以及对一种合成吡喃并[3,2-c]喹啉衍生物作为一种强效抗糖尿病药物的评估。
and evaluations of a synthetic pyrano[3,2-c]quinoline derivative as a potent anti-diabetic agent.
作者信息
Zare Nafiseh, Bandarian Fatemeh, Esfahani Ensieh Nasli, Larijani Bagher, Mahdavi Mohammad, Mohammadi-Khanaposhtani Maryam, Najafzadehvarzi Hossein
机构信息
Faculty of Pharmacy, Ayatollah Amoli Branch, Islamic Azad University, Amol, Iran.
Diabetes Research Center, Endocrinology and Metabolism Clinical Sciences Institute, University of Medical Sciences, Tehran, Iran.
出版信息
J Diabetes Metab Disord. 2023 Dec 11;23(1):809-815. doi: 10.1007/s40200-023-01355-6. eCollection 2024 Jun.
BACKGROUND
The assessment of a novel compound is a pivotal step in the development of a new drug. In this study, we selected 1-(2-bromophenyl)-1,11-dihydro-3H-benzo[h]pyrano[3,2-c]quinoline-3,12(2H)-dione (), identified as an exemplary α-glucosidase inhibitor in preliminary in vitro assays, for further evaluation in an anti-diabetic context.
METHODS
The anti-diabetic effect of was assessed using a streptozotocin (STZ)-induced diabetic Wistar rat model. Recognizing the relevance of lipid factors in diabetes, we also investigated the impact of this compound on the lipid profile of diabetic Wistar rats. studies, encompassing docking studies and pharmacokinetic predictions of 2-BDBPQD, were conducted.
RESULTS
The results obtained indicated a significant reduction in blood glucose levels with treatment compared to acarbose. However, no significant effects on the lipid profile were observed. studies revealed that interacted with key residues in the α-glucosidase active site and exhibited favorable pharmacokinetic properties.
CONCLUSION
In summary, the study demonstrated the anti-hyperglycemic activity of . Nevertheless, further evaluations are recommended to comprehensively assess its potential as a new drug for the treatment of diabetes.
背景
新型化合物的评估是新药研发中的关键步骤。在本研究中，我们选择了1-(2-溴苯基)-1,11-二氢-3H-苯并[h]吡喃并[3,2-c]喹啉-3,12(2H)-二酮（），该化合物在初步体外试验中被鉴定为一种典型的α-葡萄糖苷酶抑制剂，用于在抗糖尿病背景下进行进一步评估。
方法
使用链脲佐菌素（STZ）诱导的糖尿病Wistar大鼠模型评估的抗糖尿病作用。认识到脂质因素在糖尿病中的相关性，我们还研究了该化合物对糖尿病Wistar大鼠脂质谱的影响。进行了包括2-BDBPQD的对接研究和药代动力学预测在内的研究。
结果
与阿卡波糖相比，治疗后血糖水平显著降低。然而，未观察到对脂质谱有显著影响。研究表明与α-葡萄糖苷酶活性位点的关键残基相互作用，并表现出良好的药代动力学性质。
结论
总之，该研究证明了的抗高血糖活性。然而，建议进行进一步评估以全面评估其作为治疗糖尿病新药的潜力。
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