Inhibition of protein tyrosine phosphatase 1B by Ursane-type triterpenes isolated from Symplocos paniculata

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Title
Inhibition of protein tyrosine phosphatase 1B by Ursane-type triterpenes isolated from Symplocos paniculata
Author(s)
Min Kyun Na; Seungmi Yang; Long He; H Oh; B S Kim; Won Keun Oh; Bo Yeon KimJong Seog Ahn
Bibliographic Citation
Planta Medica, vol. 72, no. 3, pp. 261-263
Publication Year
2006
Abstract
Inhibition of protein tyrosine phosphatase IB (PTP1B) has been proposed as a therapy for treatment of type 2 diabetes and obesity. Bioassay-guided fractionation of the MeOH extract of the leaves and stems of Symplocos paniculata (Thunb.) Miq. (Symplocaceae), using an in vitro PTP1B inhibitory assay, resulted in the isolation of three ursane-type triterpenes, ursolic acid (1), corosolic acid (2) and 2α,3α,19α,23-tetrahydroxyurs-12- en-28-oic acid (3). Compounds 1-3 inhibited PTP1B with IC50 values of 3.8 ± 0.5, 7.2 ± 0.8 and 42.1 ± 1.5 μM, respectively. Kinetic studies suggest that 1 is a competitive inhibitor with a Ki value of 2.0 μM, whereas 2 is a mixed-type inhibitor of PTP1B. Our results indicate that the substitution of hydroxy groups on the ursane-type triterpenes is responsible for the loss of activity, and thus 1 and 2 possessing only one or two hydroxy groups can be potential PTP1B inhibitors.
ISSN
0032-0943
Publisher
Georg Thieme Verlag Kg
DOI
http://dx.doi.org/10.1055/s-2005-873194
Type
Article
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
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