Protein tyrosine phosphatase 1B inhibitory effects of depsidone and pseudodepsidone metabolites from the Antarctic lichen Stereocaulon alpinum
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- Protein tyrosine phosphatase 1B inhibitory effects of depsidone and pseudodepsidone metabolites from the Antarctic lichen Stereocaulon alpinum
- Other Titles
- 남극 Stereocaulon alpinum 유래 PTP1B 저해효과를 가지는 depsidone 및 pseudodepsidone계 물질
- Lee, Hong Kum
Ahn, Jong Seog
Yim, Joung Han
Sohn, Jae Hak
- Pharmacology & Pharmacy; Chemistry
- Depsidones; Lichen metabolites; Non-competitive inhibitors; PTP1B; Stereocaulon alpinum
- Issue Date
- Lee, Hong Kum, et al. 2009. "Protein tyrosine phosphatase 1B inhibitory effects of depsidone and pseudodepsidone metabolites from the Antarctic lichen Stereocaulon alpinum". BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1(19): 2801-2803.
- Seven phenolic lichen metabolites (1？7) have been isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum by various chromatographic methods. The structures of these compounds were determined mainly by analysis of NMR spectroscopic data. A depsidone-type compound, lobaric acid (1) and two pseudodepsidone-type compounds, 2 and 3, exhibited potent inhibitory activity against protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 0.87 lM, 6.86 lM, and 2.48 lM, respectively. Kinetic analyses of PTP1B inhibition by compounds 1 and 2 suggested that these compounds inhibited PTP1B activity in a non-competitive manner.
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