A new synthesis of fully phosphorylated flavones as potent pancreatic cholesterol esterase inhibitors |
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Authors: | Peng Guoping Du Yidan Wei Yingling Tang Jingming Peng Ai-Yun Rao Liqun |
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Affiliation: | College of Bioscience and Biotechnology, Hunan Agricultural University, Furong District, Changsha 410428, China. |
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Abstract: | Five flavones possessing one to four phenolic groups were fully phosphorylated efficiently and the obtained compounds showed excellent pancreatic cholesterol esterase (CEase) inhibitory activities with IC(50) in the nanomolar range, which were much more potent than their parent compounds. The inhibition mechanism and kinetic characterization studies indicate that they are irreversible competitive inhibitors. |
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