Inhibition of phospholipase Cγ1 activity by amentoflavone isolated from Selaginella tamariscina

Abstract

Amentoflavone was isolated as an inhibitor of phospholipase Cγ1 (PLCγ1) and phosphoinositides (PI)-turnover in PLCγ1 overexpressing NIH3T3 fibroblasts (NIH3T3γ1) from Selaginella tamariscina (Selaginellaceae) together with other related biflavonoids, isocryptomerin and cryptomerin B. Only amentoflavone inhibited the PLCγ1 activity with an IC50 of 29 μM and the formation of total inositol phosphates (IP(t) in PDGF-stimulated NIH3T3γ1 with an IC50 of 9.2 μM but did not show inhibitory activity against protein kinase C. Isocryptomerin and cryptomerin B did not show inhibitory activity against PLCγ1 at the concentration of 150 μ M, and did not inhibit IP(t) production in PDGF-induced NIH3T3γ1 at the concentration of 180 μM.