Purpose <p>This study aimed to investigate the potential of corylin, a bioactive compound isolated from the aerial part of <i>Pueraria lobata</i>, as a novel skin-whitening agent. Specifically, the research sought to evaluate its effects on melanin synthesis, understand its underlying mechanisms, and validate its efficacy in mitigating hyperpigmentation.</p> Methods <p>Bioactive compound was isolated from <i>Pueraria lobata</i> through a systematic fractionation process involving activated carbon pigment removal, sequential solvent extraction, and resin-based chromatography. It was shown to inhibit melanin synthesis by targeting tyrosinase activation and modulating key signaling pathways. Its efficacy in reducing melanin production was validated through cellular assays and a UVB-stimulated 3D human skin model, highlighting its potential as a skin-whitening agent.</p> Results <p>Through fractionation, the bioactive compound was identified as corylin, which reduced melanin content and tyrosinase activity without cytotoxicity, modulated signaling pathways to downregulate MITF and melanogenic enzymes, and inhibited α-glucosidase, disrupted glycosylation. In a UVB-stimulated 3D skin model, it effectively decreased melanin production, confirming its potential to mitigate hyperpigmentation.</p> Conclusion <p>Corylin is a promising candidate for skin-whitening applications, effectively mitigating hyperpigmentation by targeting multiple stages of melanin synthesis, including enzymatic activity and regulatory pathways. Further clinical studies are needed to confirm its safety and therapeutic potential for dermatological use.</p> Graphical Abstract <p></p>