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KMID : 0616120110420030218
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Korean Journal of Pharmacognosy
2011 Volume.42 No. 3 p.218 ~ p.222
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FPTase Inhibition Effect of Protostanes from Alismatis Rhizoma and Derivatives from Alisol B 23-acetate
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Lee Sang-Myung
Kwon Byoung-Mog
Min Byung-Sun
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Abstract
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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.
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KEYWORD
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Alismatis Rhizoma, Alisol, Farnesyl-protein transferase (FPTase)
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