Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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PTP1B Inhibitory Effect of Abietane Diterpenes Isolated from Salvia miltiorrhiza
Yu Mi Han, 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
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Keywords: Salvia miltiorrhiza, Labiatae, protein tyrosine phosphatase 1B (PTP1B) inhibitor, isotanshinone IIA, dihydroisotanshinone I, isocryptotanshinone
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2005 Volume 28 Issue 9 Pages 1795-1797

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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 μM, 22.4±0.6 μM and 56.1±6.3 μM, respectively.

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© 2005 The Pharmaceutical Society of Japan
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