Design, synthesis and bioactivity of chalcones and its analogues
Niu, C (Niu, Chao); Tuerxuntayi, A (Tuerxuntayi, Adila); Li, G (Li, Gen); Kabas, M (Kabas, Madina); Dong, CZ (Dong, Chang-Zhi); Aisa, HA (Aisa, Haji Akber); Aisa, HA
2017
发表期刊CHINESE CHEMICAL LETTERS
卷号28期号:7页码:1533-1538
摘要

The Vernohia anthelmintica L's extract is one of the most popular Uygur medicines used for vitiligo. It is believed that the chalcone compounds of the plant play an important role in the treatment since they may activate tyrosinase and improve melanin production. In this study, twenty-one chalcones and nine analogues were synthesized in view of three different components of chalcone (A, B ring and a, beta-unsaturated carbonyl). After biological evaluation of their activity on tyrosinase in cell-free systems, the result showed that most compounds (except polyhydroxy chalcones) possess activator effect on the tyrosinase, especially for 13a-15a, 20a and 1 b, which bearing a comparable activity to the positive control 8-MOP. SAR of these tyrosinase activator was summed up for the first time as well. Finally, compound 13a was found to increase melanin contents and tyrosinase activity 1.75 and 1.3 fold, respectively, compared with that of untreated murine B16 cells at the concentration of 40 mu g/mL (C) 2017 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.

关键词Vitiligo Activator Of Tyrosinase Chalcone B16 Cells Sar
DOI10.1016/j.cclet.2017.03.018
收录类别SCI
WOS记录号WOS:000406726500032
引用统计
文献类型期刊论文
条目标识符http://ir.xjipc.cas.cn/handle/365002/5053
专题省部共建新疆特有药用资源利用重点实验室
通讯作者Aisa, HA
作者单位1.Chinese Acad Sci, Key Lab Plant Resources & Chem Arid Zone, Urumqi 830011, Peoples R China
2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China
3.Univ Paris Diderot, Sorbonne Paris Cite, ITODYS, UMR CNRS 7086, 15 Rue JA de Baif, F-75205 Paris 13, France
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GB/T 7714
Niu, C ,Tuerxuntayi, A ,Li, G ,et al. Design, synthesis and bioactivity of chalcones and its analogues[J]. CHINESE CHEMICAL LETTERS,2017,28(7):1533-1538.
APA Niu, C .,Tuerxuntayi, A .,Li, G .,Kabas, M .,Dong, CZ .,...&Aisa, HA.(2017).Design, synthesis and bioactivity of chalcones and its analogues.CHINESE CHEMICAL LETTERS,28(7),1533-1538.
MLA Niu, C ,et al."Design, synthesis and bioactivity of chalcones and its analogues".CHINESE CHEMICAL LETTERS 28.7(2017):1533-1538.
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