[Effect of seven kinds of flavonoids on recombinant human protein tyrosine phosphatase].
OBJECTIVE
To observe the effects of seven kinds of flavonoids on recombinant human phosphatase of regenerating liver-3 activity.


METHODS
The inhibitory effect of flavonoids was tested by DiFMUP assay. Calculation of IC50 values was performed according to the law of semi-effect-probit.


RESULTS
Myricetin and gossypin could significantly inhibit recombinant PRL-3 activity in a concentration dependent manner with IC50 values of 55.54 and 68.86 micromol/L, respectively. Quercetin, luteolin and 7,8-Dihydroxyflavone had a weak inhibitory effect with IC50 values of 113.38, 151.56 and 249.49 micromol/L. respectively. While 3-hydroxyflavone and 6-hydroxyflavone had no significant effect on PRL-3 activity. Structure activity study indicated that C4 and C7 hydroxyls on the flavone skeleton were key functional groups to influencing PRL-3 inhibotory activity. The inhibitory effect of flavonoids on PRL-3 was increased with the number of hydroxyl group.


CONCLUSIONS
Myricetin and gossypin were two strong inhibitors on recombinant human protein tyrosine phosphatase PRL-3.
He
Tai-ping
TP
Institute of Biochemistry and Molecular Biology, Guangdong Medical College, Zhanjiang 524023, China. taipinghe@163.com
Liang
Nian-ci
NC
Lin
Xiao-cong
XC
Liu
Wen
W
D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D010957:Plasmids; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D011794:Quercetin / Q000494:pharmacology; D011994:Recombinant Proteins / Q000096:biosynthesis / Q000235:genetics; D011995:Recombination, Genetic; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D005419:Flavonoids; D011994:Recombinant Proteins; C040015:myricetin; D011794:Quercetin; C022944:gossypin; D017027:Protein Tyrosine Phosphatases