Parquetina nigrescens (Afzel.) Bullock 果实的抗糖尿病活性评估及其抗糖尿病剂的硅学鉴定。

IF 2.3 Q3 BIOCHEMICAL RESEARCH METHODS Bioinformatics and Biology Insights Pub Date : 2024-01-26 eCollection Date: 2024-01-01 DOI:10.1177/11779322231223857
Marcus D Ayoola, Yetunde B Ogundeko, Temiloluwa D Obanleowo, Deborah O Omole, Blessing N Chukwu, Kolade O Faloye
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引用次数: 0

摘要

这项研究调查了 Parquetina nigrescens 果实提取物的抗糖尿病潜力,目的是证明其在尼日利亚部分地区的民间抗糖尿病用途是合理的。该植物提取物的急性毒性试验采用 Lorke 法进行评估。在α-淀粉酶、α-葡萄糖苷酶、葡萄糖和链脲佐菌素诱导的糖尿病大鼠模型中,以阿卡波糖和格列本脲(5 毫克/千克)为阳性对照,按不同剂量对其抗血糖活性进行了检测。为确定提取物中的抗糖尿病成分并阐明其可能的作用机制,进行了分子对接研究。提取物的估计中位致死剂量(LD50)高于 5000 毫克/千克。在α-淀粉酶、α-葡萄糖苷酶研究中,该提取物与阿卡波糖具有相似的浓度依赖性活性。在葡萄糖诱导的高血糖模型中,200 毫克/千克的提取物是最有效的剂量,在 1 至 4 小时内,其抗高血糖活性与格列本脲 (5 毫克/千克)相当(P > .05);在链脲佐菌素诱导的糖尿病大鼠模型中,100 和 200 毫克/千克的提取物在第 4 至 14 天的活性相当(P > 0.05),在第 4 至 7 天明显优于格列本脲。提取物的正己烷和乙酸乙酯馏分(浓度均为 200 毫克/千克)活性最高,在所有时间点的活性均与格列本脲相当。分子对接研究发现,异野漆树苷是对α-淀粉酶(结合能为-9.1 kcal/mol)、α-葡萄糖苷酶(-9.4 kcal/mol)、钠-葡萄糖共转运体-2(-9.5 kcal/mol)、过氧化物酶体增殖激活受体伽马(-10.3 kcal/mol)、11β-羟类固醇脱氢酶(-10.8 kcal/mol)和二肽基肽酶 IV(-9.4 kcal/mol)。黑茶藨子果实提取物的抗糖尿病研究结果证明了其在民族医药中用于糖尿病治疗的合理性。
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Evaluation of the Antidiabetic Activities of the Fruit of Parquetina nigrescens (Afzel.) Bullock and In Silico Identification of Its Antidiabetic Agent.

The study investigated the antidiabetic potentials of the fruit extract of Parquetina nigrescens with the aim of justifying its folkloric antidiabetic usage in some part of Nigeria. Acute toxicity test of the plant extract was assessed using Lorke's method. Its antidiabetic activities were assayed in α-amylase, α-glucosidase, glucose, and streptozotocin-induced diabetic rats' models at various doses with acarbose and glibenclamide (5 mg/kg) as positive controls. Molecular docking studies were performed to identify the antidiabetic constituent of the extract and elucidate its possible mechanism of action. The estimated median lethal dose (LD50) of the extract was above 5000 mg/kg. In the α-amylase, α-glucosidase study, the extract elicited concentration-dependent activity similar to acarbose. In the glucose-induced hyperglycaemic model, 200 mg/kg of the extract was the most effective dose with comparable (P > .05) antihyperglycaemic activity to glibenclamide (5 mg kg) at 1 to 4 h. Also in the streptozotocin-induced diabetic rats model, 100 and 200 mg/kg of the extract gave comparable (P > 0.05) activity on days 4 to 14 that were significantly better than that of glibenclamide on days 4 to 7. The n-hexane and ethylacetate fractions of the extract, both at 200 mg/kg were the most active with comparable activity to glibenclamide at all time points. The molecular docking studies identified isorhoifolin as the best binder against alpha amylase with binding energy (-9.1 kcal/mol), alpha glucosidase (-9.4 kcal/mol), sodium-glucose cotransporter-2 (-9.5 kcal/mol), peroxisome proliferator activated receptor gamma (-10.3 kcal/mol), 11β-Hydroxysteroid dehydrogenase (-10.8 kcal/mol), and dipeptidyl peptidase IV (-9.4 kcal/mol). The results of the antidiabetic study of P nigrescence fruit extract justified its usage in ethnomedicne in diabetes management.

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来源期刊
Bioinformatics and Biology Insights
Bioinformatics and Biology Insights BIOCHEMICAL RESEARCH METHODS-
CiteScore
6.80
自引率
1.70%
发文量
36
审稿时长
8 weeks
期刊介绍: Bioinformatics and Biology Insights is an open access, peer-reviewed journal that considers articles on bioinformatics methods and their applications which must pertain to biological insights. All papers should be easily amenable to biologists and as such help bridge the gap between theories and applications.
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