Lithospermic acid derivatives from Lithospermum erythrorhizon increased expression of serine palmitoyltransferase in human HaCaT cells

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1815-7. doi: 10.1016/j.bmcl.2009.01.052. Epub 2009 Jan 22.

Abstract

A MeOH extract of the dry root of Lithospermum erythrorhizon showed strong increasing effect on serine palmitoyltransferase (SPT) in normal human keratinocyte cells (HaCaT cells). Bioassay-guided separation on this extract using repeated chromatography resulted in the isolation of lithospermic acid (1) and two derivative esters, 9''-methyl lithospermate (2) and 9'-methyl lithospermate (3). Compounds 1-3 significantly increased SPT expressions in the relative quantity (%) of SPT1 mRNA as well as SPT2 mRNA. These constituents also raised the level of SPT protein in HaCaT cells in a dose-dependent manner, with the increased level of SPT protein in HaCaT cells of 55%, 23%, and 81% at the concentration of 100 microg/ml, respectively. This finding suggests that lithospermic acid and its derivatives from L. erythrorhizon might improve the permeability barrier by stimulating the protein level of SPT.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzofurans / chemistry*
  • Cell Line, Tumor
  • Chemistry, Pharmaceutical / methods*
  • Depsides / chemistry*
  • Drug Design
  • Gene Expression Regulation*
  • Genes, Reporter
  • Humans
  • Keratinocytes / metabolism*
  • Lithospermum / metabolism*
  • Models, Chemical
  • NF-kappa B / metabolism
  • Permeability
  • RNA, Messenger / metabolism
  • Serine C-Palmitoyltransferase / chemistry*

Substances

  • Benzofurans
  • Depsides
  • NF-kappa B
  • RNA, Messenger
  • lithospermic acid
  • Serine C-Palmitoyltransferase