Anti-acetylcholinesterase activity and antioxidant properties of extracts and fractions of <i>Carpolobia lutea</i>

<b>Context:</b> There is an unmet need to discover new treatments for Alzheimer’s disease. This study determined the anti-acetylcholinesterase (AChE) activity, DPPH free radical scavenging and antioxidant properties of <i>Carpolobia lutea</i> G. Don (Polygalaceae). <b>Objective:</b> The objective of this study is to quantify <i>C. lutea</i> anti-AChE, DPPH free radical scavenging, and antioxidant activities and cell cytotoxicity. <b>Materials and methods:</b> Plant stem, leaves and roots were subjected to sequential solvent extractions, and screened for anti-AChE activity across a concentration range of 0.02–200 μg/mL. Plant DPPH radical scavenging activity, reducing power, and total phenolic and flavonoid contents were determined, and cytotoxicity evaluated using human hepatocytes. <b>Results:</b><i>Carpolobia lutea</i> exhibited concentration-dependent anti-AChE activity. The most potent inhibitory activity for the stem was the crude ethanol extract and hexane stem fraction oil (IC₅₀ = 140 μg/mL); for the leaves, the chloroform leaf fraction (IC₅₀ = 60 μg/mL); and for roots, the methanol, ethyl acetate and aqueous root fractions (IC₅₀ = 0.3–3 μg/mL). Dose-dependent free radical scavenging activity and reducing power were observed with increasing stem, leaf or root concentration. Total phenolic contents were the highest in the stem: ∼632 mg gallic acid equivalents/g for a hexane stem fraction oil. Total flavonoid content was the highest in the leaves: ∼297 mg quercetin equivalents/g for a chloroform leaf fraction. At 1 μg/mL, only the crude ethanol extract oil was significantly cytotoxic to hepatocytes. <b>Discussion and conclusions:</b><i>Carpolobia lutea</i> possesses anti-AChE activity and beneficial antioxidant capacity indicative of its potential development as a treatment of Alzheimer’s and other diseases characterized by a cholinergic deficit.

**背景：** 目前针对阿尔茨海默病仍存在尚未满足的新型治疗药物研发需求。本研究针对*Carpolobia lutea* G. Don（远志科Polygalaceae）的抗乙酰胆碱酯酶（anti-acetylcholinesterase, AChE）活性、DPPH自由基清除能力及抗氧化特性展开分析。
**研究目的：** 本研究旨在定量测定*C. lutea*的抗AChE活性、DPPH自由基清除活性、抗氧化活性以及细胞毒性。
**材料与方法：** 对该植物的茎、叶及根采用连续溶剂萃取法进行处理，并在0.02~200 μg/mL的浓度范围内筛选其抗AChE活性。此外，本研究测定了样品的DPPH自由基清除活性、还原能力、总酚类与总黄酮含量，并采用人肝细胞评估其细胞毒性。
**结果：** *Carpolobia lutea*呈现出浓度依赖性的抗AChE活性。其中，茎部活性最强的成分为粗乙醇提取物与正己烷茎馏分油（半数抑制浓度IC₅₀=140 μg/mL）；叶片中活性最强的成分为氯仿叶馏分（IC₅₀=60 μg/mL）；根部活性最强的成分为甲醇、乙酸乙酯及水相根馏分（IC₅₀=0.3~3 μg/mL）。随着茎、叶或根提取物浓度升高，样品呈现出剂量依赖性的自由基清除活性与还原能力。茎部的总酚类含量最高，正己烷茎馏分油的总酚类含量约为632 mg没食子酸当量/g。叶片的总黄酮含量最高，氯仿叶馏分的总黄酮含量约为297 mg槲皮素当量/g。在浓度为1 μg/mL时，仅粗乙醇提取物油对肝细胞具有显著细胞毒性。
**讨论与结论：** *Carpolobia lutea*具备抗AChE活性与有益的抗氧化能力，这表明其有望开发为阿尔茨海默病及其他以胆碱能缺陷为特征的疾病的治疗药物。

搜集汇总

背景与挑战

背景概述

该数据集研究了Carpolobia lutea植物提取物和组分的抗乙酰胆碱酯酶活性及抗氧化特性，旨在探索其作为阿尔茨海默病等疾病治疗药物的潜力。研究通过体外实验评估了不同溶剂提取物的抑制乙酰胆碱酯酶活性、自由基清除能力和细胞毒性，并发现部分组分具有显著的浓度依赖性活性。数据集包含实验原始数据和补充图表，适用于生物化学、植物药理学等相关领域的研究。