Design and synthesis of epigallocatechin (EGC) analogs selective to inhibit α-amylase over α-glucosidases via the incorporation of caffeine acid and its derivatives

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成果类型：

期刊论文

作者：

Chen, Wenming;Zhou, Cui;Chen, Jiansheng;Wang, Meizhu;Zhou, Fang;...

通讯作者：

Wang, Chunmei;Zhang, Xu;Zhou, W

作者机构：

[Chen, Wenming; Zhou, Fang] Hunan Univ Chinese Med, Hosp 1, Dept Pharmaceut Prod Ctr, 95 Shaoshan Rd, Changsha 410007, Hunan, Peoples R China.

[Chen, Wenming; Zhou, Fang] Hunan Univ Chinese Med, Hosp 1, TCM & Ethnomed Dev Int Lab, 95 Shaoshan Rd, Changsha 410007, Hunan, Peoples R China.

[Zhou, Cui; Zhou, Wen; Wang, Chunmei; Wang, CM; Zhang, X] Chinese Acad Agr Sci, Shanghai Vet Res Inst, Shanghai 200241, Peoples R China.

[Zhou, Cui; Wang, Meizhu] Guangzhou Univ Chinese Med, Sch Pharmaceut Sci, Waihuan Rd, Guangzhou 200241, Peoples R China.

[Zhang, Xu; Chen, Jiansheng] South China Agr Univ, Coll Forestry & Landscape Architecture, Guangzhou 510642, Peoples R China.

通讯机构：

[Zhou, W ; Wang, CM; Zhang, X] C

Chinese Acad Agr Sci, Shanghai Vet Res Inst, Shanghai 200241, Peoples R China.

语种：

英文

关键词：

HPA inhibitors;EGC;Selectivity;Caffeic acid;Antidiabetic drug

期刊：

Bioorganic Chemistry

ISSN：

0045-2068

年：

2022

卷：

119

页码：

105515-

DOI：

10.1016/j.bioorg.2021.105515

基金类别：

The work is partly supported by the Natural Science Foundation of Hunan Province, China (Grant No. 2021JJ80064) and Scientific Research Fund of Hunan Provincial Education Department (Grant No. 18B231). We also appreciated Dr. Jinyun Dong for guiding us to perform the molecular docking.

机构署名：

本校为第一机构

院系归属：

第一中医临床学院

摘要：

Natural products are a promising and underappreciated reservoir for the preferred chemical scaffolds in the search of antidiabetic drugs. In this study twenty-one EGC-based derivatives selective to inhibit human pancreatic α-amylase (HPA), the enzyme at the top of the starch digestion pyramid, have been designed and synthesized in terms of the lead myricetin-caffeic acid conjugate 1 reported ever. We focus on methylation of caffeic acid, length of a liker, a double bond contained in the linker on the inhibition activity and selectivity of EGC-...

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Design and synthesis of epigallocatechin (EGC) analogs selective to inhibit α-amylase over α-glucosidases via the incorporation of caffeine acid and its derivatives

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