Fernández-Galleguillos Carlos, Romero-Parra Javier, Puerta Adrián, Padrón José M, Simirgiotis Mario J
Instituto de Farmacia, Facultad de Ciencias, Universidad Austral de Chile, Campus Isla Teja, Valdivia 5090000, Chile.
Departamento de Química Orgánica y Fisicoquímica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Olivos 1007, Casilla 233, Santiago 6640022, Chile.
Metabolites. 2022 Feb 18;12(2):188. doi: 10.3390/metabo12020188.
This research aims to identify the alkaloid profile and to evaluate the enzyme inhibitory potential and antiproliferative effects of the Amaryllidaceae plant . The alkaloid extracts from bulbs and leaves were analyzed using ultrahigh performance liquid chromatography orbitrap mass spectrometry (UHPLC-Orbitrap-MS) analysis. A total of 70 alkaloids were detected in the extracts. The enzyme inhibition potential against cholinesterases (AChE: acetylcholinesterase, and BChE butyrylcholinesterase) and tyrosinase were studied. Bulbs displayed the best IC values against AChE (4.29 ± 0.03 µg/mL) and BChE (18.32 ± 0.03 µg/mL). These results were consistent with docking experiments with selected major compounds in the active sites of enzymes, while no activity was observed against tyrosinase enzyme. Antiproliferative effects were investigated against human cervical (HeLa), lung (A549, SW1573), colon (WiDr), and breast (HBL-100, T-47D) tumor cell lines. Bulbs and leaves were active in all cell lines (GI < 2.5 µg/mL). These findings suggest that the endemic Chilean plant contains diverse types of bioactive alkaloids with antiproliferative activities and inhibitory effects with potential therapeutic applications for neurodegenerative diseases.
本研究旨在确定石蒜科植物的生物碱谱，并评估其酶抑制潜力和抗增殖作用。使用超高效液相色谱-轨道阱质谱（UHPLC-Orbitrap-MS）分析对鳞茎和叶片中的生物碱提取物进行了分析。在提取物中总共检测到70种生物碱。研究了其对胆碱酯酶（AChE：乙酰胆碱酯酶和BChE：丁酰胆碱酯酶）和酪氨酸酶的酶抑制潜力。鳞茎对AChE（4.29±0.03μg/mL）和BChE（18.32±0.03μg/mL）显示出最佳的IC值。这些结果与所选主要化合物在酶活性位点的对接实验一致，而未观察到对酪氨酸酶的活性。研究了对人宫颈（HeLa）、肺（A549、SW1573）、结肠（WiDr）和乳腺（HBL-100、T-47D）肿瘤细胞系的抗增殖作用。鳞茎和叶片在所有细胞系中均有活性（GI<2.5μg/mL）。这些发现表明，这种智利本土植物含有多种具有抗增殖活性和抑制作用的生物活性生物碱，对神经退行性疾病具有潜在的治疗应用价值。
