XJIPC OpenIR  > 省部共建新疆特有药用资源利用重点实验室
新型查尔酮衍生物的合成及酪氨酸酶活性
Alternative TitleSynthesis and activity on tyrosinase of novel chalcone derivatives
牛超; 李根; 买迪娜; 阿吉艾克拜尔·艾萨
2014
Source Publication高等学校化学学报
ISSN0251-0790
Volume35Issue:6Pages:1204-1211
Abstract

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).

Other Abstract

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.

Keyword查尔酮 苯并噻唑 酰胺 酪氨酸酶活性
Indexed BySCI ; CSCD
CSCD IDCSCD:5166534
Citation statistics
Cited Times:1[CSCD]   [CSCD Record]
Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/3684
Collection省部共建新疆特有药用资源利用重点实验室
资源化学研究室
Affiliation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
GB/T 7714
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.
APA 牛超,李根,买迪娜,&阿吉艾克拜尔·艾萨.(2014).新型查尔酮衍生物的合成及酪氨酸酶活性.高等学校化学学报,35(6),1204-1211.
MLA 牛超,et al."新型查尔酮衍生物的合成及酪氨酸酶活性".高等学校化学学报 35.6(2014):1204-1211.
Files in This Item:
File Name/Size DocType Version Access License
新型查尔酮衍生物的合成及酪氨酸酶活性.p(425KB)期刊论文作者接受稿开放获取CC BY-NC-SAView Application Full Text
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[牛超]'s Articles
[李根]'s Articles
[买迪娜]'s Articles
Baidu academic
Similar articles in Baidu academic
[牛超]'s Articles
[李根]'s Articles
[买迪娜]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[牛超]'s Articles
[李根]'s Articles
[买迪娜]'s Articles
Terms of Use
No data!
Social Bookmark/Share
File name: 新型查尔酮衍生物的合成及酪氨酸酶活性.pdf
Format: Adobe PDF
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.