Carrera de Bioquímica, Departamento de Ciencias Químicas y Recursos Naturales, Facultad de Ingeniería y Ciencias, Universidad de La Frontera, Temuco, Chile.
Laboratorio de Química Ecológica, Departamento de Ciencias Químicas y Recursos Naturales, Universidad de La Frontera, Temuco, Chile.
Nat Prod Res. 2022 Mar;36(5):1370-1374. doi: 10.1080/14786419.2021.1872075. Epub 2021 Jan 18.
Alkaloid profiles from plants collected in Chile were examined by GC-MS to assess their inhibitory activity on acetylcholinesterase (AChE) using and methodologies. The alkaloid extract was roughly separated by column chromatography on silica gel. AChE inhibitory activities from extracts and purified alkaloids were tested by the Ellman method and a molecular docking study was performed to assess the interaction between AChE and purified alkaloids. Sixteen alkaloids were found from hexane and chloroform extracts, and three were isolated and identified as buphanidrine, acetylcaranine and lycorine. Chloroform extract showed the greatest AChE inhibitory activity with IC value 8.89 µg/mL, whereas buphanidrine exhibited the highest inhibitory activity, with IC value 17.56 µg/mL. Inhibition kinetics showed that buphanidrine acts as a mixed inhibitor and molecular docking supports this inhibition mechanism. Overall, our study supports the potential use of as an alkaloid source with AChE inhibitory activity.[Formula: see text].
从智利采集的植物中的生物碱谱通过 GC-MS 进行了检查，以使用 和 方法评估它们对乙酰胆碱酯酶（AChE）的抑制活性。生物碱提取物通过硅胶柱色谱进行了大致分离。用 Ellman 法测试提取物和纯化生物碱的 AChE 抑制活性，并进行了分子对接研究，以评估 AChE 与纯化生物碱之间的相互作用。从正己烷和氯仿提取物中发现了十六种生物碱，并分离和鉴定了三种，即布非那嗪、乙酰卡那宁和石蒜碱。氯仿提取物对 AChE 的抑制活性最强，IC 值为 8.89 µg/mL，而布非那嗪的抑制活性最高，IC 值为 17.56 µg/mL。抑制动力学表明布非那嗪作为一种混合抑制剂起作用，分子对接支持这种抑制机制。总的来说，我们的研究支持将 作为具有 AChE 抑制活性的生物碱来源的潜在用途。
