Zhu Jing-Jie, Yan Gui-Rui, Xu Zhi-Jian, Hu Xiao, Wang Gai-Hong, Wang Ting, Zhu Wei-Liang, Hou Ai-Jun, Wang He-Yao
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang Hi-Tech Park, Pudong, Shanghai, 201203, China.
Department of Pharmacognosy, School of Pharmacy, Fudan University, 826 Zhang Heng Road, Shanghai, 201203, China.
Phytother Res. 2015 Jul;29(7):1040-5. doi: 10.1002/ptr.5344. Epub 2015 Mar 31.
(2'R)-2',3'-Dihydro-2'-(1-hydroxy-1-methylethyl)-2,6'-bibenzofuran-6,4'-diol (DHMB) is a natural compound extracted from Morus notabilis. It was found that DHMB acts as a competitive inhibitor against mushroom tyrosinase with a Ki value of 14.77 μM. Docking results further indicated that it could form strong interactions with one copper ion with a distance of 2.7 Å, suggesting the mechanism of inhibition might be due to chelating copper ions in the active site. Furthermore, melanin production in B16-F10 murine melanoma cells was significantly inhibited by DHMB in a concentration-dependent manner without cytotoxicity. The results of western blotting also showed that DHMB decreased 3-isobuty-1-methxlzanthine-induced mature tyrosinase expression. Taken together, these findings indicated that DHMB may be a new promising pigmentation-altering agent for agriculture, cosmetic, and therapeutic applications.
(2'R)-2',3'-二氢-2'-(1-羟基-1-甲基乙基)-2,6'-联苯并呋喃-6,4'-二醇（DHMB）是从滇桑中提取的一种天然化合物。研究发现，DHMB作为蘑菇酪氨酸酶的竞争性抑制剂，其抑制常数（Ki）值为14.77 μM。对接结果进一步表明，它能与一个铜离子形成强烈相互作用，距离为2.7 Å，这表明其抑制机制可能是由于螯合了活性位点中的铜离子。此外，DHMB以浓度依赖性方式显著抑制B16-F10小鼠黑色素瘤细胞中的黑色素生成，且无细胞毒性。蛋白质免疫印迹结果还表明，DHMB可降低3-异丁基-1-甲基黄嘌呤诱导的成熟酪氨酸酶表达。综上所述，这些发现表明，DHMB可能是一种用于农业、化妆品和治疗应用的新型有前景的色素沉着改变剂。
