Planta Med 2002; 68(9): 845-847
DOI: 10.1055/s-2002-34395
Letter
© Georg Thieme Verlag Stuttgart · New York

Isolation of Acyl-CoA:Cholesterol Acyltransferase Inhibitor from Persicaria vulgaris

Hye Young Song1 , Mun-Chual Rho1 , Seung Woong Lee1 , Oh Eok Kwon1 , Young-Duck Chang2 , Hyun Sun Lee1 , Young-Kook Kim1
  • 1Cardiovascular Research Laboratory, Korea Research Institute of Bioscience and Biotechnology, Taejon, Korea
  • 2Department of Agricultural Biology, Chungnam National University, Taejon, Korea
Further Information

Publication History

Received: January 10, 2002

Accepted: May 25, 2002

Publication Date:
30 September 2002 (online)

Abstract

In the course of our search for Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors from natural sources, a new type of ACAT inhibitor was isolated from the methanol extract of Persicaria vulgaris. On the basis of spectral evidence, the structure of the active compound was identified as pheophorbide A. Pheophorbide A inhibited ACAT activity with an IC50 value of 1.1 μg/ml in an enzyme assay using rat liver microsomes with a dose dependent fashion.

References

  • 1 Suckling K E, Stange E F. Role of acyl-CoA: cholesterol acyltransferase in cellular cholesterol metabolism. J.  Lipid Res.. 1985;  26 647-71
  • 2 Stange E F, Dietschy J M. Cholesterol absorption and metabolism by the intestinal epithelium. In: Danielsson H, Sjövall J, editors New Comprehensive Biochemistry. Vol.12 Sterols and Bile Acids: Elsevier Science Publishers 1985: 121-49
  • 3 Ross R. The pathogenesis of atherosclerosis an update. New Engl. J.  Med.. 1986;  314 488-500
  • 4 Sliskovic D R, White A D. Therapeutic potential of ACAT inhibitors as lipid lowering and antiatherosclerotic agents. Trends in Pharmacol.  Sci.. 1991;  12 194-9
  • 5 Chang S u. New Medical College. Dictionary of Chinese Crude Drugs. Shanghai Scientific Techonologic Publishers Shanghai; 1977
  • 6 Schwikkard S L, Mulholland A D, Hutchings A. Pheophytins from Tupara fischeri .  Phytochemistry. 1998;  49 2391-4
  • 7 Tomoda H, Nishida H, Kim Y K, Obata R, Sunazuka T, Omura S. Relative and absolute stereochemistry of pyripyropene A, a potent, bioavailable inhibitor of Acyl-CoA:cholesterol acyltransferase (ACAT) J. Am. Chem.  Soc.. 1994;  116 12 097-8
  • 8 Sakata K, Yamamoto K, Ishikawa H, Yagi A, Etoh H, Ina K. Chlorophyllone-A, a new pheophorbide-a related compound isolated from Ruditapes philippinarum as an antioxidative compound.  Tetrahedron Lett.. 1990;  31 1165-8
  • 9 Chernomorsky S, Segelman A, Poretz R. Effect of dietary chlorophyll derivatives on mutagenesis and tumor cell growth. Teratog. Carcinog.  Mutagen.. 1999;  19 313-22
  • 10 Ohshima T, Hirata M, Oda T, Sasaki A, Shiratsuchi M. Pheophorbide a, a potent endothelin receptor antagonist for both ETA and ETB subtype. Chem. Pharm.  Bull.. 1994;  42 2174-6
  • 11 Heinrich M, Bork P M, Schmitz M L, Rimpler H, Frei B, Sticher O. Pheophorbide a from Solanum diflorum interferes with NF-kappa B activation.  Planta Med.. 2001;  67 156-7
  • 12 Kim Y K, Lee H W, Son K H, Kwon B M, Jeong T S, Lee D H, Shin J, Seo Y, Kim S U, Bok S H. GERI-BP002-A, novel inhibitor of Acyl-CoA:cholesterol acyltransferase produced by Aspergillus fumigatus F93. J.  Antibiotics. 1996;  49 31-6
  • 13 Rho M -C, Toyoshima M, Hayashi M, Uchida R, Shiomi K, Komiyama K, Omura S. Enhancement of drug accumulation by andrastin A produced by Penicillium sp. FO-3929 in vincristine-resistant KB cells. J.  Antibiotics. 1998;  51 68-72

Young-Kook Kim Ph. D.

Cardiovascular Research Laboratory

Korea Research Institute of Bioscience and Biotechnology

Taejon 305-333, Korea

Phone: +82-42-860-4556,

Fax: +82-42-861-2675

Email: kimyk@mail.kribb.re.kr