The Structure-activity Relationship Of Dietary Polyphenols Inhibiting α-glucosidases

The number of patient who has obesity and type 2 diabetes are increase rapidly with continuous development of the world,that situation has caused by excessive intake of carbohydrates and lipids.As a chronic endocrine disease,diabetes is mainly characterized by hyperglycemia and disorder of cellular metabolism.This is mainly due to the disorder of insulin secretion and the decrease of insulin sensitivity in diabetic patients.Long-term diabetes can cause a series of complications such as hypertension,retinopathy,renal failure,neuropathy,etc.It also accelerates myocardial infarction,arteriosclerosis,cerebral infarction,an d arterial occlusive disease of the extremities.The treatment of diabetes in modern medical is control the blood sugar level by use insulin or other drugs.The starch of human diet can’t be absorbed directly,they need digestive enzymes break their molecular chain that can absorbed by human body.α-glucosidases is a common digestive enzymes that can degrade macromolecules of starches and make their structure smaller.Polyphenols are secondary metabolites of plants and they have lots of potential positive effects on human health,such as anti-oxidation and anti-cardiovascular disease.Since 1990,scientists found polyphenols are benefit to treatment of diabetes that attracted great interest among researchers.Diabetes is a chronic endocrine disease characterized high blood glucose levels.Polyphenols as α-glucosidases inhibitors can decrease blood glucose levels by binding digestive enzyme.This article focus on the structure-activity relationship of polyphenols and α-glucosidase by compare their IC50 values.The structure-activity relationship between polyphenols and α-glucosidase are the following:(1)The most of hydroxylation on A-ring and B-ring of polyphenols can enhance their inhibitory activity against α-glucosidase.(2)The hydroxylation on C2 of C-ring on polyphenols reduce their inhibitory activity.(3)The methoxylation on polyphenols will decrease their inhibitory activity,and polyphenols show no inhibitory activity against α-glucosidase when they have multiple methyl groups as substituents.(4)Almost all of glycosylation on polyphenols weaken their inhibitory activity against α-glucosidase.(5)The chiral structures have obvious effect on inhibition rate of catechins against α-glucosidase.