Inhibitory effect of chalcones and their derivatives from Glycyrrhiza inflata on protein tyrosine phosphatase 1B

Goo Yoon; Woojung Lee; Su-Nam Kim; Seung Hoon Cheon

doi:10.1016/j.bmcl.2009.07.054

Inhibitory effect of chalcones and their derivatives from Glycyrrhiza inflata on protein tyrosine phosphatase 1B

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5155-7. doi: 10.1016/j.bmcl.2009.07.054. Epub 2009 Jul 24.

Authors

Goo Yoon¹, Woojung Lee, Su-Nam Kim, Seung Hoon Cheon

Affiliation

¹ KIST Gangneung Institute, Gangneung, Republic of Korea.

PMID: 19632832
DOI: 10.1016/j.bmcl.2009.07.054

Abstract

Compounds (1-6) isolated from the CH(2)Cl(2) extract of Glycyrrhiza inflata and semisynthetic licochalcone A derivatives (7-14) were evaluated for their protein tyrosine phosphatase 1B (PTP1B) inhibitory activities. Licochalcones A (4) and E (6), each with an allyl group at position 5 in the B ring exhibited significant inhibitory effects. Licochalcone A derivative 7, the most potent among the series, had an IC(50) value of 11.7+/-2.0 microM, ca. twofold better than that of licochalcone A (4).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Chalcones / chemistry*
Chalcones / isolation & purification
Chalcones / pharmacology
Glycyrrhiza / chemistry*
Plant Extracts / chemistry
Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*
Protein Tyrosine Phosphatase, Non-Receptor Type 1 / metabolism
Structure-Activity Relationship

Substances

Chalcones
Plant Extracts
Protein Tyrosine Phosphatase, Non-Receptor Type 1