Inhibitory effect of chalcones and their derivatives from Glycyrrhiza inflata on protein tyrosine phosphatase 1B.
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).
Yoon
Goo
G
KIST Gangneung Institute, Gangneung, Republic of Korea.
Lee
Woojung
W
Kim
Su-Nam
SN
Cheon
Seung Hoon
SH
D047188:Chalcones / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D006035:Glycyrrhiza / Q000737:chemistry*; D010936:Plant Extracts / Q000737:chemistry; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D047188:Chalcones; D010936:Plant Extracts; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1