KOPRI Repository

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

Cited 13 time in scopus
Metadata Downloads
Title
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
Authors
Changon Seo
Hyuncheol Oh
Jong Seog Ahn
Lee, Hong Kum
Yim, Joung Han
Yun-Hyeok Choi
Subject
Biochemistry & Molecular Biology; Pharmacology & Pharmacy
Keywords
Antarctic lichen; Lichen metabolites; Non-competitive inhibitor; Protein tyrosine phosphatase 1; Umbilicaria antarctica
Issue Date
2009
Publisher
Informa helthcare
Citation
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.
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.
URI
http://repository.kopri.re.kr/handle/201206/6369
DOI
http://dx.doi.org/10.1080/14756360802667811
Files in This Item
General Conditions
      ROMEO Green
    Can archive pre-print and post-print or publisher's version/PDF
      ROMEO Blue
    Can archive post-print (ie final draft post-refereeing) or publisher's version/PDF
      ROMEO Yellow
    Can archive pre-print (ie pre-refereeing)
      ROMEO White
    Archiving not formally supported

    qrcode

    Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

    Browse