Cespedes Carlos L, Balbontin Cristian, Avila Jose G, Dominguez Mariana, Alarcon Julio, Paz Cristian, Burgos Viviana, Ortiz Leandro, Peñaloza-Castro Ignacio, Seigler David S, Kubo Isao
Biochemistry and Phytochemical-Ecology Lab, Department of Basic Science, Facultad de Ciencias, Universidad del Bio Bio, Chillan, Chile.
Plant Production Department, Instituto Nacional de Investigaciones Agropecuarias, Quilamapu, Chillan, Chile.
Food Chem Toxicol. 2017 Nov;109(Pt 2):984-995. doi: 10.1016/j.fct.2017.05.009. Epub 2017 May 10.
It is reported in this study the effect of isolates from leaves of Aristotelia chilensis as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase enzymes. The aim of the paper was to evaluate the activity of A. chilensis towards different enzymes. In addition to pure compounds, extracts rich in alkaloids and phenolics were tested. The most active F5 inhibited AChE (79.5% and 89.8% at 10.0 and 20.0 μg/mL) and against BChE (89.5% and 97.8% at 10.0 and 20.0 μg/mL), showing a strong mixed-type inhibition against AChE and BChE. F3 (a mixture of flavonoids and phenolics acids), showed IC of 90.7 and 59.6 μg/mL of inhibitory activity against AChE and BChE, inhibiting the acetylcholinesterase competitively. Additionally, F3 showed and high potency as tyrosinase inhibitor with IC at 8.4 μg/mL. Sample F4 (anthocyanidins and phenolic composition) presented a complex, mixed-type inhibition of tyrosinase with a IC of 39.8 μg/mL. The findings in this investigation show that this natural resource has a strong potential for future research in the search of new phytotherapeutic treatments for cholinergic deterioration ailments avoiding the side effects of synthetic drugs. This is the first report as cholinesterases and tyrosinase inhibitors of alkaloids and phenolics from A. chilensis leaves.
本研究报道了智利草莓叶提取物作为乙酰胆碱酯酶（AChE）、丁酰胆碱酯酶（BChE）和酪氨酸酶抑制剂的作用。本文的目的是评估智利草莓对不同酶的活性。除了纯化合物外，还测试了富含生物碱和酚类的提取物。活性最高的F5对AChE有抑制作用（在10.0和20.0μg/mL时分别为79.5%和89.8%），对BChE也有抑制作用（在10.0和20.0μg/mL时分别为89.5%和97.8%），对AChE和BChE表现出强烈的混合型抑制作用。F3（黄酮类化合物和酚酸的混合物）对AChE和BChE的抑制活性IC分别为90.7和59.6μg/mL，对乙酰胆碱酯酶有竞争性抑制作用。此外，F3作为酪氨酸酶抑制剂表现出高效性，IC为8.4μg/mL。样品F4（花青素和酚类成分）对酪氨酸酶呈现复杂的混合型抑制作用，IC为39.8μg/mL。本研究结果表明，这种自然资源在寻找治疗胆碱能衰退疾病的新植物疗法方面具有很大的研究潜力，可避免合成药物的副作用。这是关于智利草莓叶生物碱和酚类作为胆碱酯酶和酪氨酸酶抑制剂的首次报道。
