ADINACO Research Group, Department of Pharmaceutical Botany, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
Department of Organic and Bioorganic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
Biomolecules. 2020 May 22;10(5):800. doi: 10.3390/biom10050800.
Thirteen known (- and ) and three previously undescribed Amaryllidaceae alkaloids of belladine structural type, named carltonine A-C (-), were isolated from bulbs of 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 (BUChE) inhibitory activity was demonstrated by newly described alkaloids carltonine A () and carltonine B () with IC values of 913 ± 20 nM and 31 ± 1 nM, respectively. Both compounds displayed a selective inhibition pattern for BuChE 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 and in the active site of BuChE.
从 cv. Carlton（石蒜科）的鳞茎中，通过标准的色谱方法分离出了 13 种已知的（和）和 3 种以前未描述的具有贝拉汀结构类型的石蒜科生物碱，分别命名为 carltonine A-C（-）。分离出足够数量且以前未测试过的化合物，评估了它们对体外乙酰胆碱酯酶（AChE；E.C. 3.1.1.7）、丁酰胆碱酯酶（BuChE；E.C. 3.1.1.8）和脯氨酰寡肽酶（POP；E.C. 3.4.21.26）的抑制活性。新描述的生物碱 carltonine A（）和 carltonine B（）具有抑制人 BuChE（BUChE）的活性，IC 值分别为 913 ± 20 nM 和 31 ± 1 nM。这两种化合物对 BuChE 的抑制具有选择性抑制模式，对 AChE 的抑制具有出色的选择性，超过 100。体外数据进一步得到了在 BuChE 的活性部位中对活性生物碱 和 的计算机模拟研究的支持。
