PDF(Pubmed)
Abstract：
UNASSIGNED: The in vivo 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 (2-BDBPQD), identified as an exemplary α-glucosidase inhibitor in preliminary in vitro assays, for further evaluation in an in vivo anti-diabetic context.
UNASSIGNED: The in vivo anti-diabetic effect of 2-BDBPQD 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. In silico studies, encompassing docking studies and pharmacokinetic predictions of 2-BDBPQD, were conducted.
UNASSIGNED: The results obtained indicated a significant reduction in blood glucose levels with 2-BDBPQD treatment compared to acarbose. However, no significant effects on the lipid profile were observed. In silico studies revealed that 2-BDBPQD interacted with key residues in the α-glucosidase active site and exhibited favorable pharmacokinetic properties.
UNASSIGNED: In summary, the study demonstrated the in vivo anti-hyperglycemic activity of 2-BDBPQD. Nevertheless, further in vivo evaluations are recommended to comprehensively assess its potential as a new drug for the treatment of diabetes.
UNASSIGNED: The in vivo anti-diabetic effect of 2-BDBPQD 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. In silico studies, encompassing docking studies and pharmacokinetic predictions of 2-BDBPQD, were conducted.
UNASSIGNED: The results obtained indicated a significant reduction in blood glucose levels with 2-BDBPQD treatment compared to acarbose. However, no significant effects on the lipid profile were observed. In silico studies revealed that 2-BDBPQD interacted with key residues in the α-glucosidase active site and exhibited favorable pharmacokinetic properties.
UNASSIGNED: In summary, the study demonstrated the in vivo anti-hyperglycemic activity of 2-BDBPQD. Nevertheless, further in vivo evaluations are recommended to comprehensively assess its potential as a new drug for the treatment of diabetes.
摘要：
■新型化合物的体内评估是开发新药的关键步骤。在这项研究中,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（2-BDBPQD），在初步的体外试验中被确定为示例性的α-葡萄糖苷酶抑制剂，用于体内抗糖尿病背景下的进一步评估。
使用链脲佐菌素(STZ)诱导的糖尿病Wistar大鼠模型评估2-BDBPQD的体内抗糖尿病作用。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大鼠血脂谱的影响。在硅研究中，包括2-BDBPQD的对接研究和药代动力学预测，进行了。
■获得的结果表明，与阿卡波糖相比，2-BDBPQD治疗的血糖水平显着降低。然而,对血脂没有显著影响。计算机研究表明，2-BDBPQD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特性。
■总之，该研究证明了2-BDBPQD的体内抗高血糖活性。然而，我们建议进一步进行体内评估,以全面评估其作为糖尿病治疗新药的潜力.
使用链脲佐菌素(STZ)诱导的糖尿病Wistar大鼠模型评估2-BDBPQD的体内抗糖尿病作用。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大鼠血脂谱的影响。在硅研究中，包括2-BDBPQD的对接研究和药代动力学预测，进行了。
■获得的结果表明，与阿卡波糖相比，2-BDBPQD治疗的血糖水平显着降低。然而,对血脂没有显著影响。计算机研究表明，2-BDBPQD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特性。
■总之，该研究证明了2-BDBPQD的体内抗高血糖活性。然而，我们建议进一步进行体内评估,以全面评估其作为糖尿病治疗新药的潜力.
