Nair Jerald J, van Staden Johannes
Research Centre for Plant Growth and Development, School of Life Sciences, University of KwaZulu-Natal Pietermaritzburg, Scottsville, 3209, South Africa.
Nat Prod Commun. 2012 Jul;7(7):959-62.
The plant family Amaryllidaceae occupies a privileged status within the botanical hierarchy due to its horticultural and ornamental appeal, as well as its widespread usage in the traditional medicinal practices of indigenous peoples across the globe. Of greater significance are the unique, structurally-diverse alkaloid constituents produced by members of the family, which has spawned several biologically significant molecules. In this regard, the Alzheimer's drug galanthamine has gained much prominence due to its selective and reversible inhibitory interaction with the enzyme acetylcholinesterase (AChE), of significance in the progression of neurodegeneration associated with Alzheimer's disease (AD). The lycorine series of compounds within the family have recently emerged as novel inhibitors of AChE, in some instances with higher levels of activity compared with the commercial drug galanthamine, making them attractive targets for natural product and synthetically-driven structure-activity relationship studies. This brief survey traces the emergence of lycorine compounds over the past decade as promising leads in the therapeutic approach towards AD and their possible future advancement onto the clinical stage.
石蒜科植物在植物分类体系中占据着特殊地位，这归因于其园艺和观赏价值，以及在全球各地原住民传统医学实践中的广泛应用。更重要的是，该科植物成员能产生独特的、结构多样的生物碱成分，由此衍生出了多种具有生物学意义的分子。在这方面，治疗阿尔茨海默病的药物加兰他敏备受瞩目，因为它与乙酰胆碱酯酶（AChE）存在选择性且可逆的抑制性相互作用，这在与阿尔茨海默病（AD）相关的神经退行性变进程中具有重要意义。该科植物中的石蒜碱系列化合物最近已成为新型AChE抑制剂，在某些情况下，其活性水平高于商业药物加兰他敏，这使其成为天然产物以及合成驱动的构效关系研究的有吸引力的靶点。本简要综述追溯了过去十年石蒜碱类化合物作为治疗AD的有前景的先导物的出现情况，以及它们未来可能迈向临床阶段的进展。
