Polyphenols from Broussonetia papyrifera displaying potent alpha-glucosidase inhibition = 닥나무로부터 분리한 폴리페놀성 화합물의 강한 alpha-glucosidase 저해활성

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Title
Polyphenols from Broussonetia papyrifera displaying potent alpha-glucosidase inhibition = 닥나무로부터 분리한 폴리페놀성 화합물의 강한 alpha-glucosidase 저해활성
Author(s)
Hyung Won Ryu; B W Lee; M J Curtis-Long; S Jung; Young Bae RyuWoo Song Lee; K H Park
Bibliographic Citation
Journal of Agricultural and Food Chemistry, vol. 58, no. 1, pp. 202-208
Publication Year
2010
Abstract
The organic extract of the roots of Broussonetia papyrifera showed extremely high a-glucosidase inhibitory activity with an IC50 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 (IC50 = 2.1 μKI = 2.3 μM) has an inhibitory activity slightly higher than that of the potent α-glucosidase inhibitor deoxynojlrimycln (IC50 = 3.5 μM). The novel a-glucosidase inhibitors 11 (IC50 = 27.6 μM) and 12 (IC 50 = 33.3 μM) are similar in activity to sugar-derived a-glucosidase inhibitors such as voglibose (IC50 = 23.4 μM). Interestingly, major constituents (1, 2, 6, 7, 9, and 10) of B. papyrifera displayed significant inhibitory activity with IC50 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.
Keyword
α-glucosidase inhibitorBroussonetia papyriferaFlavonoidGlycosidase
ISSN
0021-8561
Publisher
Amer Chem Soc
DOI
http://dx.doi.org/10.1021/jf903068k
Type
Article
Appears in Collections:
Ochang Branch Institute > Natural Medicine Research Center > 1. Journal Articles
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
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