首页|Polyphenols from Broussonetia papyrifera Displaying Potent α-Glucosidase Inhibition
Polyphenols from Broussonetia papyrifera Displaying Potent α-Glucosidase Inhibition
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NSTL
Amer Chemical Soc
The organic extract of the roots of Broussonetia papyrifera showed extremely high α-glucosidase inhibitory activity with an IC_(50) of around 10 μg/mL. Due to its potency, subsequent bioactivity-guided fractionation of the chloroform extract led to 12 polyphenols, 1-12, 4 of which were identified as chalcones (1-4), another 4 as flavans (5-8), 2 as flavonols (9 and 10), and 2 others as the novel species benzofluorenones (11 and 12). Broussofluorenone A (11) and broussofluorenone B (12) emerged as new compounds possessing the very rare 5,11-dioxabenzo[b]fluoren-10-one skeleton. These compounds (1-12) were evaluated for a-glucosidase inhibitory activity to identify their inhibitory potencies and kinetic behavior. The most potent inhibitor, 10 (IC_(50) = 2.1 μM, K_i = 2.3 μM), has an inhibitory activity slightly higher than that of the potent α-glucosidase inhibitor deoxynojirimycin (IC_(50) = 3.5 μM). The novel α-glucosidase inhibitors 11 (IC_(50) = 27.6 μM) and 12 (IC_(50) = 33.3 μM) are similar in activity to sugar-derived α-glucosidase inhibitors such as voglibose (IC_(50) = 23.4 μM). Interestingly, major constituents (1, 2, 6, 7, 9, and 10) of 8. papyrifera displayed significant inhibitory activity with IC_(50) values of 5.3, 11.1, 12.0, 26.3, 3.6, and 2.1 μM, respectively. In kinetic studies, chalcones (1-4) exhibited noncompetitive inhibition characteristics, whereas the others (5-12) showed mixed behavior.
Division of Applied Life Science (BK21 Program), EB-NCRC, Institute of Agriculture and Life Science, Graduate School of Gyeongsang National University, Jinju 660-701, South Korea
12 New Road, Nafferton, Driffield, East Yorkshire YO25 4JP, United Kingdom
NSTL
Amer Chemical Soc
