Synthesis & α-glucosidase inhibitory & glucose consumption-promoting activities of flavonoid-coumarin hybrids
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Updated: Feb 11, 2026

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
Hua Sun1, Xiaotong Song1, Yunchang Tao1
1China International Science & Technology Cooperation Base of Food Nutrition/Safety & Medicinal Chemistry, Key Laboratory of Industrial Fermentation Microbiology of Ministry of Education, College of Bioengineering, Tianjin University of Science & Technology, Tianjin 300457, PR China.
Aim:
The research of novel and potent antidiabetic agents is urgently needed for the control of the exploding diabetic population. We previously reported the synthesis and antidiabetic activity of natural 8-(6"-umbelliferyl)-apigenin (1), but its antidiabetic targets are not known. Therefore, four series of derivatives were synthesized and evaluated for their antidiabetic activities. Results & methodology: Compounds (5a) and (14a) were identified as new α-glucosidase and α-amylase dual inhibitors. The kinetic analysis of the most potent α-glucosidase inhibitor of each series of compounds revealed that they inhibited α-glucosidase in irreversible modes. In addition, compounds (5a) and (14a) showed potent glucose consumption-promoting activity.
Conclusion:
Compounds (5a) and (14a) could be regarded as promising starting points for the development of antidiabetic candidates.
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