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The purpose of this study was to evaluate the whitening effect of aerial part of Pueraria lobata and mechanisms. Aerial part of Pueraria lobata, dose-dependently reduced the melanin content. Aerial part of Pueraria lobata, significantly decreased cellular tyrosinase activity, while there was not any effect on tyrosinase in cell-free conditions. To elucidate the mech-anisms behind the aerial part of Pueraria lobata, treated melanogenesis regulation, the expressions of melanogensis related genes, proteins, and the activity of α-glucosidase were determined. Aerial part of Pueraria lobata, significantly inhibited gene and protein levels of MITF, tyrosinase and TRP-1. It suppressed the α-glucosidase, leading to inhibition on the maturation of tyrosinase. Also aerial part of Pueraria lobata, was observed to have the high antioxidant activity. These results suggested that whitening effect of aerial part of Pueraria lobata, should be due to the down-regulation of MITF, tyrosinase and TRP-1 expression and the intercepting maturation of tyrosinase through suppressing α-glucosidase. Another should be the high anti-oxidant activity. The findings show the possibility that aerial part of Pueraria lobata, can be used as a potential skin-whit-ening agent.

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