Isolation of the Acetylcholinesterase Inhibitor Ungeremine from Nerine bowdenii by Preparative HPLC Coupled On-Line to a Flow Assay System(Pharmacognosy)

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概要

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• In an attempt to isolate the active compound while detecting acetylcholinesterase inhibitory activity, we applied a fluorometric flow assay system to an on-line coupled preparative HPLC. The MeOH extract of Nerine bowdenii showed a strong inhibitory peak in the on-line assay, and the active compound was isolated by CPC and HPLC. It was identified as ungeremine by analysis of its ^1H-NMR, 2D-NMR, and NOESY spectra. The assignment of the active N, bowdenii constituent was also confirmed by co-TLC, co-HPLC, and co-^1H-NMR experiments using an authentic sample of synthetic ungeremine. The IC_<50> value of ungeremine was 0.35μM, showing stronger activity than galanthamine (2.2 μM).

• 公益社団法人日本薬学会の論文
• 2004-11-01

著者

• VERPOORTE Robert

  Division of Pharmacognosy, Leiden/Amsterdam Center for Drug Research, Gorlaeus Laboratories

• Rhee In

  Division Of Pharmacognosy Section Metabolomics Institute Of Biology Leiden University

• Verpoorte Robert

  Division Of Pharmacognosy Center For Bio-pharmaceutical Sciences Leiden University

• APPELS Natalie

  Assay Development Department Screen Tec. BV.

• HOFTE Bertil

  Division of Analytical Chemistry, LeidenlAmsterdam Center for Drug Research, Gorlaeus Laboratories,

• KARABATAK Bahadir

  Division of Analytical Chemistry, LeidenlAmsterdam Center for Drug Research, Gorlaeus Laboratories,

• ERKELENS Cornells

  NMR Department, Leiden Institute of Chemistry, Leiden University; Leiden, The Netherlands

• STARK Lucy

  Department of Chemistry, The Skaggs Institute for Chemical Biology, The Scripps Research Institute

• FLIPPIN Lee

  Departemtn of Medicinal Chemistry, FibroGen Inc.

• Stark Lucy

  Department Of Chemistry The Skaggs Institute For Chemical Biology The Scripps Research Institute

• Flippin Lee

  Departemtn Of Medicinal Chemistry Fibrogen Inc.

• Hofte Bertil

  Division Of Analytical Chemistry Leidenlamsterdam Center For Drug Research Gorlaeus Laboratories Lei

• Karabatak Bahadir

  Division Of Analytical Chemistry Leidenlamsterdam Center For Drug Research Gorlaeus Laboratories Lei

• Erkelens Cornells

  Nmr Department Leiden Institute Of Chemistry Leiden University; Leiden The Netherlands

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