Microbial adhesion on the tooth surface is the initiating factor for plaque formation. The majority of the early plaque flora is constituted by different Streptococci sp. In this study, we have reported the antimicrobial and antibiofilm activity of naringin against the cariogenic bacterium Streptococcus mutans MTCC 497. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the identified bioactive compound naringin were determined using a micro-dilution assay. The antibiofilm activity was screened at sublethal concentrations of naringin (75%, 50%, and 25 % of MBC) using the microtiter plate method. Further, the cytotoxicity of naringin and chlorhexidine mouth wash was tested on L132, normal human embryonic lung epithelial cell lines using a phase-contrast inverted microscope and MTT assay. Our results revealed, bioactive compound naringin exhibited a significant antimicrobial activity with MIC 12.5mg/ml, MBC 6.25mg/ml, and IC50 value 4.563mg/ml. There was more than an 85% reduction in the biofilm formation at 75% sub-MBC level Concentration. Naringin-treated cells, showed no signs of deformity even at the highest tested concentration while there was evidence of cell toxicity in the cells treated with the lowest concentration of chlorhexidine mouth wash. LC50 value of naringin was found to be 174.884 mg/ml indicating it to be safe. The findings of this study endorse that naringin has the strong ability to interfere In vitro with the biofilm formation of Streptoccocus mutans, the primary etiological agent of dental caries. It also showed the least toxicity in comparison to chlorhexidine mouth wash, the choice of drug used to control dental plaque.