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苯硫基乙基苯甲酸酯衍生物的抗糖尿病、抗氧化和抗肥胖作用及其对α-淀粉酶的分子对接研究。

Antidiabetic, antioxidant, and anti-obesity effects of phenylthio-ethyl benzoate derivatives, and molecular docking study regarding α-amylase enzyme.

机构信息

Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, P.O. Box 7, 00970, Nablus, Palestine.

Chemometrics and Analytical Chemistry, Modern Testing Services, Povinostr. 52, 86153, Augsburg, Germany.

出版信息

Sci Rep. 2022 Feb 24;12(1):3108. doi: 10.1038/s41598-022-07188-2.

DOI:10.1038/s41598-022-07188-2
PMID:35210523
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8873473/
Abstract

In addition to their wide therapeutic application, benzoates and benzoic acid derivatives are the most commonly utilized food preservatives. The purpose of this study was to estimate the antioxidant, anti-diabetic, and anti-obesity activities of four 2-(phenylthio)-ethyl benzoate derivatives utilizing standard biomedical assays. The results revealed that the 2a compound has potent antidiabetic activity through the inhibition of α-amylase and α-glycosidase with IC doses of 3.57 ± 1.08 and 10.09 ± 0.70 µg/ml, respectively, compared with the positive control acarbose (IC = 6.47 and 44.79 µg/ml), respectively. In addition, by utilizing the β-carotene linoleic acid and DPPH methods, the 2a compound showed the highest antioxidant activity compared with positive controls. Moreover, the 2a compound showed potential anti-lipase activity with an IC dose of 107.95 ± 1.88 µg/ml compared to orlistat (IC = 25.01 ± 0.78 µg/ml). A molecular docking study was used to understand the interactions between four derivatives of (2-(phenylthio)-ethyl benzoate with α-amylase binding pocket. The present study concludes that the 2a compound could be exploited for further antidiabetic, antioxidant, and anti-obesity preclinical and clinical tests and design suitable pharmaceutical forms to treat these global health problems.

摘要

除了广泛的治疗应用外，苯甲酸及其衍生物还是最常用的食品防腐剂。本研究旨在利用标准的生物医学测定法评估四种 2-(苯硫基)-乙基苯甲酸酯衍生物的抗氧化、抗糖尿病和抗肥胖活性。结果表明，与阳性对照阿卡波糖（IC = 6.47 和 44.79 µg/ml）相比，化合物 2a 通过抑制α-淀粉酶和α-糖苷酶，具有很强的抗糖尿病活性，IC 剂量分别为 3.57 ± 1.08 和 10.09 ± 0.70 µg/ml。此外，利用β-胡萝卜素亚油酸和 DPPH 法，化合物 2a 与阳性对照相比显示出最高的抗氧化活性。此外，化合物 2a 显示出潜在的抗脂肪酶活性，IC 剂量为 107.95 ± 1.88 µg/ml，而奥利司他（IC = 25.01 ± 0.78 µg/ml）。通过分子对接研究来理解四种 2-(苯硫基)-乙基苯甲酸酯衍生物与α-淀粉酶结合口袋的相互作用。本研究得出结论，化合物 2a 可用于进一步的抗糖尿病、抗氧化和抗肥胖的临床前和临床测试，并设计合适的药物形式来治疗这些全球性健康问题。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/be53/8873473/98055a7dfbb8/41598_2022_7188_Fig8_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/be53/8873473/98055a7dfbb8/41598_2022_7188_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/be53/8873473/fa03dfe8dda4/41598_2022_7188_Fig1_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/be53/8873473/3523949dda28/41598_2022_7188_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/be53/8873473/1511e6a0a659/41598_2022_7188_Fig6_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/be53/8873473/98055a7dfbb8/41598_2022_7188_Fig8_HTML.jpg

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