Carnosic acid, a new class of lipid absorption inhibitor from sage

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1943-6. doi: 10.1016/j.bmcl.2004.01.091.

Abstract

The methanolic extract from the leaves of Salvia officinalis L. (sage) showed significant inhibitory effect on serum triglyceride elevation in olive oil-loaded mice (500 and 1000 mg/kg, p.o.) and inhibitory activity (IC(50): 94 microg/mL) against pancreatic lipase, which is participated in digestion of lipids. Through bioassay-guided separation using the inhibitory activity against pancreatic lipase activity, 4 abietan-type diterpenes (carnosic acid, carnosol, royleanonic acid, 7-methoxyrosmanol) and a triterpene (oleanolic acid) were isolated from the active fraction. Among these compounds, carnosic acid and carnosol substantially inhibited pancreatic lipase activity with IC(50) values of 12 microg/mL (36 microM) and 4.4 microg/mL (13 microM), respectively. Carnosic acid significantly inhibited triglyceride elevation in olive oil-loaded mice at doses of 5-20 mg/kg (p.o.). However, other constituents (carnosol, royleanonic acid, oleanolic acid) did not show any effects at a dose of 200 mg/kg (p.o.). Furthermore, carnosic acid (20 mg/kg/day, p.o.) reduced the gain of body weight and the accumulation of epididymal fat weight in high fat diet-fed mice after 14 days.

MeSH terms

  • Abietanes
  • Animals
  • Dietary Fats / administration & dosage
  • Diterpenes / classification
  • Diterpenes / pharmacology*
  • Hypolipidemic Agents / classification
  • Hypolipidemic Agents / pharmacology*
  • Intestinal Absorption / drug effects*
  • Lipase / antagonists & inhibitors
  • Lipase / metabolism
  • Lipid Metabolism
  • Lipids / antagonists & inhibitors*
  • Male
  • Mice
  • Molecular Structure
  • Organ Size / drug effects
  • Pancreas / enzymology
  • Plant Extracts / classification
  • Plant Extracts / pharmacology*
  • Plant Leaves / chemistry
  • Salvia officinalis / chemistry*
  • Triglycerides / blood

Substances

  • Abietanes
  • Dietary Fats
  • Diterpenes
  • Hypolipidemic Agents
  • Lipids
  • Plant Extracts
  • Triglycerides
  • Lipase
  • salvin