PTP1B inhibitory effect of abietane diterpenes isolated from Salvia miltiorrhiza

  • Biol Pharm Bull. 2005 Sep;28(9):1795-7. doi: 10.1248/bpb.28.1795.
Yu Mi Han  1 ,  Hyuncheol Oh ,  MinKyun Na ,  Beom Seok Kim ,  Won Keun Oh ,  Bo Yeon Kim ,  Dae Gwin Jeong ,  Seong Eon Ryu ,  Dai-Eun Sok ,  Jong Seog Ahn
Affiliations
  • 1. Korea Research Institute of Bioscience and Biotechnology (KRIBB), Daejeon, Korea.
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 Salvia miltiorrhiza BUNGE (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 microM, 22.4+/-0.6 microM and 56.1+/-6.3 microM, respectively.

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