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Protein tyrosine phosphatase 1B inhibitory activity of 24‐norursane triterpenes isolated from Weigela subsessilis
Author(s) -
Na MinKyun,
Thuong Phuong Thien,
Hwang In Hyun,
Bae KiHwan,
Kim Bo Yeon,
Osada Hiroyuki,
Ahn Jong Seog
Publication year - 2010
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.3203
Subject(s) - terpene , caprifoliaceae , enzyme , in vitro , biochemistry , chemistry , protein tyrosine phosphatase , stereochemistry , biological activity , biology , traditional medicine , botany , medicine
During the screening effort to discover new types of protein tyrosine phosphatase 1B (PTP1B) inhibitors, it was found that a MeOH extract of the leaves and stems of Weigela subsessilis (Caprifoliaceae) inhibited the enzyme activity. By means of an in vitro bioassay‐guided fractionation on the MeOH extract, two 24‐norursane triterpenes, ilekudinol A (1) and ilekudinol B (2), were isolated as active metabolites. Compounds 1 and 2 inhibited PTP1B with IC 50 values of 29.1 ± 2.8 and 5.3 ± 0.5 μM, respectively. Kinetic studies suggest that both 1 and 2 are non‐competitive inhibitors of PTP1B. The findings indicate that the free carboxyl group at C‐28 in this type of triterpenes plays a critical role in the inhibition of PTP1B. Copyright © 2010 John Wiley & Sons, Ltd.