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DOI: 10.1055/s-2004-815545
In vitro Inhibition of Diacylglycerol Acyltransferase by Prenylflavonoids from Sophora flavescens
This research was supported by grants (PDM0020213) from Plant Diversity Research Center of 21st Century Frontier Research Program and KRIBB Research Initiative Program funded by the Ministry of Science and Technology of the Korean GovernmentPublication History
Received: August 15, 2003
Accepted: December 13, 2003
Publication Date:
23 March 2004 (online)
Abstract
Four prenylflavonoids, kurarinone (1), a chalcone of 1, kuraridin (2), kurarinol (3), kushenol H (4) and kushenol K (5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT). The flavonoids inhibited DGAT activity in a dose-dependent manner with IC50 values of 10.9 μM (1), 9.8 μM (2), 8.6 μM (3), 142.0 μM (4) and 250 μM (5). The prenylflavonoids without C3-OH (1, 2, 3) showed stronger inhibition than those with C3-OH (4, 5). On the other hand, flavonoids without side chains (hesperetin, naringenin, quercetin and kaempferol) did not inhibit the enzyme activity at a final concentration of 800 μM. These data suggest that the lavandulyl side chain and the position of the hydroxy group are important for high DGAT inhibitory activity. Compound 1 also inhibited de novo synthesis of triacylglycerol (TG) in Raji cells.
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Dr. Hyun Sun Lee
Laboratory of Lipid Metabolism
Korea Research Institute of Bioscience and Biotechnology
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Yusong
Taejon 305-333
Korea
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Email: leehs@kribb.re.kr