Chemical Research in Chinese Universities ›› 2018, Vol. 34 ›› Issue (3): 408-414.doi: 10.1007/s40242-018-7338-4

• Articles • Previous Articles     Next Articles

Design, Synthesis and Biological Activity of Novel Furocoumarin Derivatives as Stimulators of Melanogenesis and Tyrosinase in B16 Cells

NIU Chao1, ZANG Deng1,2, Haji Akber AISA1   

  1. 1. Key Laboratory of Plant Resources and Chemistry in Arid Regions, State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, P. R. China;
    2. University of Chinese Academy of Sciences, Beijing 100049, P. R. China
  • Received:2017-10-31 Revised:2017-12-27 Online:2018-06-01 Published:2018-01-22
  • Contact: Haji Akber AISA E-mail:haji@ms.xjb.ac.cn
  • Supported by:
    Supported by the Natural Science Foundation of Xinjiang, China(No.2017D01A76).

Abstract: Sixteen novel and four known(4a, 4d, 4e, 4h) amine derivatives of furocoumarin were synthesized, then submitted to evaluation as stimulators of melanogenesis and tyrosinase in B16 murine cells. Among them, five compounds(4g, 4j-4m) showed potent activating effect on both melanogenesis and tyrosinase in vitro compared with positive control(8-MOP), the most widely used drugs for vitiligo in clinic. Noticeably, compounds 4h and 4j, which contain morpholine and piperazine, were recognized as the most effective stimulator of melanogenesis and tyrosianse in B16 cells separately. These derivatives may serve as lead compounds for further drug discovery for the treatment of vitiligo.

Key words: Furocoumarin, Amine, Melanin synthesis, Tyrosinase, Vitiligo