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尼泊尔树叶的抗氧化、α-淀粉酶抑制及降血糖活性:体外、体内及计算机模拟综合研究方法

Antioxidant, Alpha-Amylase Inhibitory and Hypoglycemic Activity of Leaves from Nepal: An Integrated In Vitro, In Vivo, and In Silico Approach.

作者信息

Rawal Prakash, Pandey Bipindra, Yadav Ram Kishor, Panta Sushil

机构信息

School of Health and Allied Sciences Pokhara University Pokhara Nepal.

Department of Pharmacy Madan Bhandari Academy of Health Sciences Hetauda Nepal.

出版信息

Food Sci Nutr. 2024 Dec 26;13(1):e4672. doi: 10.1002/fsn3.4672. eCollection 2025 Jan.

Abstract

In 2019, diabetes mellitus affected 9.3% of the global population and accounted for one in nine adult deaths. Plant-based antioxidants neutralize harmful free radicals, mitigate oxidative stress, and significantly prevent diabetes and its complications. This study evaluated the in vitro antioxidant, alpha-amylase inhibitory, in vivo oral hypoglycemic, and antidiabetic potential of () leaf extract. Mice ( = 25) were divided into five groups after a 16-h fast with access to water. The groups received distilled water (normal control), metformin (100 mg/kg, standard), or ethanolic extract at 100, 250, or 500 mg/kg to compare the antidiabetic potential of the extract with that of the control. Fasting blood glucose levels were measured in tail vein blood before the experiment and at 30, 60, and 120 min post-administration to evaluate the hypoglycemic activity of the extract and standard drug. The ethanolic extract exhibited dose-dependent alpha-amylase inhibition (IC value 0.136 mg/mL) and significant hypoglycemic effects, reducing blood glucose levels similar to those of the standard drugs voglibose and metformin. The maximum blood glucose reduction was 17.99% and 15.74% in the normal and glucose-loaded mice, respectively, at 500 mg/kg within 120 min. analysis shows, polymatin B and chlorogenic acid demonstrating the highest binding affinity of -8.2 and -7.2 kcal/mol, respectively, in PPAR-γ (3G9E). Polymatin B and chlorogenic acid showed strong binding affinities of -7.3 and -7.5 kcal/mol, respectively, in alpha-amylase (4W93). These findings indicate that possesses significant hypoglycemic and antioxidant properties, suggesting its potential as an antidiabetic agent, warranting further clinical research.

摘要

2019年,糖尿病影响了全球9.3%的人口,占成年死亡人数的九分之一。植物性抗氧化剂可中和有害自由基,减轻氧化应激,并显著预防糖尿病及其并发症。本研究评估了()叶提取物的体外抗氧化、α-淀粉酶抑制、体内口服降糖和抗糖尿病潜力。禁食16小时并可饮水后的小鼠(n = 25)被分为五组。这些组分别接受蒸馏水(正常对照)、二甲双胍(100 mg/kg,标准品)或100、250或500 mg/kg的乙醇提取物,以比较提取物与对照的抗糖尿病潜力。在实验前以及给药后30、60和120分钟测量尾静脉血中的空腹血糖水平,以评估提取物和标准药物的降糖活性。乙醇提取物表现出剂量依赖性的α-淀粉酶抑制作用(IC值为0.136 mg/mL)和显著的降糖作用,降低血糖水平的效果与标准药物伏格列波糖和二甲双胍相似。在120分钟内,500 mg/kg剂量下正常小鼠和葡萄糖负荷小鼠的最大血糖降低率分别为17.99%和15.74%。分析表明,在PPAR-γ(3G9E)中,polymatin B和绿原酸分别表现出最高的结合亲和力,为-8.2和-7.2 kcal/mol。在α-淀粉酶(4W93)中,polymatin B和绿原酸分别表现出-7.3和-7.5 kcal/mol的强结合亲和力。这些发现表明()具有显著的降糖和抗氧化特性,表明其作为抗糖尿病药物的潜力,值得进一步的临床研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fd2/11717019/0655a59da19f/FSN3-13-e4672-g003.jpg

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