title: Lithospermic acid derivatives from Lithospermum erythrorhizon increased expression of serine palmitoyltransferase in human HaCaT cells.
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.
authors.affiliation: College of Pharmacy, Chosun University, 375 Seosuk-dong, Dong-gu, Gwangju 501-759, Republic of Korea.
authors.forename: Phuong Thien
authors.initials: PT
authors.lastname: Thuong
authors.forename: Keon Wook
authors.initials: KW
authors.lastname: Kang
authors.forename: Jeong Kee
authors.initials: JK
authors.lastname: Kim
authors.forename: Dae Bang
authors.initials: DB
authors.lastname: Seo
authors.forename: Sang Jun
authors.initials: SJ
authors.lastname: Lee
authors.forename: Sung Han
authors.initials: SH
authors.lastname: Kim
authors.forename: Won Keun
authors.initials: WK
authors.lastname: Oh
mesh_terms: 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*
chemical_list: D001572:Benzofurans; D053630:Depsides; D016328:NF-kappa B; D012333:RNA, Messenger; C046833:lithospermic acid; D051102:Serine C-Palmitoyltransferase