocrine and neural signaling, often using G protein-coupled receptor (GPCR)-mediated signaling pathways. However, the rate of novel peptide discovery has slowe...
Pharmacokinetics and Pharmacodynamics of Phenethyl Isothiocyanate: Implications in Breast Cancer Prevention
Phenethyl isothiocyanate (PEITC)—a naturally occurring isothiocyanate in cruciferous vegetables—has been extensively studied as a chemopreventive agent in several preclinical species and in humans. Pharma...
Comparative In Silico–In Vivo Evaluation of ASGP-R Ligands for Hepatic Targeting of Curcumin Gantrez Nanoparticles
The online version of this article (doi:10.1208/s12248-013-9474-6) contains supplementary material, which is available to authorized users.