상세 정보

underline
Metadata Downloads : dc(xml) or Excel
Cited 0 time in scopus ci

Title 

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

Authors 

Min Kyun NaSeungmi YangLong HeH OhB S KimWon Keun OhBo Yeon KimJong Seog Ahn

Publisher 

Georg Thieme Verlag

Issue Date 

2006

Citation 

Planta Medica, vol. 72, no. 3, pp. 261-263

Keywords 

protein tyrosine phosphatase 1Bsymplocos paniculata extractdrug inhibitionenzyme inhibitiondiabetes mellitus, type 2protein-tyrosine-phosphatasetriterpenessymplocos paniculata

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

Link 

http://dx.doi.org/10.1055/s-2005-873194

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


There are no files associated with this item.
qrcode

FusionCharts.
DSpace Software Coptright(c) 2010 MIT and Hewleft-Packard  /  KRIBB-REPOSITORY ( Email:jakim@kribb.re.kr)