Inhibition of phospholipase C gamma 1 by the prenylated flavonoids from Sophora flavescens.
The effect on the phospholipase C gamma 1 activity of eleven prenylated flavonoids from Sophora flavescens was investigated. These flavonoids exhibited relatively strong inhibitory activity with IC50 values ranged from 7.5 x 10(-6) M to 35 x 10(-5) M with the exception of kushenol H (4) (IC50 value; > 5.3 x 10(-4) M). The presence of C3-OH resulted in a significant diminution of activity and the configuration of C3-OH is likely to be another factor influencing the activity. In addition, hydration of the C-4"'-C-5"' double bond of the lavandulyl side chain caused complete loss of activity. These data suggest that the presence and configuration of C3-OH are related to the inhibitory activity and the lavandulyl side chain is also important for high inhibitory activity against PLC gamma 1.
Lee
H S
HS
Ko
H R
HR
Ryu
S Y
SY
Oh
W K
WK
Kim
B Y
BY
Ahn
S C
SC
Mheen
T I
TI
Ahn
J S
JS
D000818:Animals; D002417:Cattle; D002531:Cerebellum / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D051966:Phospholipase C gamma; D013329:Structure-Activity Relationship; D010738:Type C Phospholipases / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D005419:Flavonoids; D007527:Isoenzymes; D010738:Type C Phospholipases; D051966:Phospholipase C gamma