Abstract
Problem statement: Glycosidase inhibitors are vital sources for the treatment of diabetes type II with a special importance in pharmacology, food industry and biotechnology, since for diabetes control, different diets and drugs, especially herbal medicines are recommended in this era. Approach: While screening for the potent natural glycosidase inhibitors, we found the fruits of Chaenomeles sinensis (C. sinensis), as the most effective glycosidase inhibitor. The crude 80% methanolic extract of the fruits and its n-hexane, methylene chloride, ethyl acetate, n-butanol and aqueous fractions were further investigated for α-glucosidase, β-glucosidase, α-galactosidase and β-galactosidase enzyme inhibition activities. Results: All the C. sinensis extracts showed remarkable α-glucosidase and β-glucosidase inhibitory activities (at a concentration of 5 μg 210 μL reaction-1) ranging from 82-99 and 5-85%, respectively. Among all the inhibition studies, n-butanol fraction demonstrated the highest (99%) α-glucosidase inhibitory activity, whereas minor α-galactosidase (18-35%) and β-galactosidase (10-34%) inhibitions were examined in all the fractions of C. sinensis. Conclusion: C. sinensis fruits may prove as potent natural anti-diabetic source with noteworthy α-glucosidase and β-glucosidase inhibitions, because the inhibition of these enzymes provide a strong biochemical basis for the management of type II diabetes by controlling glucose absorption. These results provide intense rationale for further animal and clinical studies.
Highlights
Diabetes Mellitus (DM) is a major chronic life-threatening disorder, in which homeostasis of carbohydrate and lipid metabolism is improperly regulated by the pancreatic hormone, insulin; resulting in an increased blood glucose level
The crude extract of C. sinensis and its various fractions were evaluated at 5 μg 210 μL−1 well concentrations for α-glucosidase, β-glucosidase, α-galactosidase and β-galactosidase enzyme inhibition
All the C. sinensis extracts showed remarkable α-glucosidase inhibitory activities ranging from 82-99% and are detailed here (Fig. 1): n-butanol (99%) > water (97%) >
Summary
Diabetes Mellitus (DM) is a major chronic life-threatening disorder, in which homeostasis of carbohydrate and lipid metabolism is improperly regulated by the pancreatic hormone, insulin; resulting in an increased blood glucose level. There has been renewed interest in the DM treatment using herbal drugs as they are generally non-toxic and World Health Organization has recommended the evaluation of the effectiveness of plants in condition where we lack safe modern drugs. Plant derivatives with hypoglycaemic properties have been used in folk medicine from very ancient time[3]. Despite the introduction of hypoglycaemic agents from natural and synthetic sources, diabetes and its secondary complications continue to be a major medical problem to people[4]. Traditional herbal therapies by indigenous systems of medicine for treating this ailment are being intensively explored
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