Abstract
Inhibition of α-glucosiase and the associated reduction of glucose absorption is an attractive approach for decreasing postprandial hyperglycemia and for the discovery of potent antidiabetic agents. One of the most important sources of potential α-glucosiase inhibitors represents the class of polyphenols. This paper aims to evaluate previous herbal polyphenol-rich extracts plan on the management of diabetes mellitus, to address their α-glucosidase inhibitory activity. Polyphenol-rich extracts from thirteen widely used traditionally anti-diabetic plants in Asia and Mediterranean regions were evaluated for their potential α-glucosidaseinhibitory activity. Among these evaluated plants, 10 were much stronger than that of acarbose standard. Punica granatum manifested the highest inhibitory activity with IC50 at 3.59 ± 0.11 μg/mL, followed by Psidium guajava with IC50 at 8.08 ± 0.10 μg/mL and Cinnamomum zeylanicum with IC50 at 9.87.08 ± 0.14 μg/mLA. A high correlation (r=0.65, p<0.001) was observed between α-glucosidase inhibition and total phenolic content of all plants. Punica granatum, P. guajava, C. zeylanicum and Ziziphus spina-christi had also the highest total phenolic content. Extracts for the above studied plant species may potentially replace acarbose in its current clinical use in improving post-prandial glycaemic control in type 2 diabetics. As a result, these polyphenol-rich extracts potentially offer a complementary approach to develop functional food and potential antidiabetic agents.
Highlights
A multifactorial disease affecting over 347 million people worldwide, is characterized by hyperglycemia resulting from defects in insulin secretion, insulin action, or both [1]
Α-Glucosidase inhibitors are a class of drugs used to treat noninsulin dependent diabetes by inhibiting α-glucosidase (EC 3.2.1.20, α-D-glucoside glucohydrolase), a membrane-bound intestinal enzyme that catalyze the hydrolysis of the α -glycosidic bond of oligosaccharides to liberate glucose
Inhibition of α-Glucosidase and the associated reduction of glucose absorption is an attractive approach for the discovery of potent agents. α-Glucosidase, a key enzyme for carbohydrate digestion, has been recognized as a therapeutic target for modulation of postprandial hyperglycemia, which is the earliest metabolic abnormality to occur in type 2 diabetes [4]
Summary
A multifactorial disease affecting over 347 million people worldwide, is characterized by hyperglycemia resulting from defects in insulin secretion, insulin action, or both [1]. There has been a striking emergence of noninsulin-dependent diabetes mellitus (type 2 diabetes) as a major health problem in populations undergoing modernization of life-style, both in developing nations and in developed countries. Α-Glucosidase inhibitors are a class of drugs used to treat noninsulin dependent diabetes by inhibiting α-glucosidase (EC 3.2.1.20, α-D-glucoside glucohydrolase), a membrane-bound intestinal enzyme that catalyze the hydrolysis of the α -glycosidic bond of oligosaccharides to liberate glucose. Liberated glucose is absorbed from the intestine and contributes to postprandial hyperglycemia. Α-Glucosidase inhibitors prevent or delay the hydrolysis or absorption of carbohydrates and reduce post prandial hyperglycemia, making such inhibitors useful in the management of type 2 diabetes [2]. Acarbose, voglibose and miglitol are three such α -glucosidase inhibitors used clinically to control blood glucose levels of patients, they can cause negative gastrointestinal symptoms [3,4]
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