Protective Role of Riboflavin and Carboxymethylflavin: Toxicological and Cytotoxic Evaluation

Abstract

Riboflavin (vitamin B2) is a water-soluble vitamin that has antioxidant, anti-inflammatory, and mitochondrial-stabilizing properties, rendering it an attractive neuroprotective candidate. Its therapeutic potential has, however, been limited by low bioavailability and cellular uptake. In this study, carboxymethylflavin (CMF), a riboflavin derivative with better solubility and membrane permeability, was synthesized and compared with riboflavin to evaluate their toxicity and neuroprotective effects. The toxicity was determined using brine shrimp lethality, and antiproliferative activity was determined using MTT assays. Riboflavin was moderately cytotoxic and was more effective against cancer cell lines as compared to normal fibroblasts. CMF, on the other hand, showed significantly reduced cytotoxicity in all the cell lines examined, which implies that it could be safer compared to riboflavin. The improved biocompatibility and maintenance of the biological activity of CMF indicate the possibility of developing it into a biologically useful agent with fewer side effects without compromising its neuroprotective properties and having a safer profile in therapy.