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Title 

PTP1B inhibitory effects of tridepside and related metabolites isolated from the Antarctic lichen Umbilicaria antarctica

Authors 

C SeoY H ChoiJong Seog AhnJ H YimH K LeeH Oh

Publisher 

Informa Healthcare

Issue Date 

2009

Citation 

Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 24, no. 5, pp. 1133-1137

Keywords 

Antarctic lichenLichen metabolitesNon-competitive inhibitorProtein tyrosine phosphatase 1B (PTP1B)Umbilicaria antarctica

Abstract 

The selective inhibition of PTP1B has been widely recognized as a potential drug target for the treatment of type 2 diabetes and obesity. In the course of screening for PTP1B inhibitory natural products, the MeOH extract of the dried sample of the Antarctic lichen Umbilicaria antarctica was found to exhibit significant inhibitory effect, and the bioassay-guided fractionation and purification afforded three related lichen metabolites 1-3. Compounds 1-3 were identified as gyrophoric acid (1), lecanoric acid (2), and methyl orsellinate (3) mainly by analysis of NMR and MS data. These compounds inhibited PTP1B activity with 50% inhibitory concentration values of 3.6 ± 0.04 μM, 31 ± 2.7 μM, and 277 ± 8.6 μM, respectively. Furthermore, the kinetic analysis of PTP1B inhibition by compound 1 suggested that the compound inhibited PTP1B activity in a non-competitive manner.

ISSN 

1475-6366

Link 

http://dx.doi.org/10.1080/14756360802667811

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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