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作为胰脂肪酶抑制剂的磨碎提取物的分子对接研究及体外活性

Molecular Docking Studies and In Vitro Activity of Mill Extracts as Pancreatic Lipase Inhibitors.

作者信息

Grande Fedora, Marrelli Mariangela, Amodeo Valentina, Occhiuzzi Maria Antonietta, Pinzaru Iulia, Fucile Mary, Dehelean Cristina Adriana, Alexa Ersilia, Conforti Filomena, Statti Giancarlo

机构信息

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Cosenza, Italy.

Faculty of Pharmacy, Victor Babes University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., 300041 Timisoara, Romania.

出版信息

Antioxidants (Basel). 2024 Jan 26;13(2):160. doi: 10.3390/antiox13020160.

DOI:10.3390/antiox13020160
PMID:38397758
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10885981/
Abstract

Obesity is a risk factor for the onset of chronic diseases. One of the most promising approaches to treating obesity consists of reducing dietary fat absorption using extracts from plants because they contain phenolic compounds, especially flavonoids. , belonging to the Rhamnaceae family, is one of the five species belonging to the genus. Herein, the aerial parts of the plant were extracted with methanol through the pressurized cyclic solid-liquid extraction using the Naviglio extractor. The extracts were analyzed with High Performance Thin Layer Chromatography and investigated for their in vitro biological potential. The phytochemical analysis revealed that rutin has been shown to be the most abundant flavonoid component. The best antiradical activity was observed for the fruit extract with an IC value of 53.41 ± 1.24 µg/mL. This extract also has a better inhibitory capacity on lipid peroxidation evaluated at a different time of incubation. Potent lipase inhibitor activity of the extract from fruits was also demonstrated with in vitro experiments. This property can be attributed to a direct interaction of main components of extract with the human pancreatic enzyme as demonstrated by the results of molecular docking experiments conducted on the crystallographic structures of lipase.

摘要

肥胖是慢性疾病发病的一个风险因素。治疗肥胖最有前景的方法之一是使用植物提取物来减少膳食脂肪吸收,因为植物提取物含有酚类化合物,尤其是黄酮类化合物。鼠李属植物属于鼠李科,是该属五个物种之一。在此,使用纳维利奥提取器通过加压循环固液萃取法用甲醇提取该植物的地上部分。提取物用高效薄层色谱法进行分析,并研究其体外生物学潜力。植物化学分析表明,芦丁是最丰富的黄酮类成分。果实提取物的抗自由基活性最佳,IC值为53.41±1.24µg/mL。在不同孵育时间评估时,该提取物对脂质过氧化也具有更好的抑制能力。体外实验还证明了果实提取物具有强大的脂肪酶抑制活性。如对脂肪酶晶体结构进行分子对接实验的结果所示,这一特性可归因于提取物主要成分与人类胰腺酶的直接相互作用。

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Meat Sci. 2024 Jan;207:109362. doi: 10.1016/j.meatsci.2023.109362. Epub 2023 Oct 11.
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Paliurus spina-christi Mill fruit extracts improve glucose uptake and activate the insulin signaling pathways in HepG2 insulin-resistant cells.五倍子果实提取物可改善 HepG2 胰岛素抵抗细胞的葡萄糖摄取并激活胰岛素信号通路。
BMC Complement Med Ther. 2023 May 8;23(1):151. doi: 10.1186/s12906-023-03977-y.
3
Phytochemical Profile and Biological Activities of Different Extracts of Three Parts of : A Linkage between Structure and Ability.
三种植物不同部位不同提取物的植物化学特征及生物活性:结构与能力之间的联系
Antioxidants (Basel). 2023 Jan 23;12(2):255. doi: 10.3390/antiox12020255.
4
Polyphenols from Citrus Tacle Extract Endowed with HMGCR Inhibitory Activity: An Antihypercholesterolemia Natural Remedy.柑橘塔克提取物中的多酚具有 HMGCR 抑制活性:一种抗高胆固醇血症的天然疗法。
Molecules. 2021 Sep 21;26(18):5718. doi: 10.3390/molecules26185718.
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Bioactive component analysis and investigation of antidiabetic effect of Jerusalem thorn (Paliurus spina-christi) fruits in diabetic rats induced by streptozotocin.生物活性成分分析及新疆沙棘果实对链脲佐菌素诱导糖尿病大鼠降糖作用的研究。
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