Niu Chao, Pang Guang Xian, Li Gen, Dou Jun, Nie Li Fei, Himit Helimay, Kabas Madina, Aisa Haji Akber
The Key Laboratory of Plant Resources and Chemistry of Arid Zone, Chinese Academy of Sciences, Urumqi 830011, China; State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China.
The Key Laboratory of Plant Resources and Chemistry of Arid Zone, Chinese Academy of Sciences, Urumqi 830011, China; State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China.
Bioorg Med Chem. 2016 Nov 15;24(22):5960-5968. doi: 10.1016/j.bmc.2016.09.056. Epub 2016 Sep 23.
Furocoumarins, isolated from Psoralen corylifolia L., were found to be the most effective drug in the treatment of vitiligo nowadays. Twenty-five furocoumarin derivatives were thus designed and synthesized in order to improve the melanogenesis in B16 cells for the first time. Among them, twenty-three compounds were more potent than the positive control (8-MOP), the commonly used drug for vitiligo in clinic. Noticeably, compounds 6m (350.5%) and 6p (313.1%) based on the scaffold of 6k (2H-benzofuro[2,3-h]chromen-2-one) were nearly 3-fold stronger than 8-MOP (114.50%). The in vitro melanin synthesis evaluation of these structurally diverse analogues had also led to an outline of structure-activity relationship.
从补骨脂中分离出的呋喃香豆素被发现是目前治疗白癜风最有效的药物。因此，首次设计并合成了25种呋喃香豆素衍生物，以促进B16细胞中的黑色素生成。其中，23种化合物比阳性对照（8-甲氧基补骨脂素）更有效，8-甲氧基补骨脂素是临床上常用的治疗白癜风的药物。值得注意的是，基于6k（2H-苯并呋喃[2,3-h]色烯-2-酮）骨架的化合物6m（350.5%）和6p（313.1%）的效果比8-甲氧基补骨脂素（114.50%）强近3倍。对这些结构多样的类似物进行的体外黑色素合成评估也得出了构效关系的概述。
