Planta Med 2002; 68(5): 407-411
DOI: 10.1055/s-2002-32081
Original Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

Hepatoprotective Phenylpropanoids from Scrophularia buergeriana Roots against CCl4-Induced Toxicity: Action Mechanism and Structure-Activity Relationship

Eun Ju Lee1 , So Ra Kim1 , Jinwoong Kim1 , Young Choong Kim1
  • 1College of Pharmacy, Seoul National University, Seoul, Korea
Further Information

Publication History

July 13, 2001

November 9, 2001

Publication Date:
07 June 2002 (online)

Abstract

Phenylpropanoids isolated from the roots of Scrophularia buergeriana MIQ. (Scrophulariaceae) protected primary cultures of rat hepatocytes from toxicity induced by carbon tetrachloride (CCl4). In this report, we show that two of these phenylpropanoids, 4-O-E-p-methoxycinnamoyl-α-L-rhamnopyranoside ester (1) and p-methoxycinnamic acid (3) have significant hepatoprotective activity; another phenylpropanoid used for comparison, isoferulic acid (11), was equally active. To determine the mechanism(s) by which these three phenylpropanoids exerted their hepatoprotective activity, we measured activities of enzymes involved in the glutathione (GSH) redox system and assayed the level of hepatic mitochondrial GSH. The GSH levels in primary cultures of rat hepatocytes were significantly reduced with CCl4 insult, but were significantly preserved by the treatment with these three phenylpropanoids. The activities of glutathione disulfide reductase and glutathione-S-transferase which normally decrease in CCl4-injured rat hepatocytes were significantly preserved by the treatment with these three phenylpropanoids. In addition, in CCl4-injured rat hepatocytes, the increased formation of malondialdehyde, a byproduct of lipid peroxidation, was reduced by the treatment with these phenylpropanoids. We determined the essential structural moiety within these three phenylpropanoids needed to exert hepatoprotective activity. The α,β-unsaturated ester moiety seemed to be essential for exerting hepatoprotective activity.

Abbreviations

CCl4:carbon tetrachloride

GSH:glutathione

MDA:malondialdehyde

GST:glutathione-S-transferase

GPx:glutathione peroxidase

GR:glutathione disulfide reductase

References

Dr. Young Choong Kim

College of Pharmacy, Seoul National University, San 56 - 1, Shillim-Dong,
Kwanak-Gu

Seoul, 151 - 742, Korea

Phone: 82-2-880-7842

Fax: 82-2-888-2933

Email: [email protected]