Download PDF
Planta Med 2004; 70(3): 258-260
DOI: 10.1055/s-2004-815545
Letter
© Georg Thieme Verlag Stuttgart · New York

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
Further Information

Publication History

Received: August 15, 2003

Accepted: December 13, 2003

Publication Date:
23 March 2004 (online)

    Permissions and Reprints

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.

References

  • 1 Lehner R, Kuksis A. Biosynthesis of triacylglycerols.  Prog Lipid Res. 1996;  35 169-201
    CrossrefPubMedGoogle Scholar
  • 2 Farese Jr R V, Cases S, Smith S J. Triglyceride synthesis: Insights from the cloning of diacylglycerol acyltransferase.  Curr Opin Lipidol. 2000;  11 229-34
    CrossrefPubMedGoogle Scholar
  • 3 Ko J S, Ryu S Y, Kim Y S, Chung M Y, Kang J S, Rho M C. et al . Inhibitory activity of diacylglycerol acyltransferase by tanshinones from the roots of Salvia miltiorrhiza .  Arch Pharm Res. 2002;  25 446-8
    CrossrefPubMedGoogle Scholar
  • 4 Ko J S, Rho M C, Chung M Y, Song H Y, Kang J S, Kim K H. et al . Quinolone alkaloids, diacylglycerol acyltransferase inhibitors from the fruits of Evodia rutaecarpa .  Planta Med. 2002;  68 1131-3
    Article in Thieme ConnectPubMedGoogle Scholar
  • 5 John W R. Natural products of woody plants I. Heidelberg; Springer-Verlag 1989: pp 533-69
    Google Scholar
  • 6 Ryu S Y, Lee H S, Kim Y K, Kim S H. Determination of isoprenyl and lavandulyl positions of flavonoids from Sophora flavescens by NMR experiment.  Arch Pharm Res. 1997;  20 491-5
    PubMedGoogle Scholar
  • 7 Coleman R A. Diacylglycerol acyltransferase and monoacylglycerol acyltransferse from liver and intestine.  Methods Enzymol. 1992;  209 98-103
    PubMedGoogle Scholar
  • 8 Tomoda H, Igarashi K, Cyong J C, Omura S. Evidence for an essential role of long chain acyl-CoA synthetase in animal cell proliferation.  J Biol Chem. 1991;  26 4214-19
    PubMedGoogle Scholar
  • 9 Smith S J, Cases S, Jensen D R, Chen H C, Sande E, Tow B. et al . Obesity resistance and multiple mechanisms of triglyceride synthesis in mice lacking dgat.  Nat Genet. 2000;  25 87-90
    CrossrefPubMedGoogle Scholar

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

      >