对一种具有二氢吡喃并[3,2-c]喹啉骨架的优秀合成α-葡萄糖苷酶抑制剂的抗糖尿病和抗血脂评估。
anti-diabetic and anti-lipidemic evaluations of an excellent synthetic α-glucosidase inhibitor with dihydropyrano[3,2-c]quinoline skeleton.
作者信息
Mohammadi-Khanaposhtani Maryam, Bakhtiari Navid, Bandarian Fatemeh, Larijani Bagher, Mahdavi Mohammad, Najafzadehvarzi Hossein
机构信息
Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran.
Faculty of Pharmacy, Islamic Azad University, Ayatollah Amoli Branch, Amol, Iran.
出版信息
J Diabetes Metab Disord. 2024 Oct 5;23(2):2375-2384. doi: 10.1007/s40200-024-01505-4. eCollection 2024 Dec.
OBJECTIVES
The assay is a key step in the development of a new bioactive compound as a lead drug structure. Based on importance of α-glucosidase inhibitors in the control of blood glucose level (BGL) in diabetes, in the present work, 3-amino-1-(4-chlorophenyl)-12-oxo-11,12-dihydro-1-benzo[]pyrano[3,2-]quinoline-2-carbonitrile () that showed excellent inhibitory activity on the yeast form of α-glucosidase was selected for anti-diabetic assay.
METHODS
The anti-diabetic and anti-lipidemic effects of this synthetic compound were evaluated using by a streptozotocin (STZ)-induced diabetic Wistar rat model. docking study of was performed by Atodock tools and absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of this compound was predicted by PreADMT online software.
RESULTS
The obtained results revealed that selected compound showed a significant anti-diabetic effect on diabetic rats. In vivo anti-lipidemic assay also demonstrated that had favorable effects on cholesterol and LDL levels. Furthermore, studies showed that interacted with key residues of the α-glucosidase active site and had good pharmacokinetic and toxicity properties.
CONCLUSION
In summary, anti-hyperglycemic effects of was confirmed by study. However, more evaluations are needed to introduce as a lead drug compound.
目的
该测定是将一种新的生物活性化合物开发为先导药物结构的关键步骤。基于α-葡萄糖苷酶抑制剂在控制糖尿病患者血糖水平（BGL）中的重要性，在本研究中，选择了对酵母形式的α-葡萄糖苷酶显示出优异抑制活性的3-氨基-1-（4-氯苯基）-12-氧代-11,12-二氢-1-苯并[]吡喃并[3,2 -]喹啉-2-腈（）进行抗糖尿病测定。
方法
使用链脲佐菌素（STZ）诱导的糖尿病Wistar大鼠模型评估该合成化合物的抗糖尿病和抗血脂作用。通过Atodock工具对进行对接研究，并通过PreADMT在线软件预测该化合物的吸收、分布、代谢、排泄和毒性（ADMET）特性。
结果
所得结果表明，所选化合物对糖尿病大鼠显示出显著的抗糖尿病作用。体内抗血脂测定还表明，对胆固醇和低密度脂蛋白水平有良好影响。此外，研究表明与α-葡萄糖苷酶活性位点的关键残基相互作用，并且具有良好的药代动力学和毒性特性。
结论
总之，通过研究证实了的降血糖作用。然而，需要更多评估才能将作为先导药物化合物引入。
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