Design, synthesis and anti-diabetic activity of some novel xanthone derivatives targeting alpha-glucosidase

Authors

  • Partha Sarathi Bairy Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, Assam 786004
  • Aparoop Das Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, Assam 786004
  • Lalit Mohan Nainwal Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, Assam 786004
  • Tapan Kumar Mohanta Free Major of Natural Science, School of Basic Studies, Yeungnam University, 280, Daehak Gyeongsan, Gyeongsanbuk 712749
  • Mukesh Kumar Kumawat Anand College of Pharmacy, Keetham, Agra, Uttar Pradesh 282007
  • Pradyumna Kishore Mohapatra Regional Medical Research Centre, NE Region, Indian Council of Medical Research, Post Box. 105, Dibrugarh, 786001, Assam
  • Pratap Parida Regional Medical Research Centre, NE Region, Indian Council of Medical Research, Post Box. 105, Dibrugarh, 786 001, Assam

DOI:

https://doi.org/10.3329/bjp.v11i2.25851

Keywords:

Anti-diabetic, Design, Synthesis, Xanthone derivative, ?-Glucosidase

Abstract

Twenty eight xanthone derivatives were designed and docked into the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM) by considering Miglitol as standard drug. Most of the molecules showed excellent docking scores and docking interaction as compared to the binding cavity of the standard molecule. The five best scoring ligands were synthesized and characterized by a number of analytical and spectroscopic techniques. The molecules were screened for the in vivo antidiabetic activity in streptozotocin (STZ) induced diabetic animal model in Wistar rats. Compound P4 showed the most prominent inhibition among others. The synthesized compounds reported significant (p< 0.01) effect of lowering glucose levels in the blood compared to miglitol as a standard alpha-glucosidase inhibitor.

Video Clips of Methodology:

Synthesis of hydroxyxanthones: 7 min 2 sec   Click to watch

Induction of diabetes: 1 min 39 sec   Click to watch 

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Published

2016-03-16

How to Cite

Bairy, P. S., A. Das, L. M. Nainwal, T. K. Mohanta, M. K. Kumawat, P. K. Mohapatra, and P. Parida. “Design, Synthesis and Anti-Diabetic Activity of Some Novel Xanthone Derivatives Targeting Alpha-Glucosidase”. Bangladesh Journal of Pharmacology, vol. 11, no. 2, Mar. 2016, pp. 308-1, doi:10.3329/bjp.v11i2.25851.

Issue

Section

Research Articles