期刊
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
卷 1820, 期 7, 页码 962-969出版社
ELSEVIER
DOI: 10.1016/j.bbagen.2012.03.018
关键词
Melanogenesis; (E)-3-(2,4-dihydroxybenzylidene)pyrrolidine-2,5-dione (3-DBP); Tyrosinase inhibitor; HRM2 hairless mouse
资金
- National Research Foundation of Korea (NRF)
- Ministry of Education, Science and Technology [2009-0083538]
Background: Tyrosinase inhibitors have become increasingly important because of their ability to inhibit the synthesis of the pigment melanin. A search for new agents with strong tyrosinase activity led to the synthesis of the tyrosinase inhibitor (E)-3-(2,4-dihydroxybenzylidene)pyrrolidine-2,5-dione (3-DBP). Methods: The inhibitory effect of 3-DBP on tyrosinase activity and melanin production was examined in murine melanoma B16F10 cells. Additional experiments were performed using HRM2 hairless mice to demonstrate the effects of 3-DBP in vivo. Results: The novel compound, 3-DBP, showed an inhibitory effect against mushroom tyrosinase (IC50 = 0.53 mu M), which indicated that it was more potent than the well-known tyrosinase inhibitor kojic acid (IC50 =- 8.2 mu M). When tested in B16F10 melanoma cells treated with a-melanocyte stimulating hormone (alpha-MSH), 3-DBP also inhibited murine tyrosinase activity, which in turn induced a decrease in melanin production in these cells. The anti-melanogenic effect of 3-DBP was further verified in HRM2 hairless mice. The skin-whitening index (L value) of HRM2 hairless mice treated with 3-DBP before irradiation with UVB was greater than that of UVB-irradiated mice that were not treated with 3-DBP. General significance: The newly synthesized 3-DBP has a potent inhibitory effect on tyrosinase. In addition to an in vitro investigation of the effects of 3-DBP on tyrosinase, in vivo studies using an HRM2 hairless mouse model demonstrated the anti-melanogenic potency of 3-DBP. Our newly synthesized 3-DBP showed efficient tyrosinase inhibitory effect in vivo and in vitro. Our finding suggests that 3-DBP can be an effective skin-whitening agent. (C) 2012 Elsevier B.V. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据