PTP1B inhibitory effects of tridepside and related metabolites isolated from the Antarctic lichen Umbilicaria antarctica
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- PTP1B inhibitory effects of tridepside and related metabolites isolated from the Antarctic lichen Umbilicaria antarctica
- Other Titles
- 남극지의류 Umbilicaria antarctica로 부터 분리한 tridepside의 PTP1B 저해효과
- Changon Seo
Jong Seog Ahn
Lee, Hong Kum
Yim, Joung Han
- Biochemistry & Molecular Biology; Pharmacology & Pharmacy
- Antarctic lichen; Lichen metabolites; Non-competitive inhibitor; Protein tyrosine phosphatase 1; Umbilicaria antarctica
- Issue Date
- Informa helthcare
- Changon Seo, et al. 2009. "PTP1B inhibitory effects of tridepside and related metabolites isolated from the Antarctic lichen Umbilicaria antarctica". JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 24(5): 1133-1137.
- 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.
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