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.
Phuong Thien Thuong  1 ,  Keon Wook Kang ,  Jeong Kee Kim ,  Dae Bang Seo ,  Sang Jun Lee ,  Sung Han Kim ,  Won Keun Oh
Affiliations
  • 1. College of Pharmacy, Chosun University, 375 Seosuk-dong, Dong-gu, Gwangju 501-759, Republic of Korea.
PMID: 19217780 DOI: 10.1016/j.bmcl.2009.01.052
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.

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