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PTP1B inhibitory effect of abietane diterpenes isolated from Salvia miltiorrhiza

被引：36
作者：
Han, YM
Oh, H
Na, MK
Kim, BS
Oh, WK
Kim, BY
Jeong, DG
Ryu, SE
Sok, DE
Ahn, JS
机构：
[1] Korea Res Inst Biosci & Biotechnol, Taejon 305333, South Korea
[2] Silla Univ, Coll Nat Sci, Sasang Gu 617736, Busan, South Korea
[3] Chungnam Natl Univ, Coll Pharm, Taejon 305764, South Korea
来源：
BIOLOGICAL & PHARMACEUTICAL BULLETIN | 2005年 / 28卷 / 09期
关键词：
salvia miltiorrhiza; Labiatae; protein tyrosine phosphatase 1B (PTP1B) inhibitor; isotanshinone IIA; dihydroisotanshinone I; isocryptotanshinone;
D O I：
10.1248/bpb.28.1795
中图分类号：
R9 [药学];
学科分类号：
1007 ;
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 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 1 (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 mu M, 22.4 +/- 0.6 mu M and 56.1 +/- 6.3 mu M, respectively.
引用
收藏
页码：1795 / 1797
页数：3
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