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Α-Glucosidase Inhibition Assay of Galbanic Acid and It Amide Derivatives: New Excellent Semi-Synthetic Α-Glucosidase Inhibitors Publisher Pubmed



Mohammadikhanaposhtani M1 ; Sayahi MH2, 3 ; Yazzaf R4 ; Dastyafteh N4 ; Halimi M5 ; Iraji A6, 7, 8 ; Dadgar A4 ; Mojtabavi S9 ; Faramarzi MA9 ; Palimi M10 ; Mirzazadeh R11 ; Larijani B4 ; Delnavazi MR12 ; Mahdavi M4, 13
Authors
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Authors Affiliations
  1. 1. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
  2. 2. Department of Chemistry, Payame Noor University, Tehran, Iran
  3. 3. Chemistry Department, College of Science, Shahid Chamran University of Ahvaz, Ahvaz, 61357-4-3169, Iran
  4. 4. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
  5. 5. Department of Biology, Babol Branch, Islamic Azad University, Babol, Iran
  6. 6. Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
  7. 7. Central Research Laboratory, Shiraz University of Medical Sciences, Shiraz, Iran
  8. 8. Liosa Pharmed Parseh Company, Shiraz, Iran
  9. 9. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  10. 10. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  11. 11. Biochemistry Department, Pasteur Institute of Iran, Tehran, Iran
  12. 12. Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  13. 13. Diabetes Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran

Source: Bioorganic Chemistry Published:2024


Abstract

α-Glucosidase inhibitory activity of galbanic acid and its new amide derivatives 3a–n were investigated. Galbanic acid and compounds 3a–n showed excellent anti-α-glucosidase activity with IC50 values ranging from 0.3 ± 0.3 μM to 416.0 ± 0.2 μM in comparison to positive control acarbose with IC50 value of = 750.0 ± 5.6. In the kinetic study, the most potent compound 3h demonstrated a competitive mode of inhibition with Ki = 0.57 µM. The interaction of the most potent compound 3h with the α-glucosidase was further elaborated by in vitro Circular dichroism assessment and in silico molecular docking and Molecular dynamics studies. Compound 3h was also non-cytotoxic on human normal cells. In silico study on pharmacokinetics and toxicity profile of the most potent galbanic acid derivatives demonstrated that these compounds are valuable lead compounds for further study in order to achieve new anti-diabetic agents. © 2024 Elsevier Inc.
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