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淡黄木犀草(野生木犀草)及7种分离得到的黄酮醇苷的综合评价:采用体外和计算机模拟方法测定抗氧化活性、抗阿尔茨海默病活性、抗糖尿病活性和细胞毒性作用。

Comprehensive evaluation of Reseda lutea L. (Wild Mignonette) and 7 isolated flavonol glycosides: determination of antioxidant activity, anti-Alzheimer, antidiabetic and cytotoxic effects with in vitro and in silico methods.

作者信息

Kiziltaş Hatice

机构信息

Department of Pharmacy Services, Van Vocational School of Health Services, Van Yüzüncü Yıl University Van, Turkey.

出版信息

Turk J Chem. 2022 Apr 8;46(4):1185-1198. doi: 10.55730/1300-0527.3426. eCollection 2022.

Abstract

In this study, anticholinergic, antidiabetic, antioxidant and cytotoxic activities of L. () were determined. Ethanol extracts of (EERL) and water extract of (WERL) were prepared for biochemical analysis. The antioxidant capacities of EERL and WERL were evaluated with 6 different methods. In addition, acetylcholinesterase (AChE), α-amylase and glycosidase enzyme inhibition by EERL were measured. According to the results, EERL exhibited high inhibition effects against α-amylase, α-glycosidase and AChE enzymes. The IC values of EERL against AChE (2.21 μg/mL), α-glycosidase (1.38 μg/mL), and α-amylase (0.11 μg/mL) were determined. Also, high cytotoxic effect of EERL was observed on human lung cancer cell lines (A549) with an value of 3.58 ± 1.10 μg/mL. The affinities of 7 kaempferol and isorhamnetin rhamnopyranoside molecules, previously isolated from , for AChE, α-amylase and, α-glycosidase were determined by molecular docking studies. Molecular docking results supported the in vitro results of the study. The results showed that the aerial parts of have effective antioxidant, anticholinergic, antidiabetic and cytotoxic activities. This research will form the basis for further studies about usage for drug development.

摘要

在本研究中,测定了L.()的抗胆碱能、抗糖尿病、抗氧化和细胞毒性活性。制备了L.()的乙醇提取物(EERL)和水提取物(WERL)用于生化分析。采用6种不同方法评估了EERL和WERL的抗氧化能力。此外,还测定了EERL对乙酰胆碱酯酶(AChE)、α-淀粉酶和糖苷酶的抑制作用。结果显示,EERL对α-淀粉酶、α-糖苷酶和AChE酶表现出较高的抑制作用。测定了EERL对AChE(2.21μg/mL)、α-糖苷酶(1.38μg/mL)和α-淀粉酶(0.11μg/mL)的IC值。同时,观察到EERL对人肺癌细胞系(A549)具有较高的细胞毒性作用,IC值为3.58±1.10μg/mL。通过分子对接研究确定了先前从L.()中分离出的7种山奈酚和异鼠李素鼠李糖苷分子对AChE、α-淀粉酶和α-糖苷酶的亲和力。分子对接结果支持了该研究的体外实验结果。结果表明,L.()的地上部分具有有效的抗氧化、抗胆碱能、抗糖尿病和细胞毒性活性。本研究将为进一步研究L.()在药物开发中的应用奠定基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8bfa/10395699/e2a495180955/turkjchem-46-4-1185f1.jpg

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