Yokozawa Takako, Kim You Jung
Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama, Japan.
Biol Pharm Bull. 2007 Nov;30(11):2007-11. doi: 10.1248/bpb.30.2007.
In our efforts to find new skin lightening agents, piceatannol (PICE) was investigated for its antioxidative property and ability to inhibit melanogenesis. In this study, PICE's effect on inhibition of mushroom tyrosinase, and tyrosinase inhibiting activity and melanin content were assessed utilizing the B16F10 melanoma cell (B16 cell) culture system. Results indicated that PICE has a strong antityrosinase activity (IC(50)=1.53 microM). To evaluate the relative efficacy of PICE compared to other tyrosinase inhibitors, its inhibitory effect was compared and showed that PICE was significantly stronger than kojic acid (IC(50)=50.1 microM) and resveratrol (IC(50)=63.2 microM). Furthermore, PICE was shown to down-regulate melanin content. To document PICE's antioxidative property, which is known to influence melanogenic activity, we assessed reactive species (RS) generation, reduced glutathione (GSH) and oxidized glutathione (GSSG) levels in these B16 cells. The results showed that PICE suppressed RS generation and enhanced the GSH/GSSG ratio. In conclusion, our results indicated that the antimelanogenic action of PICE is likely exhibited by the combined effect of PICE's antioxidative property and its ability to suppress RS generation while increasing the GSH/GSSG ratio.
在我们寻找新型皮肤美白剂的过程中,对白皮杉醇(PICE)的抗氧化性能及其抑制黑色素生成的能力进行了研究。在本研究中,利用B16F10黑色素瘤细胞(B16细胞)培养系统评估了PICE对蘑菇酪氨酸酶的抑制作用、酪氨酸酶抑制活性和黑色素含量。结果表明,PICE具有很强的抗酪氨酸酶活性(IC(50)=1.53 microM)。为了评估PICE与其他酪氨酸酶抑制剂相比的相对疗效,对其抑制作用进行了比较,结果显示PICE明显强于曲酸(IC(50)=50.1 microM)和白藜芦醇(IC(50)=63.2 microM)。此外,PICE还能下调黑色素含量。为了证明已知会影响黑色素生成活性的PICE的抗氧化性能,我们评估了这些B16细胞中活性物质(RS)的产生、还原型谷胱甘肽(GSH)和氧化型谷胱甘肽(GSSG)的水平。结果表明,PICE抑制了RS的产生并提高了GSH/GSSG比值。总之,我们的结果表明,PICE的抗黑色素生成作用可能是通过其抗氧化性能以及抑制RS产生同时提高GSH/GSSG比值的综合作用来实现的。