FPTase inhibition effect of protostanes from Alismatis Rhizoma and derivatives from alisol B 23-acetate = 택사(Alismatis Rhizoma)에서 분리한 Protostane계 화합물과 그 유도체의 FPTase 억제활성

Abstract

The purpose of this research is to study of inhibitory activity of protostane type triterpens against farnesyl-protein transferase (FPTase). The ingredients of Alismatis Rhizoma, alisol B 23-acetate, C 23-acetate, alisols B and A 24-acetate, and thirteen synthetic analogues from alisol B 23-acetate exhibited inhibition activity against FPTase by scintillation proximity assay method. As a result, alisol C 23-acetate, one of the constituents of Alismatis Rhizoma, the synthetic analogues carboxylated and hydroxylated on branch chain of protostane exhibited a significant inhibitory activity. However, the compounds significantly lowered the inhibitory activity, when there is no 3 position keto on protostane skeletone.