Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 24, Issue 5, Pages 1133-1137Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756360802667811
Keywords
Umbilicaria antarctica; Antarctic lichen; Lichen metabolites; Protein tyrosine phosphatase 1B (PTP1B); Non-competitive inhibitor
Funding
- KOPRI [PE08050]
- Ministry of Education, Science & Technology (MoST), Republic of Korea [PE08050] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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 mu M, 31 +/- 2.7 mu M and 277 +/- 8.6 mu M, respectively. Furthermore, the kinetic analysis of PTP1B inhibition by compound 1 suggested that the compound inhibited PTP1B activity in a non-competitive manner.
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