Abstract

The inhibitory properties of epicatechin-(4β,8)-epicatechingallate (B2-3’-O-gallate), epicatechin gallate (ECG), and epicatechin (EC) isolated from Rhodiola crenulata toward maltase and sucrase were investigated. The half-maximal inhibitory concentration (IC50) values for maltase were as follows: B2-3’-O-gallate (1.73 ± 1.37 μM), ECG (3.64 ± 2.99 μM), and EC (6.25 ± 1.84 μM). Inhibition kinetic assays revealed the inhibition constants (Ki) of the mixed-competitive inhibitors of maltase, as follows: B2-3’-O-gallate (1.99 ± 0.02 μM), ECG (3.14 ± 0.04 μM), and EC (7.02 ± 0.26 μM). These compounds also showed a strong inhibitory activity toward sucrase, and the IC50 values of B2-3’-O-gallate, ECG, and EC were 6.91 ± 3.41, 18.27 ± 3.99, and 18.91 ± 3.66 μM, respectively. Inhibition kinetic assays revealed the inhibition constants (Ki) of the mixed-competitive inhibitors of sucrase as follows: B2-3’-O-gallate (6.05 ± 0.04 μM), ECG (8.58 ± 0.08 μM), and EC (13.72 ± 0.15 μM). Overall, these results suggest that B2-3’-O-gallate, ECG, and EC are potent maltase and sucrase inhibitors.

Highlights

  • Over the past three decades, the number of people with diabetes mellitus has quadrupled, with the result being that diabetes mellitus is the ninth leading cause of death worldwide

  • Results and Potent maltase and sucrase inhibitors have been considered for use for treating diabetes mellitus

  • Maltase and Sucrase Inhibitory Activity of B2-3’-O-gallate, Epicatechin gallate (ECG), EC, and Quercetin derived from R. crenulata

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Summary

Introduction

Over the past three decades, the number of people with diabetes mellitus has quadrupled, with the result being that diabetes mellitus is the ninth leading cause of death worldwide. 1 in 11 adults have diabetes mellitus, and roughly 90% of those cases are type 2. The most pronounced symptom of diabetes mellitus is an abnormal postprandial increase in blood glucose levels [1,2]. It is widely believed that control over postprandial hyperglycemia is crucial to the effective treatment of diabetes mellitus [3]. It is well known that dietary carbohydrates are broken down into monosaccharides by hydrolytic enzymes, α-glucosidases, which are absorbed into the intestinal brush border membrane. The final step of carbohydrate digestion can be catalyzed by α-glucosidases. A number of physiologically important enzymes are involved in the process of digesting dietary carbohydrates [4,5]

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