琥珀酰亚胺酮衍生物抗糖尿病潜能的探索:体外和体内方法

IF 3.8 4区 工程技术 Q2 CHEMISTRY, MULTIDISCIPLINARY
Ayesha Talib, Shafiq Ali Shah, Muhammad Saeed Jan, Muhammad Zaeem Ahsan, Abubakr Munir, Ishfaq A. Bukhari, Halima Sadia, Taghrid S. Alomar, Najla AlMasoud, Abdur Rauf
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引用次数: 0

摘要

摘要糖尿病(DM)是近年来最具挑战性的疾病之一,是危及生命的疾病。α-葡萄糖苷酶和α-淀粉酶是治疗糖尿病的最佳靶酶。为此,我们探索了许多具有酮类功能的琥珀酰亚胺。首先,我们对这些化合物进行了体外分析。在体外实验中,化合物1和4对这两种酶均有良好的抑制作用。这些化合物对α-葡萄糖苷酶的ic50分别为3.69和1.526µg·mL−1。在α-淀粉酶抑制实验中,化合物1的IC 50值为1.07µg·mL - 1,化合物4的IC 50值为0.115µg·mL - 1,表现出良好的抑制潜力。在体外分析的基础上,进一步对有效化合物进行体内分析。在体内分析之前,检查了毒性谱,确认化合物在1,500µg·kg−1时是安全的。然后,这些化合物在糖尿病小鼠模型中进行了体内抗糖尿病潜力的研究。以格列本脲为标准药物,通过体内分析探讨了化合物1和4的不同浓度。实验组和对照组分别于第0 ~ 15天测定血糖水平。同样,我们也探索了化合物1和4在0-120 min以格列本脲为标准药物的口服葡萄糖耐量试验。因此,具有酮段的琥珀酰亚胺显示出良好的抗糖尿病潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Exploration of ketone derivatives of succinimide for their antidiabetic potential: In vitro and in vivo approaches
Abstract Diabetes mellitus (DM) is one of the most challenging diseases among all the other diseases in the recent era, and it is a life-threatening disorder. The best enzymes to target for treating DM are α-glucosidase and α-amylase. For this purpose, we explored numerous succinimides with ketone functionalities. First, we explored these compounds for their in vitro analysis. Compounds 1 and 4 exhibited excellent inhibition of both enzymes in in vitro studies. These compounds displayed excellent activity with IC 50 values of 3.69 and 1.526 µg·mL −1 against the α-glucosidase enzyme. In the α-amylase inhibitory assay, compound 1 has shown excellent potential with an IC 50 value of 1.07 µg·mL −1 and compound 4 with an IC 50 value of 0.115 µg·mL −1 . Based on the in vitro analysis, the potent compounds were further subjected to their in vivo analysis. Before the in vivo analysis, the toxicity profile was checked, and it was confirmed that the compounds were safe at 1,500 µg·kg −1 . Then, these compounds were subjected for their in vivo anti-diabetic potential in a mouse model of diabetes. Various concentrations of compounds 1 and 4 were explored by in vivo analysis using glibenclamide as a standard drug. The blood glucose level of the tested and control groups was measured at 0 to 15 days accordingly. Similarly, we also explored compounds 1 and 4 for the oral glucose tolerance test at 0–120 min using glibenclamide as the standard drug. Hence, the succinimide having ketone moiety displayed excellent potential against diabetes.
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来源期刊
Green Processing and Synthesis
Green Processing and Synthesis CHEMISTRY, MULTIDISCIPLINARY-ENGINEERING, CHEMICAL
CiteScore
6.70
自引率
9.30%
发文量
78
审稿时长
7 weeks
期刊介绍: Green Processing and Synthesis is a bimonthly, peer-reviewed journal that provides up-to-date research both on fundamental as well as applied aspects of innovative green process development and chemical synthesis, giving an appropriate share to industrial views. The contributions are cutting edge, high-impact, authoritative, and provide both pros and cons of potential technologies. Green Processing and Synthesis provides a platform for scientists and engineers, especially chemists and chemical engineers, but is also open for interdisciplinary research from other areas such as physics, materials science, or catalysis.
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