Mithun Singh Rajput*, Rashmi Dahima
School of Pharmacy, Devi Ahilya Vishwavidyalaya, Takshashila Campus, Khandwa Road, Indore-452001, M.P., India
*Address for Correspondence
Dr. Mithun Singh Rajput,
Postdoctoral Fellow,
School of Pharmacy, Devi Ahilya Vishwavidyalaya, Takshashila Campus, Khandwa Road, Indore-452001, M.P., India.
Abstract
Background: α-Glucosidase is a membrane bound intestinal enzyme that transforms polysaccharides into simple absorbable monosaccharides and glucose within the gastrointestinal tract and thus absorbed glucose contributes to postprandial hyperglycemia. Therefore, inhibition of α-glucosidase is a prominent therapeutic strategy to control diabetes mellitus. Objective: In this study, an attempt has been made to investigate the ability of dimethyl cardamonin (DMC) to inhibit enzyme α-glucosidase as well as in combination with an antidiabetic drug, acarbose and to study inhibition kinetics of DMC. Material and Methods: The inhibitory effect of various dose of DMC (0.5–100.0μg/ml) on α-glucosidase was assessed using microtitre plate assay in vitro, so as to evaluate its antidiabetic potential. An enzyme kinetic analysis was performed and the type of inhibition was determined by Lineweaver-Burk plot obtained by plotting velocities of reaction and substrate concentrations reciprocally. Results: DMC exhibited satisfactory inhibitory activity against α-glucosidase with IC50 value 87.56μg/ml, which was much higher than acarbose (IC50 value of 262.39μg/ml). The Lineweaver–Burk plots for α-glucosidase inhibition by DMC indicated a noncompetitive enzyme inhibition. It was found that acarbose combined with DMC at all the three concentrations (¼IC50, ½IC50 and IC50) resulted in significant (p<0.05) inhibition compared with the individual compounds at the same concentration indicating synergistic inhibitory activity against α-glucosidase. Conclusion: The present study provides the first evidence that DMC could find application as α-glucosidase inhibitor. This study could facilitate effective utilization of DMC as an oral antidiabetic drug or functional food ingredient with a promising role in the formulation of medicines and nutrition supplements.
Keywords: α-glucosidase; chalcones; diabetes; dimethyl cardamonin
