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Korean Thistle (Cirsium japonicum var. maackii (Maxim.) Matsum.): A Potential Dietary Supplement against Diabetes and Alzheimer’s Disease

机译:高丽蓟(Cirsium japonicum var。maackii(Maxim。)Matsum。):潜在的膳食补充剂可预防糖尿病和阿尔茨海默氏病

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摘要

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 (Cirsium japonicum var. maackii (Maxim.) Matsum), and its fractional constituents by in vitro enzymatic and in silico molecular docking studies. Cirsium maackii 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 (IC50 = 51.27 ± 1.23 and 13.75 ± 0.26 μM; Ki 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.
机译:在寻找对糖尿病和阿尔茨海默氏病具有双重抑制作用的天然产物时,本研究通过体外酶促和化学方法研究了朝鲜蓟(Cirsium japonicum var。maackii(Maxim。)Matsum)不同部位的活性及其部分成分。在计算机分子对接研究中。大果枸杞已被用作治疗多种疾病的传统药物。叶提取物的乙酸乙酯和二氯甲烷馏分分别显示α-葡萄糖苷酶和BACE1抑制活性。此外,分离出的化合物木犀草素对α-葡萄糖苷酶和BACE1均表现出浓度依赖性的非竞争性抑制作用(IC50分别为51.27±1.23和13.75±0.26μM; Ki值分别为52.04和14.76μM)。此外,对接研究表明木犀草素与周围结合的氨基酸残基形成强氢键,并与α-葡萄糖苷酶和BACE1酶发生疏水相互作用。因此,由于活性成分木犀草素的优势,高丽蓟可能成为抵抗糖尿病和阿尔茨海默氏病(尤其是叶子)的重要膳食补充剂,这使得高丽蓟成为有希望的候选人,可以进行更详细的体内和体外研究。

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