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  • 标题:PTP1B Inhibitory Effect of Abietane Diterpenes Isolated from Salvia miltiorrhiza
  • 本地全文:下载
  • 作者:Yu Mi Han ; Hyuncheol Oh ; MinKyun Na
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2005
  • 卷号:28
  • 期号:9
  • 页码:1795-1797
  • DOI:10.1248/bpb.28.1795
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Protein tyrosine phosphatase 1B (PTP1B) acts as a negative regulator of insulin signaling, and selective inhibition of PTP1B has served as a potential drug target for the treatment of type 2 diabetes. In the course of screening for PTP1B inhibitory natural products, the MeOH extract of the dried root of Salvia miltiorrhiza B UNGE (Labiatae) was found to exhibit significant inhibitory effect. Bioassay-guided fractionation and purification afforded three related abietane-type diterpene metabolites 1—3. Compounds 1—3 were identified as isotanshinone IIA (1), dihydroisotanshinone I (2), and isocryptotanshinone (3) mainly by analysis of NMR and MS data. Compounds 1—3 non-competitively inhibited PTP1B activity with 50% inhibitory concentration values of 11.4±0.6 μ M , 22.4±0.6 μ M and 56.1±6.3 μ M , respectively.
  • 关键词:Salvia miltiorrhiza;Labiatae;protein tyrosine phosphatase 1B (PTP1B) inhibitor;isotanshinone IIA;dihydroisotanshinone I;isocryptotanshinone
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