In vitro Inhibition of Diacylglycerol Acyltransferase by Prenylflavonoids from Sophora flavescens

Mi Yeon Chung; Mun-Chual Rho; Jeong Suk Ko; Shi Yong Ryu; Kyung Hee Jeune; Koanhoi Kim; Hyun Sun Lee; Young Kook Kim

doi:10.1055/s-2004-815545

Planta Med 2004; 70(3): 258-260
DOI: 10.1055/s-2004-815545

Letter

In vitro Inhibition of Diacylglycerol Acyltransferase by Prenylflavonoids from Sophora flavescens

Mi Yeon Chung¹ , Mun-Chual Rho¹ , Jeong Suk Ko¹ , Shi Yong Ryu² , Kyung Hee Jeune³ , Koanhoi Kim¹ , Hyun Sun Lee¹ , Young Kook Kim¹

¹Laboratory of Lipid Metabolism, Korea Research Institute of Bioscience and Biotechnology, Taejon, Korea
²Korea Research Institute of Chemical Technology, Taejon, Korea
³Department of Biology, Yeungnam University, Kyungsan, Korea

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 Government

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

P.O. Box 115

Yusong

Taejon 305-333

Korea

Phone: +82-42-860-4314

Fax: +82-42-861-2675

Email: leehs@kribb.re.kr