PTP1B inhibitory activity of kaurane diterpenes isolated from Siegesbeckia glabrescens

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Title
PTP1B inhibitory activity of kaurane diterpenes isolated from Siegesbeckia glabrescens
Author(s)
S Kim; M Na; H Oh; Junpil Jang; C B Sohn; Bo Yeon Kim; Won Keun Oh; Jong Seog Ahn
Bibliographic Citation
Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 21, no. 4, pp. 379-383
Publication Year
2006
Abstract
Protein tyrosine phosphatase 1B (PTP1B) is considered as a therapeutic target for the treatment of diabetes and obesity. In our preliminary screening study, a MeOH extract of the aerial part of Siegesbeckia glabrescens was found to inhibit PTP1B activity at 30 μg/mL. Bioassay-guided fractionation led to the isolation of two active diterpenes, ent-16βH,17-isobutyryloxy-kauran-19-oic acid (1) and ent-16βH,17-acetoxy-18-isobutyryloxy-kauran-19-oic acid (2), along with ent-16βH,17-hydroxy-kauran-19-oic acid (3). Compounds 1 and 2 inhibited the PTP1B activity with IC50 values of 8.7 ± 0.9 and 30.6 ± 2.1 μM, respectively. Kinetic studies suggest that both 1 and 2 are non-competitive inhibitors of PTP1B. However, compound 3 substituted with a hydroxyl group at C-17 in kaurane-type showed no inhibitory effects towards PTP1B.
Keyword
17-acetoxy-18-isobutyryloxy-kauran-19-oic acid17-isobutyryloxy-kauran-19-oic acident-16βHinhibitionkaurane diterpenesnon-competitive inhibitorsprotein tyrosine phosphatase 1Bsiegesbeckia glabrescens
ISSN
1475-6366
Publisher
T&F (Taylor & Francis)
DOI
http://dx.doi.org/10.1080/14756360600741560
Type
Article
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
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