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标题：Anti-diabetic Properties of Chrysophanol and Its Glucoside from Rhubarb Rhizome
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作者：Myung Sun Lee ; Cheon Bae Sohn
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2008
卷号：31
期号：11
页码：2154-2157
DOI：10.1248/bpb.31.2154
出版社：The Pharmaceutical Society of Japan
摘要：An ethanol extract of rhubarb rhizome exhibited marked glucose transport activity in differentiated L6 rat myotubes. Activity-guided fractionation resulted in the isolation of two anthraquinones, chrysophanol-8- O -β- D -glucopyranoside (1) and chrysophanol (2). The anti-diabetic effect was examined by glucose transport activity, glucose transporter 4 (Glut4) expression in myotubes, and the level of insulin receptor (IR) tyrosine phosphorylation as influenced by tyrosine phosphatase 1B, each of which is a major target of diabetes treatment. Chrysophanol-8- O -β- D -glucopyranoside up to 25 μ M dose-dependently activated glucose transport in insulin-stimulated myotubes. Increased tyrosine phosphorylation of IR due to tyrosine phosphatase 1B inhibitory activity with an IC₅₀ value of 18.34±0.29 μ M and unchanged Glut4 mRNA levels was observed following chrysophanol-8- O -β- D -glucopyranoside treatment. Chrysophanol up to 100 μ M exerted mild glucose transport activity and elevated the tyrosine phosphorylation of IR via tyrosine phosphatase 1B inhibition (IC₅₀=79.86±0.12 μ M ); Glut4 mRNA expression was also significantly increased by 100 μ M . The ED₅₀ values of the two compounds were 59.38±0.66 and 79.69±0.03 μ M , respectively. Therefore, these two anthraquinones from rhubarb rhizome, chrysophanol-8- O -β- D -glucopyranoside and chrysophanol, have mild cytotoxicity and anti-diabetic properties and could play metabolic roles in the insulin-stimulated glucose transport pathway.
关键词：rhubarb;anthraquinone;diabetes;glucose transport