Evaluation of Hesperetin 7-O-lauryl Ether as Lipid-Lowering Agent in High-Cholesterol-Fed Rats

Bioorg Med Chem. 2004 Jul 1;12(13):3599-605. doi: 10.1016/j.bmc.2004.04.020.

Abstract

The lipid-lowering efficacy of hesperetin was revealed in preliminary studies on experimental animals. As such, the current study compared the effect of hesperetin 7-O-lauryl ether, with that of hesperetin and lovastatin on the lipid profile and cholesterol-regulating mechanism in high-cholesterol-fed rats. Male rats were fed a high-cholesterol diet (1%, wt/wt) or high-cholesterol diet supplemented with lovastatin (1, 0.02%, wt/wt), hesperetin (2, 0.02%, wt/wt), or hesperetin 7-O-lauryl ether (3, 0.031%, wt/wt) for six weeks. The supplemental amount of 3 was 0.066mmol/100g diet as an equivalent to the supplemental amount of 2. The plasma total cholesterol and triglyceride levels were significantly lowered by the 2 and 3 supplements compared with the control or 1-supplemented group. The hepatic HMG-CoA reductase activities were also significantly lower in all the supplemented groups compared with the control group, and the hepatic ACAT activity was significantly lower in the 2- and 3-supplemented groups. The supplementation of 3 resulted in a higher excretion of total neutral sterol and total fecal sterol compared with the control or 1-supplemented group. Accordingly, overall, compound 3, exhibited a more potent plasma lipid-lowering effect than compound 1 based on inhibiting cholesterol biosynthesis and esterification, while also increasing the fecal sterol excretion.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animal Feed
  • Animals
  • Body Weight / drug effects
  • Cholesterol, Dietary / administration & dosage
  • Cholesterol, Dietary / pharmacology*
  • Ethers / chemistry
  • Ethers / pharmacology*
  • Feces / chemistry
  • Hesperidin / chemistry
  • Hesperidin / pharmacology*
  • Hypolipidemic Agents / chemistry
  • Hypolipidemic Agents / pharmacology*
  • Lipids / analysis
  • Lipids / blood
  • Liver / drug effects
  • Liver / enzymology
  • Liver / metabolism
  • Male
  • Molecular Structure
  • Organ Size / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Sterols / metabolism
  • Weight Gain / drug effects

Substances

  • Cholesterol, Dietary
  • Ethers
  • Hypolipidemic Agents
  • Lipids
  • Sterols
  • hesperetin 7-O-lauryl ether
  • Hesperidin