Exploring the Therapeutic Potential of Betaine and Its Derivatives in Cancer Treatment: From Mechanisms to Clinical Implications

Introduction

Cancer remains a critical global health challenge as the second leading cause of death worldwide. Tumor heterogeneity, metastasis, drug resistance, and systemic toxicity limit the efficacy of conventional chemotherapy and radiotherapy. Consequently, there is growing interest in bioactive natural compounds derived from plants and dietary sources that modulate cancer progression with lower toxicity. Betaine (trimethyl glycine) is such a metabolite with notable antioxidant, anti-inflammatory, and epigenetic regulatory roles that have been increasingly associated with anticancer activity. Acting predominantly as a methyl donor in DNA methylation processes, betaine influences gene expression modulating oncogenes and tumor suppressors vital to carcinogenesis. This review critically examines betaine’s mechanisms in tumor suppression, its diverse efficacy across cancer types, and the emerging therapeutic platforms enabled by its chemical derivatives and nanotechnology-based drug delivery systems.

Production and Biological Significance of Betaine