PTP1B Inhibitory Effect of Abietane Diterpenes Isolated from Salvia miltiorrhiza

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Author(s)

Abstract

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 <i>Salvia miltiorrhiza</i> B<small>UNGE</small> (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<small>M</small>, 22.4±0.6 μ<small>M</small> and 56.1±6.3 μ<small>M</small>, respectively.

Journal

  • Biological and Pharmaceutical Bulletin

    Biological and Pharmaceutical Bulletin 28(9), 1795-1797, 2005

    The Pharmaceutical Society of Japan

Cited by:  1

Codes

  • NII Article ID (NAID)
    110003666516
  • NII NACSIS-CAT ID (NCID)
    AA10885497
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    0918-6158
  • NDL Article ID
    7410108
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-V41
  • Data Source
    CJPref  NDL  NII-ELS  J-STAGE 
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