Inhibition of phospholipase C gamma 1 activity by amentoflavone isolated from Selaginella tamariscina.
Amentoflavone was isolated as an inhibitor of phospholipase C gamma 1 (PLC gamma 1) and phosphoinositides (PI)-turnover in PLC gamma 1 overexpressing NIH3T3 fibroblasts (NIH3T3 gamma 1) from Selaginella tamariscina (Selaginellaceae) together with other related biflavonoids, isocryptomerin and cryptomerin B. Only amentoflavone inhibited the PLC gamma 1 activity with an IC50 of 29 microM and the formation of total inositol phosphates (IPt) in PDGF-stimulated NIH3T3 gamma 1 with an IC50 of 9.2 microM but did not show inhibitor activity against protein kinase C. Isocryptomerin and cryptomerin B did not show inhibitor activity against PLC gamma 1 at the concentration of 150 microM, and did not inhibit IPt production in PDGF-induced NIH3T3 gamma 1 at the concentration of 180 microM.
Lee
H S
HS
Korea Research Institute of Bioscience and Biotechnology (KRIBB), Yusong, Taejon, Korea.
Oh
W K
WK
Kim
B Y
BY
Ahn
S C
SC
Kang
D O
DO
Shin
D I
DI
Kim
J
J
Mheen
T I
TI
Ahn
J S
JS
D016475:3T3 Cells; D000818:Animals; D044946:Biflavonoids; D002417:Cattle; D002531:Cerebellum / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D051379:Mice; D051966:Phospholipase C gamma; D008517:Phytotherapy; D010946:Plants, Medicinal; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000378:metabolism; D019311:Staurosporine / Q000494:pharmacology; D010738:Type C Phospholipases / Q000037:antagonists & inhibitors*
D044946:Biflavonoids; D004791:Enzyme Inhibitors; D005419:Flavonoids; D007527:Isoenzymes; C011164:amentoflavone; D011493:Protein Kinase C; D010738:Type C Phospholipases; D051966:Phospholipase C gamma; D019311:Staurosporine