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题名: 新型查尔酮衍生物的合成及酪氨酸酶活性
其他题名: Synthesis and activity on tyrosinase of novel chalcone derivatives
作者: 牛超; 李根; 买迪娜; 阿吉艾克拜尔·艾萨
关键词: 查尔酮 ; 苯并噻唑 ; 酰胺 ; 酪氨酸酶活性
刊名: 高等学校化学学报
发表日期: 2014
卷: 35, 期:6, 页:1204-1211
收录类别: SCI ; EI ; CSCD
资助者: 国家“九七三”计划项目(批准号:2011CB512013);中国科学院西部之光项目(批准号:XBBS201212,200918);中国科学院新疆理化研究所重点支持资助项目(批准号:Y25A791401)资助
摘要: 合成了8个新型含苯并噻唑环的查尔酮衍生物及8个酰胺查尔酮,并对化合物的结构进行了表征. 生物活性测试结果表明,化合物4d,4h,5d,7b 和7d 表现出一定的酪氨酸酶激动活性,其中化合物7d 对酪氨酸酶的活性最好,其EC_(50) = 9. 6 mumol /L,优于阳性对照药8-MOP(EC_(50) = 14. 8 mumol /L).
英文摘要: Ver-nohia anthelmintica L was endemic plant in Xinjiang, which was often used in the treatment of Vitiligo. It was believed that the chalcone compounds of Ver-nohia anthelmintica L played an important role in this treatment. Since it may activate tyrosinase and improve the melanin production, many chalcone compounds and derivatives were described as potential inhibitor on tyrosinase which may act as skin lightening and whitening agents. However, chalcones which showed activator effect were seldom reported. In order to search for chalcones with high activities on tyrosinase, eight novel chalcone derivatives containing benzothiazole and eight amide-derived chalcones were synthesized in this work. All the compounds were identified by 1H NMR, 13C NMR, IR, HRMS and evaluated their activator effect on tyrosinase by measuring the oxidation rate of L-dopa. Compared with the reference drug 8-methoxypsoralen, compounds 4d, 4h, 5d, 7b and 7d showed some activator effect on tyrosinase. Amomg them, compound 7d demonstrated more potent activity with EC50=9.6 μmol/L than 8-methoxypsoralen, which EC50 value was 14.8 μmol/L. Further structural modification of this novel chalcones containing benzothiazole will be required for improving the solubility of them.
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内容类型: 期刊论文
URI标识: http://ir.xjipc.cas.cn/handle/365002/3684
Appears in Collections:新疆维吾尔自治区植物资源化学重点实验室 _期刊论文

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作者单位: 中国科学院干旱区植物资源化学重点实验室;新疆特有药用资源利用省部共建实验室,中国科学院新疆理化技术研究所;中国科学院大学

Recommended Citation:
牛超,李根,买迪娜,等. 新型查尔酮衍生物的合成及酪氨酸酶活性[J]. 高等学校化学学报,2014,35(6):1204-1211.
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