Lithospermic acid derivatives from Lithospermum erythrorhizon increased expression of serine palmitoyltransferase in human HaCaT cells.
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.
Thuong
Phuong Thien
PT
College of Pharmacy, Chosun University, 375 Seosuk-dong, Dong-gu, Gwangju 501-759, Republic of Korea.
Kang
Keon Wook
KW
Kim
Jeong Kee
JK
Seo
Dae Bang
DB
Lee
Sang Jun
SJ
Kim
Sung Han
SH
Oh
Won Keun
WK
D001572:Benzofurans / Q000737:chemistry*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D053630:Depsides / Q000737:chemistry*; D015195:Drug Design; D005786:Gene Expression Regulation; D017930:Genes, Reporter; D006801:Humans; D015603:Keratinocytes / Q000378:metabolism*; D029684:Lithospermum / Q000378:metabolism*; D008956:Models, Chemical; D016328:NF-kappa B / Q000378:metabolism; D010539:Permeability; D012333:RNA, Messenger / Q000378:metabolism; D051102:Serine C-Palmitoyltransferase / Q000737:chemistry*
D001572:Benzofurans; D053630:Depsides; D016328:NF-kappa B; D012333:RNA, Messenger; C046833:lithospermic acid; D051102:Serine C-Palmitoyltransferase