In vivo and in silico evaluations of a synthetic pyrano[3,2-c]quinoline derivative as a potent anti-diabetic agent

被引:1
|
作者
Zare, Nafiseh [1 ]
Bandarian, Fatemeh [2 ]
Esfahani, Ensieh Nasli [2 ]
Larijani, Bagher [3 ]
Mahdavi, Mohammad [3 ]
Mohammadi-Khanaposhtani, Maryam [4 ]
Najafzadehvarzi, Hossein [4 ]
机构
[1] Islamic Azad Univ, Fac Pharm, Ayatollah Amoli Branch, Amol, Iran
[2] Univ Tehran Med Sci, Endocrinol & Metab Clin Sci Inst, Diabet Res Ctr, Tehran, Iran
[3] Univ Tehran Med Sci, Endocrinol & Metab Clin Sci Inst, Endocrinol & Metab Res Ctr, Tehran, Iran
[4] Babol Univ Med Sci, Hlth Res Inst, Cellular & Mol Biol Res Ctr, Babol, Iran
关键词
Synthetic; Diabetes; Wistar rat; Streptozotocin; Pyrano[3,2-c]quinoline; ALPHA-GLUCOSIDASE; DESIGN;
D O I
10.1007/s40200-023-01355-6
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
Background 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 alpha-glucosidase inhibitor in preliminary in vitro assays, for further evaluation in an in vivo anti-diabetic context.Methods 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.Results 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 alpha-glucosidase active site and exhibited favorable pharmacokinetic properties.Conclusion 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.
引用
收藏
页码:239 / 249
页数:11
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