Department of Food and Life Science, Pukyong National University, Busan 48513, Korea.
Department of Food Science and Human Nutrition, Chonbuk National University, Jeonju 54896, Korea.
Molecules. 2019 Feb 12;24(3):649. doi: 10.3390/molecules24030649.
In the search for natural products having a dual inhibitory action on diabetes and Alzheimer's disease, this study investigated the activity of different parts of Korean thistle ( var. (Maxim.) Matsum), and its fractional constituents by in vitro enzymatic and in silico molecular docking studies. has been used as a traditional medicine for the treatment of several diseases. The ethyl acetate and dichloromethane fractions of a leaf extract showed α-glucosidase and BACE1 inhibitory activity, respectively. Furthermore, the isolated compound, luteolin, exhibited concentration-dependent non-competitive inhibition against both α-glucosidase and BACE1 (IC = 51.27 ± 1.23 and 13.75 ± 0.26 μM; value = 52.04 and 14.76 μM, respectively). Moreover, docking studies showed that luteolin formed a strong hydrogen bond with the peripheral binding amino acid residues, and hydrophobic interactions with the α-glucosidase and BACE1 enzymes. Therefore, Korean thistle may act as an important dietary supplement against diabetes and Alzheimer's disease, especially the leaves, because of the preponderance of the active component, luteolin, making Korean thistle a promising candidate for more detailed in vitro and in vivo studies.
在寻找同时具有糖尿病和阿尔茨海默病双重抑制作用的天然产物的过程中，本研究通过体外酶活性和计算机分子对接研究，考察了朝鲜蓟（var. (Maxim.) Matsum）不同部位及其分级成分的活性。朝鲜蓟作为一种传统药物，已被用于治疗多种疾病。叶提取物的乙酸乙酯和二氯甲烷部分分别显示出α-葡萄糖苷酶和 BACE1 抑制活性。此外，分离得到的化合物木樨草素对α-葡萄糖苷酶和 BACE1 表现出浓度依赖性的非竞争性抑制作用（IC = 51.27 ± 1.23 和 13.75 ± 0.26 μM； 值= 52.04 和 14.76 μM）。此外，对接研究表明，木樨草素与外周结合氨基酸残基形成强氢键，与 α-葡萄糖苷酶和 BACE1 酶形成疏水相互作用。因此，朝鲜蓟可能是一种重要的针对糖尿病和阿尔茨海默病的膳食补充剂，特别是叶部，因为活性成分木樨草素含量较高，使朝鲜蓟成为更详细的体外和体内研究的有前途的候选物。
