Acetylcholinesterase-inhibiting steroidal alkaloid from the sponge Corticium sp.

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• 作者：Roosanee Langjae ; Somchai Bussarawit ; Supreeya Yuenyongsawad ; Kornkanok Ingkaninan ; Anuchit Plubrukarn
• 关键词：4-Acetoxy-plakinamine B ; Corticium ; Acetylcholinesterase inhibitors ; Steroidal alkaloids
• 刊名：Steroids
• 出版年：2007
• 期刊代码：142_0039128x
• 类别：bio
• 出版时间：September 2007
• 卷：72
• 期：9-10
• 页码：682-685
• 文件大小：255 K

摘要

A new stigmastane-type steroidal alkaloid, 4-acetoxy-plakinamine B (1), was isolated from the Thai sponge Corticium sp. The compound was subjected to the acetylcholinesterase inhibitory activity determination to reveal a high inhibitory activity (IC₅₀ 3.75 ± 1.69 μM). The kinetics of enzyme inhibition showed a decrease in V_max, whereas K_m was increased, thus suggesting an unusual mixed-competitive mode of inhibition. Compound 1 is the first steroidal alkaloid bearing a stigmastane skeleton ever been reported to exhibit such good potency in the acetylcholinesterase inhibition bioassay.