Download PDF
Planta Med 2004; 70(7): 678-679
DOI: 10.1055/s-2004-827193
Letter
© Georg Thieme Verlag KG Stuttgart · New York

Guineensine, an Acyl-CoA: Cholesterol Acyltransferase Inhibitor, from the Fruits of Piper longum

Seung Woong Lee1 , Mun-Chual Rho1 , Jung Yeon Nam1 , Eun Hee Lim1 , Oh Eok Kwon1 , Young Ho Kim2 , Hyun Sun Lee1 , Young Kook Kim1
  • 1Laboratory of Lipid Metabolism, Korea Research Institute of Bioscience and Biotechnology, Taejon, Korea
  • 2College of Pharmacy, Chungnam National University, Taejon, Korea
This research was supported by a grant from Plant Diversity Research Center of 21st Century Frontier Research Program funded by Ministry of Science and Technology of Korean government, and by a grant of KRIBB Research Initiative Program.
Further Information

Publication History

Received: January 20, 2004

Accepted: February 22, 2004

Publication Date:
15 July 2004 (online)

    Permissions and Reprints

Abstract

Bioactivity-guided fractionations for ACAT inhibitor led to the isolation of guineensine from the CHCl3 extract of Piper longum. Its structure was identified by spectroscopic means (IR, UV, MS and NMR). Guineensine inhibited ACAT activity in a dose-dependent manner with an IC50 value of 3.12 µM.

References

  • 1 Heinonen T M. Acyl coenzyme A: cholesterol acyltransferase inhibition: potential atherosclerosis therapy or springboard for other discoveries?.  Expert Opin Investig Drugs. 2002;  11 1519-27
    CrossrefPubMedGoogle Scholar
  • 2 Steinberg D. Atherosclerosis in perspective: hypercholesterolemia and inflammation as partners in crime.  Nature Med. 2002;  8 1211-7
    CrossrefPubMedGoogle Scholar
  • 3 Sliskovic D R, Picard J A, Krause B R. ACAT inhibitors: The search for a novel and effective treatment of hypercholesterolemia and atherosclerosis.  Prog Med Chem. 2002;  39 121-71
    PubMedGoogle Scholar
  • 4 Doshi R, Wu J, Fishelevich R, Rodriguez A. Update on the role of acyl-CoA: cholesterol acyltransferase inhibitors in atherosclerosis.  Expert Opin Ther Patents. 2001;  11 1655-62
    CrossrefPubMedGoogle Scholar
  • 5 Jung B S, Shin M K. Piperaceae.  In: Encyclopedia of illustrated Korean natural drugs. Kwon SB, editor Seoul; Young Lim Sa 1998: pp 817-9
    Google Scholar
  • 6 Koul S K, Taneja S C, Agarwal V K, Dhar K L. Minor amides of Piper species.  Phytochemistry. 1988;  27 3523-7
    CrossrefPubMedGoogle Scholar
  • 7 Banerji A, Banerji J, Chatterjee A. Structure and stereochemistry of an alkamide from Piper sylvaticum .  Indian J Chemistry. 1980;  19B 346-9
    PubMedGoogle Scholar
  • 8 Kwon O E, Rho M C, Song H Y, Lee S W, Chung M Y, Lee J H. et al . Phenylpyropenes A and B, new inhibitors of acyl-CoA: cholesterol acyltransferase produced by Penicillium griseofulvum F1959.  J Antibiotics. 2002;  55 1004-8
    PubMedGoogle Scholar
  • 9 Shoji N, Umeyama A, Saito N, Takemoto T, Kajiwara A, Ohizumi Y. Dehydropipernonaline, an amide possessing coronary vasodilating activity, isolated from Piper longum L.  J Pharm Sci. 1986;  75 1188-9
    PubMedGoogle Scholar
  • 10 Lee S U, Mahoney N E, Campbell B C. Inhibition of aflatoxin B1 biosynthesis by piperlongumine isolated from Piper longum L.  J Microbiol Biotechnol. 2002;  12 679-82
    PubMedGoogle Scholar
  • 11 Song H Y, Rho M C, Lee S W, Kwon O E, Chang Y D, Lee H S. et al . Isolation of acyl-CoA: cholesterol acyltransferase inhibitor from Persicaria vulgaris .  Planta Med. 2002;  68 845-7
    Article in Thieme ConnectPubMedGoogle Scholar

Dr. Young Kook Kim

Laboratory of Lipid Metabolism

Korea Research Institute of Bioscience and Biotechnology

52 Oun-dong

Yusong-gu

Taejon 305 - 333

Korea

Phone: +82-42-860-4556

Fax: +82-42-861-2675

Email: kimyk@kribb.re.kr

      >