PTP1B Inhibitory Effect of Abietane Diterpenes Isolated from Salvia miltiorrhiza

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 roo...

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Bibliographic Details
Published in:Biological & Pharmaceutical Bulletin 2005, Vol.28(9), pp.1795-1797
Main Authors: Han, Yu Mi, Oh, Hyuncheol, Na, MinKyun, Kim, Beom Seok, Oh, Won Keun, Kim, Bo Yeon, Jeong, Dae Gwin, Ryu, Seong Eon, Sok, Dai-Eun, Ahn, Jong Seog
Format: Article
Language:English
Subjects:
dihydroisotanshinone I
Diterpenes, Abietane - chemistry
Diterpenes, Abietane - isolation & purification
Diterpenes, Abietane - pharmacology
Hydrolysis
isocryptotanshinone
isotanshinone IIA
Kinetics
Labiatae
Magnetic Resonance Spectroscopy
Mass Spectrometry
Plant Roots - chemistry
protein tyrosine phosphatase 1B (PTP1B) inhibitor
Protein Tyrosine Phosphatase, Non-Receptor Type 1
Protein Tyrosine Phosphatases - antagonists & inhibitors
Salvia - chemistry
Salvia miltiorrhiza
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Summary: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 μM, 22.4±0.6 μM and 56.1±6.3 μM, respectively.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.28.1795