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 82-99and 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.
Five distinct organic compounds with protected and unprotected phenolic hydroxyl groups were screened for their a-glucosidase inhibitory potential. Of these compounds, 2,4,6-trihydroxybenzaldehyde (THB) showed the strongest noncompetitive a-glucosidase inhibition (IC 50 = 4.60 lM) and the most powerful antioxidant activity (DPPH assay) (IC 50 = 71.4 lM) in vitro. In in vivo studies, THB significantly reduced blood glucose levels in normal and diabetic rats after glucose load compared to maltose load.
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