Thirteen known (1–12 and 16) and three previously undescribed Amaryllidaceae alkaloids of belladine structural type, named carltonine A-C (13–15), were isolated from bulbs of Narcissus pseudonarcissus cv. Carlton (Amaryllidaceae) by standard chromatographic methods. Compounds isolated in sufficient amounts, and not tested previously, were evaluated for their in vitro acetylcholinesterase (AChE; E.C. 3.1.1.7), butyrylcholinesterase (BuChE; E.C. 3.1.1.8) and prolyl oligopeptidase (POP; E.C. 3.4.21.26) inhibition activities. Significant human BuChE (hBUChE) inhibitory activity was demonstrated by newly described alkaloids carltonine A (13) and carltonine B (14) with IC₅₀ values of 913 ± 20 nM and 31 ± 1 nM, respectively. Both compounds displayed a selective inhibition pattern for hBuChE with an outstanding selectivity profile over AChE inhibition, higher than 100. The in vitro data were further supported by in silico studies of the active alkaloids 13 and 14 in the active site of hBuChE.

中文翻译：

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水仙假水仙的颠茄类型的芳科生物碱。卡尔顿作为丁酰胆碱酯酶的新的选择性抑制剂。

从水仙假鳞茎的鳞茎中分离出十三种已知的（1 – 12和16）和三个以前未描述的颠茄结构类型的金石科生物碱，称为carltonine AC（13 – 15）。卡尔顿（Amaryllidaceae）采用标准色谱法。评估了足够量且未事先测试的化合物的体外乙酰胆碱酯酶（AChE; EC 3.1.1.7），丁酰胆碱酯酶（BuChE; EC 3.1.1.8）和脯氨酰寡肽酶（POP; EC 3.4.21.26）抑制活性。新描述的生物碱肉碱A证明了人类BuChE（h BUChE）的显着抑制活性（13）和卡尔顿B（14）的IC ₅₀值分别为913±20 nM和31±1 nM。两种化合物均显示出对h BuChE的选择性抑制模式，其选择性优于AChE抑制，高于100。在计算机上研究了h BuChE活性位点中的活性生物碱13和14，进一步支持了体外数据。